JPH0336806B2 - - Google Patents
Info
- Publication number
- JPH0336806B2 JPH0336806B2 JP57198253A JP19825382A JPH0336806B2 JP H0336806 B2 JPH0336806 B2 JP H0336806B2 JP 57198253 A JP57198253 A JP 57198253A JP 19825382 A JP19825382 A JP 19825382A JP H0336806 B2 JPH0336806 B2 JP H0336806B2
- Authority
- JP
- Japan
- Prior art keywords
- parts
- manufactured
- minutes
- microhydrogel
- centipoise
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 229920001296 polysiloxane Polymers 0.000 claims description 66
- -1 polysiloxane Polymers 0.000 claims description 56
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 50
- 229920005645 diorganopolysiloxane polymer Polymers 0.000 claims description 29
- 229910052697 platinum Inorganic materials 0.000 claims description 25
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 23
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 22
- 239000004615 ingredient Substances 0.000 claims description 12
- 230000001070 adhesive effect Effects 0.000 claims description 10
- 239000000853 adhesive Substances 0.000 claims description 9
- 150000003058 platinum compounds Chemical class 0.000 claims description 7
- 239000000203 mixture Substances 0.000 description 51
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 33
- 239000000047 product Substances 0.000 description 32
- 239000002585 base Substances 0.000 description 25
- 229940079593 drug Drugs 0.000 description 23
- 239000003814 drug Substances 0.000 description 23
- 239000012153 distilled water Substances 0.000 description 18
- NPERTKSDHFSDLC-UHFFFAOYSA-N ethenol;prop-2-enoic acid Chemical compound OC=C.OC(=O)C=C NPERTKSDHFSDLC-UHFFFAOYSA-N 0.000 description 17
- 239000004745 nonwoven fabric Substances 0.000 description 14
- 229920000298 Cellophane Polymers 0.000 description 12
- 239000003795 chemical substances by application Substances 0.000 description 12
- 238000010521 absorption reaction Methods 0.000 description 11
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 10
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 10
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 9
- 230000000694 effects Effects 0.000 description 9
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- 210000003491 skin Anatomy 0.000 description 9
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- 238000004132 cross linking Methods 0.000 description 7
- 239000004698 Polyethylene Substances 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 230000003110 anti-inflammatory effect Effects 0.000 description 6
- 229920001577 copolymer Polymers 0.000 description 6
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- 229920000573 polyethylene Polymers 0.000 description 6
- 239000004372 Polyvinyl alcohol Substances 0.000 description 5
- 230000035597 cooling sensation Effects 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 238000010438 heat treatment Methods 0.000 description 5
- 229960000905 indomethacin Drugs 0.000 description 5
- 229960001047 methyl salicylate Drugs 0.000 description 5
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- 229920002451 polyvinyl alcohol Polymers 0.000 description 5
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 4
- 239000005995 Aluminium silicate Substances 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 239000005062 Polybutadiene Substances 0.000 description 4
- 235000012211 aluminium silicate Nutrition 0.000 description 4
- 239000003054 catalyst Substances 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- DNTGGZPQPQTDQF-XBXARRHUSA-N crotamiton Chemical compound C/C=C/C(=O)N(CC)C1=CC=CC=C1C DNTGGZPQPQTDQF-XBXARRHUSA-N 0.000 description 4
- 229960003338 crotamiton Drugs 0.000 description 4
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 4
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 description 4
- 229960000991 ketoprofen Drugs 0.000 description 4
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 description 4
- 230000002688 persistence Effects 0.000 description 4
- 229920002857 polybutadiene Polymers 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 3
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 3
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 3
- NLHHRLWOUZZQLW-UHFFFAOYSA-N Acrylonitrile Chemical compound C=CC#N NLHHRLWOUZZQLW-UHFFFAOYSA-N 0.000 description 3
- 241000723346 Cinnamomum camphora Species 0.000 description 3
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 3
- 108010010803 Gelatin Proteins 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 3
- 239000003513 alkali Substances 0.000 description 3
- 229910052783 alkali metal Inorganic materials 0.000 description 3
- 230000000202 analgesic effect Effects 0.000 description 3
- 230000001760 anti-analgesic effect Effects 0.000 description 3
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 3
- 229930008380 camphor Natural products 0.000 description 3
- 229960000846 camphor Drugs 0.000 description 3
- 239000013065 commercial product Substances 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 229960002390 flurbiprofen Drugs 0.000 description 3
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 description 3
- 229920000159 gelatin Polymers 0.000 description 3
- 239000008273 gelatin Substances 0.000 description 3
- 235000019322 gelatine Nutrition 0.000 description 3
- 235000011852 gelatine desserts Nutrition 0.000 description 3
- 230000035807 sensation Effects 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 229920000247 superabsorbent polymer Polymers 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- 238000011282 treatment Methods 0.000 description 3
- 229920003169 water-soluble polymer Polymers 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 2
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 description 2
- HBTAOSGHCXUEKI-UHFFFAOYSA-N 4-chloro-n,n-dimethyl-3-nitrobenzenesulfonamide Chemical compound CN(C)S(=O)(=O)C1=CC=C(Cl)C([N+]([O-])=O)=C1 HBTAOSGHCXUEKI-UHFFFAOYSA-N 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 2
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- FOGXJPFPZOHSQS-AYVLZSQQSA-N Hydrocortisone butyrate propionate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)CC)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O FOGXJPFPZOHSQS-AYVLZSQQSA-N 0.000 description 2
- 108010076876 Keratins Proteins 0.000 description 2
- 102000011782 Keratins Human genes 0.000 description 2
- 239000004677 Nylon Substances 0.000 description 2
- MITFXPHMIHQXPI-UHFFFAOYSA-N Oraflex Chemical compound N=1C2=CC(C(C(O)=O)C)=CC=C2OC=1C1=CC=C(Cl)C=C1 MITFXPHMIHQXPI-UHFFFAOYSA-N 0.000 description 2
- 239000004100 Oxytetracycline Substances 0.000 description 2
- 239000004743 Polypropylene Substances 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- VIROVYVQCGLCII-UHFFFAOYSA-N amobarbital Chemical compound CC(C)CCC1(CC)C(=O)NC(=O)NC1=O VIROVYVQCGLCII-UHFFFAOYSA-N 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 230000002921 anti-spasmodic effect Effects 0.000 description 2
- 229940124575 antispasmodic agent Drugs 0.000 description 2
- 230000004888 barrier function Effects 0.000 description 2
- 229960005274 benzocaine Drugs 0.000 description 2
- CNBGNNVCVSKAQZ-UHFFFAOYSA-N benzydamine Chemical compound C12=CC=CC=C2C(OCCCN(C)C)=NN1CC1=CC=CC=C1 CNBGNNVCVSKAQZ-UHFFFAOYSA-N 0.000 description 2
- KVYGGMBOZFWZBQ-UHFFFAOYSA-N benzyl nicotinate Chemical compound C=1C=CN=CC=1C(=O)OCC1=CC=CC=C1 KVYGGMBOZFWZBQ-UHFFFAOYSA-N 0.000 description 2
- 229960004311 betamethasone valerate Drugs 0.000 description 2
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 description 2
- XSIFPSYPOVKYCO-UHFFFAOYSA-N butyl benzoate Chemical compound CCCCOC(=O)C1=CC=CC=C1 XSIFPSYPOVKYCO-UHFFFAOYSA-N 0.000 description 2
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 2
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- 229920002678 cellulose Polymers 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- FOCAUTSVDIKZOP-UHFFFAOYSA-N chloroacetic acid Chemical compound OC(=O)CCl FOCAUTSVDIKZOP-UHFFFAOYSA-N 0.000 description 2
- 239000004927 clay Substances 0.000 description 2
- DGBIGWXXNGSACT-UHFFFAOYSA-N clonazepam Chemical compound C12=CC([N+](=O)[O-])=CC=C2NC(=O)CN=C1C1=CC=CC=C1Cl DGBIGWXXNGSACT-UHFFFAOYSA-N 0.000 description 2
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- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 description 2
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- IZEKFCXSFNUWAM-UHFFFAOYSA-N dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 description 2
- 239000004744 fabric Substances 0.000 description 2
- PGBHMTALBVVCIT-VCIWKGPPSA-N framycetin Chemical compound N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CN)O2)N)O[C@@H]1CO PGBHMTALBVVCIT-VCIWKGPPSA-N 0.000 description 2
- 229960004580 glibenclamide Drugs 0.000 description 2
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 description 2
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- LNEPOXFFQSENCJ-UHFFFAOYSA-N haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
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- 229910003475 inorganic filler Inorganic materials 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
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- KSCKTBJJRVPGKM-UHFFFAOYSA-N octan-1-olate;titanium(4+) Chemical compound [Ti+4].CCCCCCCC[O-].CCCCCCCC[O-].CCCCCCCC[O-].CCCCCCCC[O-] KSCKTBJJRVPGKM-UHFFFAOYSA-N 0.000 description 2
- 229960000625 oxytetracycline Drugs 0.000 description 2
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- IWVCMVBTMGNXQD-PXOLEDIWSA-N oxytetracycline Chemical compound C1=CC=C2[C@](O)(C)[C@H]3[C@H](O)[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O IWVCMVBTMGNXQD-PXOLEDIWSA-N 0.000 description 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 2
- 229960002508 pindolol Drugs 0.000 description 2
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- FKNXQNWAXFXVNW-WBMJQRKESA-N procaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@H](O)[C@H](NC(C)C)CC FKNXQNWAXFXVNW-WBMJQRKESA-N 0.000 description 2
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 description 2
- QJBZDBLBQWFTPZ-UHFFFAOYSA-N pyrrolnitrin Chemical compound [O-][N+](=O)C1=C(Cl)C=CC=C1C1=CNC=C1Cl QJBZDBLBQWFTPZ-UHFFFAOYSA-N 0.000 description 2
- VMXUWOKSQNHOCA-LCYFTJDESA-N ranitidine Chemical compound [O-][N+](=O)/C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-LCYFTJDESA-N 0.000 description 2
- 229960000620 ranitidine Drugs 0.000 description 2
- 230000035484 reaction time Effects 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- 150000003839 salts Chemical group 0.000 description 2
- 229960004499 scopolamine hydrobromide Drugs 0.000 description 2
- WTGQALLALWYDJH-MOUKNHLCSA-N scopolamine hydrobromide (anhydrous) Chemical compound Br.C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 WTGQALLALWYDJH-MOUKNHLCSA-N 0.000 description 2
- 210000000434 stratum corneum Anatomy 0.000 description 2
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Description
本願発明は薬物放出,経皮吸収に特に優れ、且
つ剥離時の痛みがいちぢるしく緩和された新規な
医療用貼付薬に関するものである。
従来よりテープ状物、あるいはシート状物に薬
物を含有させ皮膚を覆い各種治療を行なう貼付療
法が行なわれているが、皮膚角質層が主として高
分子化されたケラチンのマトリツクスと脂質によ
つて満たされた死細胞が重層して成りたつてお
り、全体として脂質バリヤーの役割を果している
ため期待された十分な量の薬効成分が皮膚より吸
収され難いという問題があり、したがつて薬物を
高濃度に含有させなければならないという欠点が
あつた。又、一方、皮膚角質層の水分含量を増大
させることにより皮膚角質層のバリヤー能を低下
させ、薬物吸収効果が高まるとの知見に基づき、
感圧接着剤層に薬物を含有させ12時間ないし24時
間貼付する密封包帯治療法(ODT療法)が知ら
れているが、該当方法も薬剤が粘着剤層中を拡散
移動しにくいことから有効な薬物放出がなされた
こと、又長時間の貼付により、痒み,気触れ、過
度の白化等が生じやすいこと等の欠点を依然有し
ており満足しうる方法ではない。
本願発明はこれらの技術的諸問題を解決すべ
く、鋭意研究を重ね種々検討したところ、その末
端基がビビニル基であるジオルガノポリシロキサ
ンと両末端基が活性水素原子であるオルガノハイ
ドロジエンポリシロキサンとを白金又は白金化合
物の存在下反応させて得られるオルガノポリシロ
キサンを基剤成分としこれにミクロヒドロゲルを
分散させることにより、
1 薬物の放出性,持続性
2 薬物の皮膚への吸収性,持続性
3 適度な冷感の持続
4 貼付時の適度な弾性
5 皮膚への密着性
6 皮膚への適度な粘着性
7 剥離時の痛み及び膏体残り
8 痒み,気触れ,過度の白化等の皮膚障害
等の条件について、満足しうる貼付薬が得られる
ことを見い出し本発明を完成したものである。
即ち、本願発明は貼付薬の基剤成分として、そ
の末端基がビニル基であるジオルガノポリシロキ
サンと両末端基が活性水素原子であるオルガノハ
イドロジエンポリシロキサンとを白金又は白金化
合物の存在下反応させて得られるオルガノポリシ
ロキサンを基剤成分としこれにミクロヒドロゲル
を分散させることを大きな特徴とするものであ
る。
当該オルガノポリシロキサンは、更に詳細には
ジオルガノポリシロキサン中のケイ素原子に直結
した水素原子が白金系触媒の存在下で付加反応す
るハイドロサイレーシンによつて硬化するものを
いい、いわゆる2液型RTVゴムと称されるもの
である。又、当該オルガノポリシロキサンを得る
ために用いるジオルガノポリシロキサン及びオル
ガノハイドロジエンポリシロキサンとしては
KE106−LTV〔(株)信越化学製〕,KE−103RTV
〔(株)信越化学製〕,KE−104GEL〔(株)信越化学製〕,
X−32−465−2A,2B〔(株)信越化学製〕,KE−
11300RTV〔(株)信越化学製〕,YE−5626〔(株)東芝シ
リコーン製〕,TSE−3032RTV〔(株)東芝シリコー
ン製〕,TSE−3402RTV〔(株)東芝シリコーン製〕,
YE−5822〔(株)東芝シリコーン製〕,YE−5818〔(株)
東芝シリコーン製〕,SH−9583〔(株)トーレシリコ
ーン製〕,SH−9555〔(株)トーレシリコーン製〕,
SH−9585〔(株)トーレシリコーン製〕等が挙げられ
る、これは広く市販されており容易に得ることが
できる。
本願発明の基剤成分を得る為、これらは適宜選
択され組み合わされて用いられるものである。
更に、本願発明の基剤成分について詳述する。
本願発明の貼付薬に基剤成分として用いられる
オルガノポリシロキサンは、その末端基がビニル
基であるジオルガノポリシロキサン(以下、単に
ジオルガノポリシロキサンとという)と両末端基
が活性水素原子であるオルガノハイドロジエンポ
リシロキサン(以下、単にオルガノハイドロジエ
ンポリシロキサンという)を白金又は白金化合物
の存在下、反応させて得られるものである。
上記において、用いれるジオルガノポリシロキ
サンの粘度は600〜700000センチポイズのものが
本発明の基剤成分を得るためには適しており好ま
しくは700〜70000センチポイズのものである。
オルガノハイドロジエンポリシロキサンは、各
種類のものが自由に用いることが出来る。
上記両者は、ジオルガノシロキサン100重量部
に対して、オルガノハイドロジエンポリシロキサ
ンを1〜100重量部、好ましくは2〜9重量部配
合することにより本願発明に適した基剤成分を得
ることが出来るものである。
上記両者の反応に際しては、白金又は白金化合
物が触媒として用いられるが、その量は通常の触
媒量で十分の効果を得ることができる。
尚、上記触媒の添加はジオルガノポリシロキサ
ン及びオルガノハイドロジエンポリシロキサンと
は別個に行なつてもよく、又オルガノハイドロジ
エンポリシロキサンに事前に含有させて用いても
よい。
又、ジオルガノポリシロキサンとオルガノハイ
ドロジエンポリシロキサンとの白金又は白金化合
物の存在下における反応温度は、室温付近では架
橋硬化の進行が徐々であり、温度の上昇と共に架
橋硬化が早くなる為、所望の条件に基づき反応温
度,反応時間は設定されねばならないが、通常0
〜100℃であり、好ましくは20〜50℃である。又、
反応時間は24時間以内であり好ましくは3時間以
内である。上記の配合及び方法によつて得られた
本発明の基剤成分は2液型RTVシリコーンゴム
には粘着性がないとの通常の概念を打ち破り、貼
付薬に十分に適し粘着性を具備するものである。
次に、こうして得れたオルガノポリシロキサン
を基剤成分とする貼付薬に理想的な経皮吸収効果
を出現させるため、本願発明の大きな特徴の1つ
であるミクロヒドロゲルが添加される。ここで用
いられるミクロヒドロゲルとは、高吸水性高分子
に水を吸収させて製造されるものである。高吸水
性高分子とは、自量の10〜1000倍の水を吸収しミ
クロゲルの集合体を生成、加熱しても溶解せず、
加圧下,減圧下においても離水し難いという特色
を持つものであつて、構造的には、水酸基,カル
ボキシル基,又はその塩等の親水性基を有する水
溶性ポリマーに軽度な架橋結合を導入することに
より、樹脂全体を網目状構造にし水不溶可させた
ものである。
更に、前記高吸水性高分子について詳細に例示
すると
イ デンプンにアクリル酸,メタアクリル酸、あ
るいは無水マレイン酸をグラフト重合したもの
又はそのアルカリ中和物の架橋体〔たとえば(株)
三洋化成製・サンウエツトIM−300など〕
ロ アクリル酸アルカリ金属塩あるいはメタアク
リル酸アルカリ金属塩から得られる自己架橋型
アクリル酸アルカリ金属塩重合体〔たとえば(株)
製鉄化学製・アクアキープ4S,アクアキープ
10SHなど〕
ハ α−オレフインと無水マレイン酸あるいはそ
の誘導体との共重合体またはそのアルカリ中和
物の架橋体
ニ ビニルエステルとアクリル酸塩共重合体〔た
とえばスミカゲルS−50,スミカゲルN−50,
スミカゲルN−1100など〕
ホ 酢酸ビニル,メチルビニルエーテル等を無水
マレイン酸あるいはその誘導体との共重合物
ヘ デンプンにアクリルニトリルをグラフト重合
したものまたはそのアルカリ中和物の架橋体
ト セルロースにアクリルニトリルをグラフト重
合したものまたはそのアルカリ中和物の架橋体
チ デンプンをモノクロル酢酸等でカルボキシメ
チル化したものをホルマリン等で架橋したもの
リ セルロースをモノクロル酢酸等でカルボキシ
メチル化したものを架橋したもの
ヌ PVAをジアルデヒドや放射線等で架橋した
もの
ル 無水マレイン酸,イタコン酸またはクロトン
酸で変性したPVAを架橋したもの
オ 二官能性化合物とアクリル酸との共重合体
ワ アクリル酸,アクリルアミド,アクリルニト
リル及びその金属塩と塩化ビニル,塩化ビニリ
デンよりなる共重合体をアルカル処理してなる
もの
等があげられる。これらは、単独あるいは2種以
上の混合により自量の10〜1000倍、好ましくは
100〜500倍の水を吸収させ、本願発明に用いるミ
クロヒドロゲルとなすものである。
当該ミクロヒドロゲルは、基剤成分である前記
オルガノポリシロキサンの含水量が0.1〜80重量
%、好ましくは10〜60%となるような割合で添加
分散させることにより、好ましい効果が期待でき
る。尚、含水量が0.1%以以下では本願発明の特
徴である薬物の経皮吸収効果が薄れるし、また貼
付中の冷感もとぼしいものとなり、また、80%以
上では強度的にも十分なものができず、さらに安
定性も悪くなり、いずれも好ましくない。
上記した粘着性を具備したオルガノポリシロキ
サンにミクロヒドロゲルを分散させることにより
経皮吸収効果を高めるという、特徴ある配合及び
方法は本願発明が最初になしえたことである。
さて、上記した方法及び配合によつて得られた
ミクロヒドロゲル含有オルガノポリシロキサン基
剤成分には、薬効成分が配合されて貼付薬とされ
る。
本願貼付薬に配合される薬効成分としては、例
えばサリチル酸,サリチル酸メチル,サリチル酸
グリコール,l−メントール,カンフル,ハツカ
油,チモール,ニコチン酸ベンジルエステル,ト
ウガラシエキス,カプサイシン,オキシフエンブ
タゾン,ペンタゾシン,エプタゾシン,フエナゾ
ール,メピリゾール,ピロキシカム,ベンジダミ
ン,チアラミド,ブフエキサマツク,アセトアミ
ノフエン,およびイブプロフエン,アルクロフエ
ナツク,アセメタシン,ケトプロフエン,フルル
ビプロフエン,ジクロフエナツク,フエノプロフ
エン,ピルプロフエン,ナプロキセン,スリンダ
ツク,ベノキサプロフエン,インドブフエン,メ
フエナム酸,トルメチン,メチアジン酸,プロチ
ジン酸,プラノプロフエン,ゾンタール,フエン
ブフエン,フエンチアザツク,ジフルニザール,
ゾメピラツク,イブプロフエンピコノール,ベン
ダザツク,ミロプロフエン,アムフエナツク,ロ
キソプロフエン,クリダナツク,スプロフエン並
びにこれらのエステル誘導体である皮膚刺激剤お
よび鎮痛消炎剤:フルフエナジン,チオリダジ
ン,ジアゼパム,クロルプロマジン臭化水素酸ス
コポラミン,ロラゼパム,ハロペリドール,ニト
ラゼパム等の中枢神経作用剤:酢酸ヒドロコルチ
ゾン,ヒドロコルチゾン,プレドニゾロン,トリ
アムシノロンアセトニド,デキサメタゾンリン酸
エステル,メチルプレドニゾロン,酢酸ダイクロ
リゾン,酢酸メチルプレドニゾロン,フルオシノ
ロンアセトニド,酢酸デキサメタゾン,デキサメ
タゾン,フルオロメソロン,ベタメタゾンリン酸
ナトリウム,ベタメタゾン,吉草酸ベタメタゾ
ン,ホルモコルタール,ピバル酸フルメタゾン,
プロピオン酸ベクロメタゾン,フルドロキシコル
チド酪酸プロピオン酸ヒドロコルチゾン,酪酸ヒ
ドロコルチゾン,ジプロピオン酸ベタメタゾン,
フルオシノニド,プロピオン酸クロベタゾール,
吉草酸ジフルコルトロン,ハルシノニド,アムシ
ノニド,吉草酸プレドニゾロン等の副腎皮質ホル
モン剤:リドカイン,ベンゾカイン,アミノ安息
香酸エチル,塩酸プロカイン,ジブカイン,プロ
カイン等の局所麻酔剤:塩酸ジフエンヒドラミ
ン,クロルフエニラミン,ジフエニルイミダゾー
ル,マレイン酸クロルフエラミン,グリチルレチ
ン酸,トラニラスト,ケトチフエン等の抗ヒスタ
ミン剤及び抗アレルギー剤:ハイドロサイアザイ
ド,ペンドロフルナサイアザイド,レセルピン等
の降圧利尿剤:クロニジン等の抗高圧剤:ペニシ
リン,ニトラサイクリン,オキシテトラサイクリ
ン,クロルテトラサイクリン,クロラムフエニコ
ール,スルホンアマイド,オキシテトラサイクリ
ン,硫酸フラジオマイシン,エリスロマイシン,
塩酸テトラサイクリン,フラジオマイシン,ロイ
コマイシン,セフアロスポリン,セフアレキシ
ン,ネオマイシン硫酸塩,バシトラシン,カナマ
イシン,ストレプトマイシン,ゲンタマイシン,
グラミジンS,ミカマイシン,コリスチン等の抗
生物質:塩化ベンザルコニウム,ニトロフラゾ
ン,ナイスタチン,アセトフルフアミン,クロト
リマゾール,ナリジクス,スルフアメチゾール,
トルナフテート,ペンタマイシン,アムホテリシ
ンB,ピロールニトリン,ウンデシレン酸,ミコ
ナゾール,トリコマイシン,バリオチン,ハロプ
ロミジン,塩酸ジマゾール等の抗菌・抗真菌剤:
サリチル酸,モクタール,クリサロビン等の角質
軟化剤:ニトログリセリン,ニトログリコールニ
コランジル,イソソルバイトジナイトレート,塩
酸パパベリン,ジピリダモール,ニフエジピン,
ヘルペツサー,アダラート等の冠血管拡張剤:プ
ロカテロール,メプチン,ピンドロール,イソプ
ロテノール,テオフイリンカルテオロール,プロ
プラノロール等の気管支喘息剤:ニトラゼムパム
クロナゼパム,メブロパメート等のてんかん剤:
ブレオマイシン、アクラシノマイシン,アドリア
マイシン,ペプレオマイシン,5−フルオロウラ
シルおよびその誘導体,マイトマイシン等の抗悪
性腫瘍剤:フエノバルビタール,アモバルビター
ル,コデイン,カリブロマール,シクロバルビタ
ールエスタゾラム等の催眠鎮静剤:ジキタリス,
ジコキシン,ノイキノン等の強心剤:テストステ
ロン,エナント酸テストステロン,トリエチステ
ロン,メチルエストレノロン,メストラノール,
吉草酸エストラジオール,エチニルエストラジオ
ール等の性ホルモン剤:ビタミンA,ビタミン
D,ビタミンE,又はその他のビタミン類および
エルゴカルシフエロール,コレカルシフエロー
ル,オタトチミン,リボフラビン酪酸エステル等
のビタミン剤:リン酸コデイン,ビソルビンサル
ブタモール,プロカルテロール等の鎮咳去たん
剤:リゾチームおよびその他の消炎酵素剤:イン
シユリングリベンクラミドおよびその他の糖尿病
治療剤:D−ペニシラミン,ベスタチン,レバミ
ゾール,カルフエニール,プラトニン等の免疫に
関与する薬剤:コルヒチン等の痛風治療剤:メチ
ル硫酸メチルスコポラミン等の鎮けい剤:その他
の抗けいれん剤:抗マラリア剤:プロスタグラン
デイン類:すい臓ホルモン,生薬エキス,シメチ
ジン,ラニチジン,フアモチジン等の抗潰瘍剤等
が挙げられ、これら薬効成分は一種又は二種以上
が適宜配合されて用いられる。もちろん、これら
の薬物は単独で前記基剤成分に配合されてもよ
く、又ポリエチレングリコール,プロピレングリ
コール,ベンジルアルコール,ブチルベンゾエー
ト,ミリスチン酸イソプロピル,ポリプロピレン
グリコール,クロタミトン,エチレングリコー
ル,ブチレングリコール,ジエチルセバケート,
ジイソプロピルアジペート,等の溶解剤に該薬物
を溶解させて用いてもよい。
又、更に従来公知の経皮吸収促進剤や安定剤,
老化防止剤,香料鉱油,酸化防止剤,補強用充填
剤,増量無機充填剤,粘着剤等の添加剤が必要に
応じて配合される。添加剤としては、例えば水溶
性高分子であるポリビニルアルコール,ポリビニ
ルピロリドン,ポリアクリル酸,ビニルアルコー
ル系共重合体,ポリブテン,ロジン,エステルガ
ム,アクリル酸エステル等の粘着剤、シリカ,カ
オリン,タルク,酸化亜鉛,等の増量無機充填剤
等が挙げられる。
前記薬効成分は、前述した本願発明の特徴ある
基剤成分オルガノポリシロキサンにミクロヒドロ
ゲルを分散させたもの(以下、分散基剤成分とい
う)100重量部に対し、0.03〜25重量部、好まし
くは0.03〜15重量部配合される。又必要に応じ配
合される各種添加剤は前記分散基剤成分100重量
部に対し5〜20重量部、好ましくは7〜15重量部
配合される。
次に薬効成分及び添加剤の配合方法について述
べる。薬効成分は、本願発明の基剤成分であるオ
ルガノポリシロキサンに前述したミクロヒドロゲ
ルを添加分散させた後、前記した配合量を添加す
ることが好ましい。更に必要に応じて添加剤が該
オルガノポリシロキサンの架橋硬化をさまたげな
い範囲で、薬効成分の添加と同時に、又はその後
に加える。
又、薬効成分及び添加剤の配合は前述の基剤成
分を得るために用いられた同一槽の中で行なわれ
てよく、温度も基剤成分を得る為の反応温度内で
十分である。
上記の如くして得られた分散基剤成分及び薬効
成分、必要に応じては添加剤の混合物は柔軟な支
持体、例えばポリエチレン,ポリプロピレン,ポ
リブタジエン,エチレン−酢酸ビニル共重合体,
ポリ塩化ビニル,ポリエステル,ナイロンなどの
フイルム又はシートあるいはこれからなる多孔質
体,発泡体そして紙,布,不織布,などの通気性
シート状物のどにドクターブレード,ドクターロ
ール等の塗布機を用いて50μm〜2mm、好ましく
は100μm〜1mmの厚さに展延し、室温〜150℃好
ましくは40〜80℃で3分〜24時間好ましくは15〜
40分間加熱し架橋硬化の処理を行なう。その後、
表面を剥離処理がほどこされた剥離紙,セフアン
又はポリエチレン,ポリプロピレン等のプラスチ
ツクフイルムで覆い所望の大きさに切断して本願
発明の目的物とするか、あるいは一旦熱に対し安
定性の良い支持体に展延後、前記した加熱,架橋
硬化の処理を行ないその後目的とする合成樹脂,
布等の支持体で覆つた後、圧着転写させ所望の大
きさに切断し本願発明の目的物とすることもでき
る。
上記の方法は、目的とする支持体に応じて適時
選択することができる。
次に本願発明の貼付薬の効果について述べる。
前述の如くして得られた本願発明の貼付薬は人
体の皮膚に対して適度な密着力と粘着力を持ち、
前記ミクロヒドロゲルの水分保持力のため冷感が
長時間にわたつて持続し、しかも長時間貼付し続
けても全く気触れ等の副作用もく、剥離時の毛の
引張り,角質の破壊も起こさず又一度貼付したも
のを剥離し、再度貼付しても初回の密着力と粘着
力を有する等の大きな特徴を有するものである。
又、薬物の放出性,持続性及び経皮吸収性も非
常に良く理想的な貼付薬として産業上非常に有用
である。
尚、本願発明の効果は前述した如く、特徴ある
基剤成分によるものであることは勿論である。
上述の効果については以下試験例においてこれ
を説明する。試験例において実施例及び参考例と
あるは本願明細書において後述されているそれを
さすものである。
試験例 1
使用感比較試験
10名の被験者に本発明の実施例1及び2、比較
例として市販の消炎鎮痛プラスターA(基剤とし
て天然ゴム+合成ゴム、薬物サリチル酸メチル含
有のものである)とパツプ剤B(ゼラチン+カオ
リン+水溶性高分子基剤のもの、薬物はサリチル
酸メチル含有のものである)の4種を用いて前腕
表部側に貼付し、8時間後剥離した。下記の各項
目につき試験し判定した。その結果を表1に示す
が、本発明の実施例1及び2は市販の消炎鎮痛プ
ラスターA及びパツプ剤Bに比較、両方の利点を
兼ね備えた上、有為に優れていることが判明、
本発明の有用さをうらづけるものであつた。
試験項目
イ 冷感
冷感がるもの……◎
冷感がないもの…×
ロ 速効性(刺激を感じはじめる時間)
5分以内……◎
5〜10分以内…〇
10分以上……×
ハ 持続性(刺激がなくなるまでの時間)
4時間以上……◎
2〜4時間……〇
2時間以内……×
ニ 密着性
貼付中を通して
良くついているもの……◎
端の部分がはがれているもの…〇
半分以上はがれたもの……×
ホ 刺激の強さ
非常に強い……◎
強い……〇
弱い……×
ヘ 剥離時の痛み
容易にはがせる……◎
痛みを感じる……〇
強い痛みがある……×
ト 剥離時の再貼付
5回以上の再貼付……◎
つかない……×
The present invention relates to a novel medical patch that is particularly excellent in drug release and transdermal absorption, and which significantly alleviates pain upon peeling. Traditionally, patch therapy has been used in which drugs are contained in a tape or sheet-like material and the skin is covered for various treatments. It is made up of multiple layers of dead cells, which act as a lipid barrier.Therefore, there is a problem in that it is difficult for a sufficient amount of the expected medicinal ingredients to be absorbed through the skin. The disadvantage was that it had to be contained in On the other hand, based on the knowledge that increasing the water content of the stratum corneum of the skin reduces the barrier ability of the stratum corneum of the skin and increases the drug absorption effect,
Occlusive bandage therapy (ODT therapy) is known, in which a pressure-sensitive adhesive layer contains a drug and is applied for 12 to 24 hours, but this method is also not effective because the drug does not easily diffuse through the adhesive layer. This is not a satisfactory method as it still has drawbacks such as drug release and the tendency to cause itching, irritation, excessive whitening, etc. due to long-term application. In order to solve these technical problems, the present invention has been made through intensive research and various examinations, and has been developed into a diorganopolysiloxane whose terminal group is a bivinyl group and an organohydrodiene polysiloxane whose terminal groups are active hydrogen atoms. By dispersing microhydrogel into the base component, organopolysiloxane obtained by reacting with and in the presence of platinum or a platinum compound, 1. Drug release and persistence 2. Drug absorption and persistence into the skin Properties 3 Appropriate cooling sensation sustained 4 Appropriate elasticity when applied 5 Adhesion to the skin 6 Appropriate adhesion to the skin 7 Pain upon removal and plaster residue 8 Skin irritation, irritation, excessive whitening, etc. The present invention was completed by discovering that a patch drug that satisfies conditions such as disorders can be obtained. That is, the present invention uses a diorganopolysiloxane whose terminal group is a vinyl group and an organohydrodiene polysiloxane whose terminal groups are active hydrogen atoms as a base component of a patch in the presence of platinum or a platinum compound. The main feature of this method is that the microhydrogel is dispersed in the organopolysiloxane obtained by using the organopolysiloxane as a base component. More specifically, the organopolysiloxane is one that is cured by hydrothyresin, in which hydrogen atoms directly bonded to silicon atoms in the diorganopolysiloxane undergo an addition reaction in the presence of a platinum-based catalyst, and is a so-called two-component type. It is called RTV rubber. In addition, the diorganopolysiloxane and organohydrodiene polysiloxane used to obtain the organopolysiloxane include
KE106−LTV [manufactured by Shin-Etsu Chemical Co., Ltd.], KE−103RTV
[Manufactured by Shin-Etsu Chemical Co., Ltd.], KE-104GEL [Manufactured by Shin-Etsu Chemical Co., Ltd.],
X-32-465-2A, 2B [Shin-Etsu Chemical Co., Ltd.], KE-
11300RTV [manufactured by Shin-Etsu Chemical Co., Ltd.], YE-5626 [manufactured by Toshiba Silicone Corporation], TSE-3032RTV [manufactured by Toshiba Silicone Corporation], TSE-3402RTV [manufactured by Toshiba Silicone Corporation],
YE-5822 [manufactured by Toshiba Silicone Corporation], YE-5818 [manufactured by Toshiba Silicone Corporation]
manufactured by Toshiba Silicone], SH-9583 [manufactured by Toray Silicone Co., Ltd.], SH-9555 [manufactured by Toray Silicone Co., Ltd.],
Examples include SH-9585 (manufactured by Toray Silicone Co., Ltd.), which is widely commercially available and can be easily obtained. In order to obtain the base component of the present invention, these are appropriately selected and used in combination. Furthermore, the base component of the present invention will be explained in detail. The organopolysiloxane used as a base component in the patch of the present invention is a diorganopolysiloxane whose terminal group is a vinyl group (hereinafter simply referred to as diorganopolysiloxane) and whose terminal groups are active hydrogen atoms. It is obtained by reacting organohydrodiene polysiloxane (hereinafter simply referred to as organohydrodiene polysiloxane) in the presence of platinum or a platinum compound. In the above, the diorganopolysiloxane used has a viscosity of 600 to 700,000 centipoise, which is suitable for obtaining the base component of the present invention, and preferably 700 to 70,000 centipoise. Various types of organohydrodiene polysiloxanes can be used freely. For both of the above, a base component suitable for the present invention can be obtained by blending 1 to 100 parts by weight, preferably 2 to 9 parts by weight, of organohydrodiene polysiloxane to 100 parts by weight of diorganosiloxane. It is something. In the above-mentioned reactions, platinum or a platinum compound is used as a catalyst, and a sufficient effect can be obtained with a normal amount of the catalyst. The catalyst may be added separately from the diorganopolysiloxane and the organohydrodiene polysiloxane, or may be added in advance to the organohydrodiene polysiloxane. In addition, the reaction temperature of diorganopolysiloxane and organohydrodiene polysiloxane in the presence of platinum or a platinum compound is not as high as desired because crosslinking and curing progresses gradually near room temperature, and crosslinking and curing accelerates as the temperature rises. The reaction temperature and reaction time must be set based on the conditions, but usually 0
-100°C, preferably 20-50°C. or,
The reaction time is within 24 hours, preferably within 3 hours. The base component of the present invention obtained by the above-mentioned formulation and method breaks the general concept that two-component RTV silicone rubber has no tackiness, and has tackiness sufficiently suitable for patch medicines. It is. Next, microhydrogel, which is one of the major features of the present invention, is added to the patch containing the organopolysiloxane as a base component, which is one of the major characteristics of the present invention, in order to achieve an ideal transdermal absorption effect. The microhydrogel used here is produced by making a super absorbent polymer absorb water. Super absorbent polymers absorb 10 to 1000 times their own amount of water, form microgel aggregates, and do not dissolve even when heated.
It has the characteristic of not easily releasing water even under pressure or reduced pressure, and has a structure that introduces a slight cross-linking bond into a water-soluble polymer that has hydrophilic groups such as hydroxyl groups, carboxyl groups, or salts thereof. As a result, the entire resin has a network structure and is water-insoluble. Further, detailed examples of the superabsorbent polymers include (a) starch graft polymerized with acrylic acid, methacrylic acid, or maleic anhydride, or a crosslinked product of an alkali neutralized product thereof [for example, manufactured by Co., Ltd.
Sanyo Chemical Co., Ltd., Sunwet IM-300, etc.] Self-crosslinking type alkali metal acrylate polymer obtained from alkali metal acrylate or alkali metal methacrylate (for example, manufactured by Co., Ltd.)
Aqua Keep 4S, Aqua Keep, manufactured by Seitetsu Kagaku
10SH, etc.] C. Copolymers of α-olefin and maleic anhydride or its derivatives, or crosslinked vinyl ester and acrylate copolymers of their alkali neutralized products [e.g. Sumikagel S-50, Sumikagel N-50,
Sumikagel N-1100, etc.] A copolymer of vinyl acetate, methyl vinyl ether, etc. with maleic anhydride or its derivatives A graft polymer of acrylonitrile on starch or a crosslinked product of its alkaline neutralized product A crosslinked product of acrylonitrile on cellulose Cross-linked products obtained by graft polymerization or their alkali neutralized products; Cross-linked products obtained by carboxymethylating starch with monochloroacetic acid, etc.; and Cross-linked products obtained by carboxymethylating cellulose with monochloroacetic acid, etc.; PVA. Cross-linked with dialdehyde or radiation, etc. Cross-linked PVA modified with maleic anhydride, itaconic acid, or crotonic acid. Copolymers of bifunctional compounds and acrylic acid. Acrylic acid, acrylamide, acrylonitrile, Examples include those obtained by alkal-treating a copolymer consisting of the metal salt, vinyl chloride, and vinylidene chloride. These can be used alone or in combination of two or more to produce 10 to 1000 times their own amount, preferably
It absorbs 100 to 500 times more water and forms the microhydrogel used in the present invention. Preferable effects can be expected by adding and dispersing the microhydrogel in such a proportion that the water content of the organopolysiloxane, which is a base component, is 0.1 to 80% by weight, preferably 10 to 60%. If the water content is less than 0.1%, the transdermal absorption effect of the drug, which is a feature of the present invention, will be weakened, and the cooling sensation during application will be poor, and if it is more than 80%, the strength will not be sufficient. In addition, the stability deteriorates, both of which are undesirable. The present invention is the first to achieve the unique formulation and method of enhancing the transdermal absorption effect by dispersing microhydrogel in organopolysiloxane having the above-mentioned adhesive properties. Now, the microhydrogel-containing organopolysiloxane base component obtained by the above-described method and formulation is blended with a medicinal ingredient to form a patch. The medicinal ingredients contained in the patch of the present invention include, for example, salicylic acid, methyl salicylate, glycol salicylate, l-menthol, camphor, pepper oil, thymol, nicotinic acid benzyl ester, capsicum extract, capsaicin, oxyphenbutazone, pentazocine, and eptazocine. , fenazole, mepirizole, piroxicam, benzydamine, tiaramide, bufexamac, acetaminophen, and ibuprofen, alclofenac, acemethacin, ketoprofen, flurbiprofen, diclofenac, fenoprofen, pirprofen, naproxen, sulindac, benoxaprofen, indobufen , mefenamic acid, tolmetin, methiazine acid, protidic acid, pranoprofen, zontar, fenbufuene, fentiazac, diflunisal,
Zomepiratuk, ibuprofen piconol, bendazatuk, miloprofen, amfuenatuk, loxoprofen, clidantuk, suprofen and their ester derivatives as skin irritants and analgesic anti-inflammatory agents: fluphenazine, thioridazine, diazepam, chlorpromazine, scopolamine hydrobromide, lorazepam , haloperidol, nitrazepam, and other central nervous system agents: hydrocortisone acetate, hydrocortisone, prednisolone, triamcinolone acetonide, dexamethasone phosphate, methylprednisolone, diclorizone acetate, methylprednisolone acetate, fluocinolone acetonide, dexamethasone acetate, dexamethasone, fluoro Mesolone, betamethasone sodium phosphate, betamethasone, betamethasone valerate, formocortal, flumethasone pivalate,
Beclomethasone propionate, fludroxycortide hydrocortisone butyrate propionate, hydrocortisone butyrate, betamethasone dipropionate,
fluocinonide, clobetasol propionate,
Corticosteroids such as diflucortoron valerate, halcinonide, amcinonide, and prednisolone valerate: Local anesthetics such as lidocaine, benzocaine, ethyl aminobenzoate, procaine hydrochloride, dibucaine, and procaine: diphenhydramine hydrochloride, chlorfenilla Antihistamines and antiallergic agents such as min, diphenylimidazole, chlorpheramine maleate, glycyrrhetinic acid, tranilast, and ketotifen: Antihypertensive diuretics such as hydrothiazide, pendroflunathiazide, and reserpine; Antihypertensive agents such as clonidine: penicillin, Nitracycline, oxytetracycline, chlortetracycline, chloramphenicol, sulfonamide, oxytetracycline, fradiomycin sulfate, erythromycin,
Tetracycline hydrochloride, fradiomycin, leucomycin, cephalosporin, cephalexin, neomycin sulfate, bacitracin, kanamycin, streptomycin, gentamicin,
Antibiotics such as gramidin S, micamicin, colistin: benzalkonium chloride, nitrofurazone, nystatin, acetoflufamine, clotrimazole, nalidix, sulfamethizole,
Antibacterial and antifungal agents such as tolnaftate, pentamycin, amphotericin B, pyrrolnitrine, undecylenic acid, miconazole, trichomycin, variotin, halopromidine, dimazole hydrochloride:
Keratin softeners such as salicylic acid, Moctal, Crisarobin, etc.: nitroglycerin, nitroglycol nicorandil, isosorbite dinitrate, papaverine hydrochloride, dipyridamole, nifedipine,
Coronary vasodilators such as Herpetusar and Adalate; Bronchial asthma agents such as procaterol, meptin, pindolol, isoprotenol, theophylline carteolol, and propranolol; Epilepsy agents such as nitrazempam clonazepam and mebropamate:
Anti-neoplastic agents such as bleomycin, aclacinomycin, adriamycin, pepleomycin, 5-fluorouracil and its derivatives, mitomycin; hypnotic-sedative agents such as phenobarbital, amobarbital, codeine, caribromal, cyclobarbital estazolam; digitalis,
Cardiotropes such as dicoxin and neuquinone: testosterone, testosterone enanthate, triethisterone, methylestrenolone, mestranol,
Sex hormones such as estradiol valerate and ethinyl estradiol: Vitamin A, vitamin D, vitamin E, or other vitamins, and vitamins such as ergocalciferol, cholecalciferol, otatothymine, and riboflavin butyrate: codeine phosphate , bisorbin, antitussive expectorants such as salbutamol, procarterol; lysozyme and other anti-inflammatory enzymes; insulin; glibenclamide and other antidiabetic agents; involved in immunity such as D-penicillamine, bestatin, levamisole, carfenil, platonin, etc. Drugs: Gout treatments such as colchicine: Antispasmodics such as methylscopolamine sulfate: Other antispasmodics: Antimalarials: Prostaglandins: Pancreatic hormones, herbal medicine extracts, antiulcer agents such as cimetidine, ranitidine, famotidine, etc. These medicinal ingredients may be used singly or in combination as appropriate. Of course, these drugs may be blended alone into the base component, or polyethylene glycol, propylene glycol, benzyl alcohol, butyl benzoate, isopropyl myristate, polypropylene glycol, crotamiton, ethylene glycol, butylene glycol, diethyl sebacate. ,
The drug may be dissolved in a dissolving agent such as diisopropyl adipate. In addition, conventionally known transdermal absorption enhancers and stabilizers,
Additives such as anti-aging agents, flavoring mineral oils, antioxidants, reinforcing fillers, extender inorganic fillers, and adhesives are added as necessary. Examples of additives include water-soluble polymers such as polyvinyl alcohol, polyvinylpyrrolidone, polyacrylic acid, vinyl alcohol copolymers, polybutene, rosin, ester gum, adhesives such as acrylic esters, silica, kaolin, talc, Examples include bulking inorganic fillers such as zinc oxide, etc. The medicinal ingredient is 0.03 to 25 parts by weight, preferably 0.03 parts by weight, per 100 parts by weight of the microhydrogel dispersed in organopolysiloxane, the characteristic base component of the present invention (hereinafter referred to as the dispersion base component). ~15 parts by weight is blended. Various additives may be blended as needed in an amount of 5 to 20 parts by weight, preferably 7 to 15 parts by weight, per 100 parts by weight of the dispersion base component. Next, the method of blending medicinal ingredients and additives will be described. The medicinal ingredient is preferably added in the amount described above after the microhydrogel described above is added and dispersed in the organopolysiloxane that is the base component of the present invention. Furthermore, if necessary, additives may be added at the same time as or after the addition of the medicinal ingredients to the extent that they do not hinder the crosslinking and curing of the organopolysiloxane. Furthermore, the medicinal ingredients and additives may be blended in the same tank used to obtain the base component described above, and the temperature is sufficient to be within the reaction temperature for obtaining the base component. The mixture of the dispersion base component and medicinal ingredient obtained as described above, and optionally additives, can be applied to a flexible support such as polyethylene, polypropylene, polybutadiene, ethylene-vinyl acetate copolymer,
Using a coating machine such as a doctor blade or doctor roll, coat a film or sheet such as polyvinyl chloride, polyester, or nylon, or a porous material made of the same, a foam, or an air-permeable sheet material such as paper, cloth, or nonwoven fabric to a thickness of 50 μm using a coating machine such as a doctor blade or doctor roll. Spread to a thickness of ~2 mm, preferably 100 μm to 1 mm, and heat at room temperature to 150 °C, preferably 40 to 80 °C, for 3 minutes to 24 hours, preferably 15 to 1 mm.
Heat for 40 minutes to perform crosslinking and hardening. after that,
The object of the present invention can be obtained by covering the surface with a release paper, a plastic film made of polyethylene, polypropylene, etc. that has been subjected to a release treatment, or by cutting it into a desired size, or by using a support that is stable against heat. After spreading, the above-mentioned heating and cross-linking curing process is performed to obtain the desired synthetic resin,
The object of the present invention can also be obtained by covering with a support such as cloth, pressing and transferring, and cutting into a desired size. The above methods can be appropriately selected depending on the intended support. Next, the effects of the patch of the present invention will be described. The patch of the present invention obtained as described above has appropriate adhesion and adhesive strength to human skin,
Due to the water retention ability of the microhydrogel, the cooling sensation lasts for a long time, and even if it is applied for a long time, there are no side effects such as irritation, and there is no pulling of the hair or destruction of the keratin when it is removed. It also has great features such as maintaining the initial adhesion and adhesive strength even if it is peeled off and reapplied once it has been applied. In addition, the drug's release properties, sustainability, and transdermal absorption properties are very good, making it very useful industrially as an ideal patch. It goes without saying that the effects of the present invention are due to the characteristic base components as described above. The above-mentioned effects will be explained in the following test examples. Examples and reference examples in the test examples refer to those described later in the specification of the present application. Test Example 1 Usability Comparison Test Ten subjects were given Examples 1 and 2 of the present invention, commercially available anti-inflammatory and analgesic plaster A (natural rubber + synthetic rubber as a base, and containing the drug methyl salicylate) as a comparative example. Four kinds of plaster B (gelatin + kaolin + water-soluble polymer base, drug containing methyl salicylate) were applied to the surface of the forearm and peeled off after 8 hours. The following items were tested and judged. The results are shown in Table 1, and it was found that Examples 1 and 2 of the present invention were significantly superior to the commercially available anti-inflammatory and analgesic plaster A and plaster B, as they had the advantages of both. This hinted at the usefulness of the invention. Test item A Cold sensation Cold sensation...◎ No cold sensation...× B Fast-acting (time to start feeling irritation) Within 5 minutes...◎ Within 5 to 10 minutes...〇 10 minutes or more...× H Persistence (time until irritation disappears) More than 4 hours...◎ 2 to 4 hours...〇 Less than 2 hours...× D Adhesion Good adhesion throughout application...◎ Edges peeling off …〇 More than half of the peeled off……× E Intensity of irritation Very strong……◎ Strong……〇 Weak……× F Pain during peeling Easily peeled off……◎ Feeling pain……〇 There is strong pain ……× G Reapplying after peeling Reapplying 5 or more times……◎ Does not stick……×
【表】
以上の結果から明らかな如く、本願発明の貼付
薬は冷感,速効性,持続性,密着性、刺激の強
さ,剥離時の痛み,剥離時の再貼付に関しても好
結果を得た。
試験例 2
保水性比較試験
実施例1及び2で得れた本発明による消炎鎮痛
貼付薬と市販の消炎鎮痛パップ剤2種(Cおよび
D)を用い、25℃,50%RHの雰囲気中に放置し
て、その重量変化に基づいて水分残存率を求め
た。その結果を、第1図に示す。(図中1は実施
例1を、2は実施例2を、C市販品Cを、Dは市
販品Dをそれぞれ示す)この結果から明らかなよ
うに、本発明によるものは市販品に比較、高い保
水性を持つものであつた。
試験例 3
ヒトでの経皮吸収試験
被験者として5名の健康男子志願者の背部皮膚
面に2×2cm2の大きさに裁断した本発明による実
施例3の製品と参考例1の製品を8時間連続貼付
し、剥離後その粘着剤中の残存薬物量を高速液体
クロマトグラフイーにより定量し、初期含量との
比より薬物の経皮吸収率(%)を求めた。
試験結果を表2に示すが、本発明になる製品は
薬物放出性及び経皮吸収が非常に良く本発明の有
用性をうらづけるものであつた。[Table] As is clear from the above results, the adhesive patch of the present invention obtained good results in terms of cooling sensation, fast-acting, persistence, adhesion, strength of stimulation, pain upon peeling, and reapplication after peeling. Ta. Test Example 2 Water Retention Comparison Test Using the anti-inflammatory analgesic patch according to the present invention obtained in Examples 1 and 2 and two types of commercially available anti-inflammatory analgesic poultices (C and D), the test was carried out in an atmosphere of 25°C and 50% RH. After being left to stand, the residual moisture rate was determined based on the weight change. The results are shown in FIG. (In the figure, 1 indicates Example 1, 2 indicates Example 2, C indicates commercial product C, and D indicates commercial product D.) As is clear from these results, the product according to the present invention is compared to the commercial product. It had high water retention. Test Example 3 Human Transdermal Absorption Test The product of Example 3 according to the present invention and the product of Reference Example 1 cut into 2 x 2 cm 2 pieces were placed on the back skin of five healthy male volunteers as test subjects. After continuous application for a period of time and peeling off, the amount of drug remaining in the adhesive was determined by high performance liquid chromatography, and the percutaneous absorption rate (%) of the drug was determined from the ratio to the initial content. The test results are shown in Table 2, and the product according to the present invention had very good drug release properties and transdermal absorption, which suggested the usefulness of the present invention.
【表】
試験例 4
水中放出試験
実施例4,5及び参考例2を用いインドメタシ
ンの水中への溶出を測定した。
各サンプルを4×4cm2に裁断し、30℃の純水に
浸漬して、浸漬時間と放出率(%)との関係を調
べた。図2にその結果を示すが、本発明による実
施例4,5は参考例2に比較し、はるかに高い放
出率を示した。
以上の試験結果から明らかな様に。ジオルガノ
ポリシロキサンとオルガノハイドロジエンポルシ
ロキサンを白金又は白金化合物の存在下、反応さ
せて得られるオルガノポリシロキサンを基剤成分
とし、これにミクロヒドロゲルを分散させること
を特徴とする本願発明は従来の貼付薬の持つ欠点
を解消した新しい型の貼付薬ということができ
る。
以下、本願発明を実施例により更に具体的に説
明する。但し、本願発明は実施例のみに限定され
るものではないことは勿論である。
尚、実施例において部とあるのは全て重量部を
示す。
実施例 1
25℃で4000センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるTSE−
3032RTV〔(株)東芝シリコーン製〕100部と25℃で
250センチポイズの両末端基が活性水素原子を有
するオルガノハイドロジエンポリシロキサンで白
金含有ずみのYE−5822B〔(株)東芝シリコーン製〕
10部とを30℃にて10分間撹拌混合した。一方、ス
ミカゲルS−50〔(株)住友化学製〕に自重の200倍の
蒸留水を吸収させたもの45部をオルガノポリシロ
キサン混合物中に添加、よく分散させた。ついで
l−メントール6部,サリチル酸メチル6部,カ
ンフル5部を添加、20分間混合して均一なものに
した。得られた混合物を水に対する不透過処理を
した不織布に厚さ1mmになるように展延し、25分
間加熱して硬化させ表面をセロフアンで覆い所望
の大きさに切断し製品とした。このものを人体に
貼付したところ、薬効と共に冷感が持続し、消炎
鎮痛貼付剤として非常に有用であることがわかつ
た。
実施例 2
25℃で4000センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるKE−
106LTV〔(株)信越化学製〕100部と25℃で250セン
チポイズの両末端基が活性水素原子を有するオル
ガノハイドロジエンポリシロキサンで白金含有ず
みのYE−5822B〔(株)東芝シリコーン製〕7部とを
30℃にて10分間撹拌混合した。一方サンウエツト
IM−300〔(株)三洋化成工業製〕に自重の200倍の蒸
留水を吸収させミクロヒドロゲルとなした。前記
混合物にこのミクロヒドロゲル80部を添加、よく
分散させた。ついでl−メントール10部,サリチ
ル酸メチル10部,カンフル5部を添加、20分間撹
拌混合して均一なものにした。得らられた混合物
を水に対する不透過処理をした不織布に厚さ1mm
になるように展延し、30分間加熱して硬化させ表
面をポリエチレンフイルムで覆い所望の大きさに
切断し製品とした。人体に使用したところ、実施
例1と同様であつた。
実施例 3
25℃で4000センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるKE−
106LTV〔(株)信越化学製〕100部と25℃で600〜
1000センチポイズの両末端基が活性水素原子を有
するオルガノハイドロジエンポリシロキサンで白
金含有ずみのTSE−3032RTV−B〔(株)東芝シリ
コーン製〕9部とを25℃にて10分間撹拌混合した
一方、サンウエツトIM−300〔(株)三洋化成工業製〕
に自重の150倍の蒸留水を吸収させミクロヒドロ
ゲルとなした。前記混合物にこのミクロヒドロゲ
ル60部を添加、よく分散させた。ついでエチレン
グリコール15部に溶解させたケトプロフエン5.7
部を添加、15分間混合して均一なものにした。得
られた混合物を厚さ500μmのポリブタジエンシー
トに100μmの厚さに展延し25分間加熱して硬化さ
せた後、表面をポリエチレンフイムで覆い製品と
した。
実施例 4
25℃で70000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるYE−
5626〔(株)東芝シリコーン製〕100部と25℃で600〜
1000センチポイズの両末端基が活性水素原子を有
するオルガノハイドロジエンポリシロキサンで白
金含有ずみのTSE−3032RTV−B〔(株)東芝シリ
コーン製〕8部とを25℃にて20分間撹拌混合し
た。一方、アクアキープ4S〔(株)製鉄化学社製〕に
自重の250倍の蒸留水を吸収させミクロヒドロゲ
ルとなした。前記混合物にこのミクロヒドロゲル
80部を添加、よく分散させた。ついでクロタミト
ン6部に溶液させたインドメタシン6部を添加、
10分間混合して均一なものにした。得られた混合
物を水に対する不透過処理をした不織布に厚さ
200μmで展延し、表面をセロフアンで覆い製品品
とした。
実施例 5
25℃で4000センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるTSE−
3032RTV〔(株)東芝シリコーン製〕100部と25℃で
250センチポイズの両末端基が活性水素原子を有
するオルガノハイドロジエンポリシロキサンで白
金含有ずみのYE−5822B〔(株)東芝シリコーン製〕
7部とを45℃にて20分間よく混合した。一方、ス
ミカゲルN−100〔(株)住友化学製〕に自重の200倍
の蒸留水を吸収させミクロヒドロゲルとした。前
記混合物にこのミクロヒドロゲル62部を添加、よ
く分散させた。ついでクロタミトン5部に溶解さ
せたインドメタシン5部を添加、30分間よく混合
した。得られた混合物をポリブタジエンシートに
厚さ200μmになるように展延し、25分間加熱硬化
させた後表面を剥離紙で覆い製品とした。
実施例 6
25℃で1100センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるKE−
103RTV〔(株)信越化学製〕100部と25℃で602セン
チポイズの両末端基が活性水素原子を有するオル
ガノハイドロジエンポリシロキサンで白金含有ず
みのYE−5822B〔(株)東芝シリコーン製〕とを50℃
にて10分間撹拌混合した。一方スミカゲルS−50
〔(株)住友化学製〕に自重の200倍の蒸留水を吸収さ
せミクロヒドロゲルとした。前記混合物にこのミ
クロヒドロゲル70部を添加、よく分散させた。つ
いでジエチルセバケート10部に溶解させたフルル
ビプロフエン5.2部を添加、15分間よく混合した。
得られた混合物をナイロン製支持体(商品名:ア
イエルN−1070(株)旭化成製〕に100μmの厚さにな
るように展延し25分間加熱硬化させた。表面をセ
ロフアンで覆い所望の大きさに切断し製品とし
た。
実施例 7
25℃で1102センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるX−32−
465−2A〔(株)信越化学製〕100部に25℃で602セン
チポイズの両末端基が活性水素原子を有するオル
ガノハイドロジエンポリシロキサンで白金含有ず
みのX−32−465−2B〔(株)信越化学製〕95部を加
え25℃にて10分間撹拌混合した。一方、サンウエ
ツトIM−300〔(株)三洋化成製〕に自重の300倍の蒸
留水を吸収させミクロヒドロゲルとした。前記混
合物にこのミクロヒドロゲル65部を添加、よく分
散させた。ついで吉草酸ベタメタゾン0.05部とプ
ロピレングリコール1部とを添加し20分間よく混
合した。得れた混合物を剥型紙に厚さ100μmに展
延し、30分間加熱硬化させた後、ポリエチレンフ
イルムで覆い圧着転写、所望の大きさに切断し製
品とした。
実施例 8
25℃で700センチポイズの末端基がビニル基を
有するオルガノハイドロジエンポリシロキサンで
あるKE−104GEL〔(株)信越化学製〕100部と25℃
で80センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみのCat104〔(株)信越化学製〕10部とを20℃
にて10分間よく混合した。一方、スミカゲルS−
50〔(株)住友化学製〕に自重の250倍の蒸留水を吸収
させミクロヒドロゲルとした。ついでエチルアル
コール8部に溶解させたポリリ酢酸ビニル5.5部
とジピリダモール4部とを添加、均一になるよう
に15分間よく混合撹拌した。得られた混合物を不
織布に100μmの厚さで展延し、35分間加熱硬化さ
せた。表面を剥型紙で覆い所望の大きさに切断し
製品とした。
実施例 9
25℃で4000センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるKE−
106LTV〔(株)信越化学製〕100部と25℃で250セン
チポイズの両末端基が活性水素原子を有するオル
ガノハイドロジエンポリシロキサンで白金含有ず
みのYE−5822B〔(株)東芝シリコーン製〕9部とを
40℃にて10分間撹拌混合した。一方、スミカゲル
N−100〔(株)住友化学製〕に自重の300倍の蒸留水
を吸収させミクロヒドロゲルとした。前記混合物
にこのミクロヒドロゲル50部を添加、よく分散さ
せた。ついでジイソプロピルアジペート5部に溶
解させたアルクロフエナツク4部を添加、20分間
よく混合した。得られた混合物をポリブタジエン
シートに100μmの厚さになるように展延し、20分
間加熱硬化させた。表面をポリエチレンフイルム
で覆い所望の大きさに切断し製品とした。
実施例 10
25℃で1012センチポイズの末端基がビニル基を
有するジオルガノポリシロキサンであるX−32−
465−2A〔(株)信越化学製〕100部に25℃で602セン
チポイズの両末端基が活性水素原子を有するオル
ガノハイドロジエンポリシロキサンで白金含有ず
みのX−32−465−2B〔(株)信越化学製〕100部を加
え30℃にて5分間撹拌混合した。一方、スミカゲ
ルS−50〔(株)住友化学製〕に自重の250倍の蒸留水
を吸収させミクロヒドロゲルとした。前記混合物
にこのミクロヒドロゲル100部を添加、よく分散
させた。ついでクロタミトン15部に溶解させたフ
ルルビプロフエン9.7部を添加し、15分間混合し
た。得られた混合物を水に対する不透過処理を不
織布に厚さ1mmになるように展延し、20分間加熱
して硬化させ表面をセロフアンで覆い所望の大き
さに切断し製品とした。
実施例 11
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部と臭化水素酸スコポラミン0.2部を20分
間混合分散させた。得られた混合物を水に対し、
不透過処理をした不織布に厚さ1mmになるように
展延し、20分間加熱して硬化させ表面をセロフア
ンで覆い所望の大きさに切断し、製品とした。
実施例 12
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部と酪酸プロピオン酸ヒドロコルチゾンを
20分間混合分散させた。得られた混合物を水に対
し、不透過処理をした不織布に厚さ1mmになるよ
う展延し、20分間加熱して硬化させ表面をセロフ
アンで覆い所望の大きさに切断し、製品とした。
実施例 13
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留を吸収させミクロヒドロゲ
ルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部とクロナゼパム0.2部を20分間混合分散
させた。得られた混合物を水に対し、不透過処理
をした不織布に厚さ1mmになるように展延し、20
分間加熱して硬化させ表面をセロフアンで覆い所
望の大きさに切断し、製品とした。
実施例 14
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部とピンドロール0.8部を20分間混合分散
させた。得られた混合物を水に対し、不透過処理
をした不織布に厚さ1mmになるよう展延し、20分
間加熱して硬化させ表面をセロフアンで覆い所望
の大きさに切断し、製品とした。
実施例 15
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクヒドロ100部
を添加よく分散させた。次いで流動パラフイン10
部とグリベンクラミド1部を20分間混合分散させ
た。得られた混合物を水に対し、不透過処理をし
た不織布に厚さ1mmになるよう展延し、20分間加
熱して硬化させ表面をセロフアンで覆い所望の大
きさに切断し、製品とした。
実施例 16
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部とコルヒチン0.2部を20分間混合分散さ
せた。得られた混合物を水に対し、不透過処理を
した不織布に厚さ1mmにななるよう展延し、20分
間加熱して硬化させ表面をセロフアンで覆い所望
の大きさに切断し、製品とした。
実施例 17
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した、次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部とジメチル10部を20分間混合分散させ
た。得られた混合物を水に対し、不透過処理をし
た不織布に厚さ1mmになるよう展延し、20分間加
熱して硬化させ表面をセロフアンで覆い所望の大
きさゆ切断し、製品とした。
実施例 18
25℃で80000センチポイズの末端基がビニル基
を有するジオルガノポリシロキサンであるMDX
−4−4210(ダウコーニング社製)100部と25℃で
1200センチポイズの両末端基が活性水素原子であ
るオルガノハイドロジエンポリシロキサンで白金
含有ずみの硬化剤4部とを30℃にて8分間よく混
合した。次いでスミカゲルS−50〔(株)住友化学製〕
に自重の250倍の蒸留水を吸収させミクロヒドロ
ゲルとした。前記混合物にこのミクロヒドロゲル
100部を添加よく分散させた。次いで流動パラフ
イン10部とラニチジン10部を20分間混合分散させ
た。得られた混合物を水に対し、不透過処理をし
た不織布に厚さ1mmになるよう展延し、20分間加
熱して硬化させ表面をセロフアンで覆い所望の大
きさに切断し、製品とした。
参考例 1
下記配合で公知のパツプ剤を試作、ケトプロフ
エン含有パツプ剤参考例1とした。
基剤成分 部
ゼラチン 7
カルボキシメチルセルロース 2
ポリビニルアルコール 3
カオリンクレー 20
酸化チタン 5
水 35
ケトプロフエン 3
エチレングリコール 5
グリセリン 20
(合計100部)
参考例 2
公知のパツプ剤を下記配合で試作し、インドメ
タシン含有パツプとした。
配 合 部
ゼラチン 10
ポリビニルアルコール 3
グリセリン 20
水 38
カオリンクレー 20
酸化チタン 4
カルボキシメチルセルロース 2
インドメタシン 3
(合計100部)[Table] Test Example 4 Release Test in Water Using Examples 4 and 5 and Reference Example 2, the elution of indomethacin into water was measured. Each sample was cut into 4×4 cm 2 pieces and immersed in pure water at 30° C. to examine the relationship between immersion time and release rate (%). The results are shown in FIG. 2, and Examples 4 and 5 according to the present invention showed a much higher release rate than Reference Example 2. As is clear from the above test results. The present invention is characterized in that an organopolysiloxane obtained by reacting a diorganopolysiloxane and an organohydrodiene polysiloxane in the presence of platinum or a platinum compound is used as a base component, and a microhydrogel is dispersed in this. It can be said to be a new type of patch drug that eliminates the drawbacks of patch drugs. Hereinafter, the present invention will be explained in more detail with reference to Examples. However, it goes without saying that the present invention is not limited only to the examples. In the examples, all parts indicate parts by weight. Example 1 TSE-, a diorganopolysiloxane with vinyl end groups, 4000 centipoise at 25°C.
3032RTV [manufactured by Toshiba Silicone Corporation] 100 copies at 25℃
YE-5822B is a platinum-containing organohydrodiene polysiloxane with 250 centipoise terminal groups having active hydrogen atoms [manufactured by Toshiba Silicone Corporation]
10 parts were stirred and mixed at 30°C for 10 minutes. Separately, 45 parts of Sumikagel S-50 (manufactured by Sumitomo Chemical Co., Ltd.), which had absorbed 200 times its own weight of distilled water, was added to the organopolysiloxane mixture and well dispersed. Next, 6 parts of l-menthol, 6 parts of methyl salicylate, and 5 parts of camphor were added and mixed for 20 minutes to make it homogeneous. The resulting mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 25 minutes to harden, the surface was covered with cellophane, and the product was cut into a desired size. When this patch was applied to the human body, it had a long-lasting cooling sensation as well as medicinal efficacy, and was found to be extremely useful as an anti-inflammatory and analgesic patch. Example 2 KE-, a diorganopolysiloxane with vinyl end groups, 4000 centipoise at 25°C
106LTV [manufactured by Shin-Etsu Chemical Co., Ltd.] 100 parts and 250 centipoise at 25°C YE-5822B, an organohydrodiene polysiloxane containing active hydrogen atoms at both end groups and containing platinum [manufactured by Toshiba Silicone Co., Ltd.] 7 parts and
The mixture was stirred and mixed at 30°C for 10 minutes. On the other hand, Sunwetsu
IM-300 (manufactured by Sanyo Chemical Industries, Ltd.) was made to absorb 200 times its own weight of distilled water to form a microhydrogel. 80 parts of this microhydrogel was added to the mixture and well dispersed. Next, 10 parts of l-menthol, 10 parts of methyl salicylate, and 5 parts of camphor were added, and the mixture was stirred and mixed for 20 minutes to make it homogeneous. The resulting mixture was spread onto a water-impermeable nonwoven fabric with a thickness of 1 mm.
The mixture was spread and heated for 30 minutes to harden, and the surface was covered with polyethylene film and cut into desired sizes to produce products. When used on the human body, the results were similar to those in Example 1. Example 3 KE-, a diorganopolysiloxane with vinyl end groups, 4000 centipoise at 25°C
106LTV [manufactured by Shin-Etsu Chemical Co., Ltd.] 100 parts and 600 ~ at 25℃
9 parts of platinum-containing TSE-3032RTV-B [manufactured by Toshiba Silicone Corporation], which is an organohydrodiene polysiloxane having active hydrogen atoms in both end groups of 1000 centipoise, was stirred and mixed at 25°C for 10 minutes. Sunwet IM-300 [manufactured by Sanyo Chemical Industries, Ltd.]
It was made into a microhydrogel by absorbing 150 times its own weight of distilled water. 60 parts of this microhydrogel was added to the mixture and well dispersed. Then 5.7 g of ketoprofen dissolved in 15 parts of ethylene glycol
100% and mixed for 15 minutes until homogeneous. The resulting mixture was spread on a 500 μm thick polybutadiene sheet to a thickness of 100 μm, heated for 25 minutes to cure, and then the surface was covered with polyethylene film to prepare a product. Example 4 YE-, a diorganopolysiloxane with vinyl end groups, 70,000 centipoise at 25°C
5626 [manufactured by Toshiba Silicone Corporation] 100 parts and 600 ~ at 25℃
8 parts of platinum-containing TSE-3032RTV-B (manufactured by Toshiba Silicone Corporation), which is an organohydrodiene polysiloxane having active hydrogen atoms at both end groups of 1000 centipoise, was stirred and mixed at 25° C. for 20 minutes. On the other hand, Aqua Keep 4S (manufactured by Seitetsu Kagaku Co., Ltd.) was made to absorb 250 times its own weight of distilled water to form a microhydrogel. Add this microhydrogel to the mixture
80 parts were added and well dispersed. Then add 6 parts of indomethacin dissolved in 6 parts of crotamiton,
Mixed for 10 minutes until homogeneous. The resulting mixture is applied to a nonwoven fabric that has been treated to be impermeable to water.
It was spread to a thickness of 200 μm, and the surface was covered with cellophane to produce a finished product. Example 5 TSE-, a diorganopolysiloxane with vinyl end groups, 4000 centipoise at 25°C.
3032RTV [manufactured by Toshiba Silicone Corporation] 100 copies at 25℃
YE-5822B is a platinum-containing organohydrodiene polysiloxane with 250 centipoise end groups having active hydrogen atoms [manufactured by Toshiba Silicone Corporation]
7 parts were thoroughly mixed at 45°C for 20 minutes. On the other hand, Sumikagel N-100 (manufactured by Sumitomo Chemical Co., Ltd.) was made to absorb 200 times its own weight of distilled water to form a microhydrogel. 62 parts of this microhydrogel was added to the mixture and well dispersed. Next, 5 parts of indomethacin dissolved in 5 parts of crotamiton was added and mixed well for 30 minutes. The obtained mixture was spread on a polybutadiene sheet to a thickness of 200 μm, heated and cured for 25 minutes, and then the surface was covered with release paper to prepare a product. Example 6 KE-, a diorganopolysiloxane with vinyl end groups, 1100 centipoise at 25°C
103RTV [manufactured by Shin-Etsu Chemical Co., Ltd.] 100 parts and YE-5822B [manufactured by Toshiba Silicone Co., Ltd.], which is an organohydrodiene polysiloxane containing active hydrogen atoms at both end groups, and 602 centipoise at 25°C. 50℃
The mixture was stirred and mixed for 10 minutes. On the other hand, Sumikagel S-50
[Manufactured by Sumitomo Chemical Co., Ltd.] was made to absorb 200 times its own weight of distilled water to form a microhydrogel. 70 parts of this microhydrogel was added to the mixture and well dispersed. Next, 5.2 parts of flurbiprofen dissolved in 10 parts of diethyl sebacate was added and mixed well for 15 minutes.
The obtained mixture was spread on a nylon support (trade name: IEL N-1070 manufactured by Asahi Kasei Co., Ltd.) to a thickness of 100 μm and cured by heating for 25 minutes.The surface was covered with cellophane and the desired size was Example 7 X-32- which is a diorganopolysiloxane having a vinyl group as an end group with a temperature of 1102 centipoise at 25°C.
465-2A [manufactured by Shin-Etsu Chemical Co., Ltd.] 100 parts of X-32-465-2B, which is an organohydrodiene polysiloxane containing active hydrogen atoms at both end groups and containing platinum, at 602 centipoise at 25°C [manufactured by Shin-Etsu Chemical Co., Ltd.] 95 parts of Shin-Etsu Chemical Co., Ltd.] were added, and the mixture was stirred and mixed at 25°C for 10 minutes. On the other hand, Sunwet IM-300 (manufactured by Sanyo Kasei Co., Ltd.) was made to absorb 300 times its own weight of distilled water to form a microhydrogel. 65 parts of this microhydrogel was added to the mixture and well dispersed. Next, 0.05 part of betamethasone valerate and 1 part of propylene glycol were added and mixed well for 20 minutes. The resulting mixture was spread on release paper to a thickness of 100 μm, heated and cured for 30 minutes, covered with a polyethylene film, pressure-transferred, and cut into desired sizes to produce products. Example 8 100 parts of KE-104GEL (manufactured by Shin-Etsu Chemical Co., Ltd.), which is an organohydrodiene polysiloxane having a vinyl group as the end group of 700 centipoise at 25°C, and 25°C
10 parts of Cat104 (manufactured by Shin-Etsu Chemical Co., Ltd.), a platinum-containing organohydrodiene polysiloxane in which both end groups are active hydrogen atoms, and 80 centipoise at 20°C.
Mix well for 10 minutes. On the other hand, Sumikagel S-
50 [manufactured by Sumitomo Chemical Co., Ltd.] was made to absorb 250 times its own weight of distilled water to form a microhydrogel. Next, 5.5 parts of polyvinyl acetate dissolved in 8 parts of ethyl alcohol and 4 parts of dipyridamole were added, and the mixture was thoroughly mixed and stirred for 15 minutes so as to be uniform. The resulting mixture was spread on a nonwoven fabric to a thickness of 100 μm and cured by heating for 35 minutes. The surface was covered with release paper and the product was cut into a desired size. Example 9 KE-, a diorganopolysiloxane with vinyl end groups, 4000 centipoise at 25°C
106LTV [manufactured by Shin-Etsu Chemical Co., Ltd.] 100 parts and YE-5822B (manufactured by Toshiba Silicone Co., Ltd.), which is an organohydrodiene polysiloxane containing active hydrogen atoms at both end groups and contains platinum, 9 parts at 250 centipoise at 25°C and
The mixture was stirred and mixed at 40°C for 10 minutes. On the other hand, Sumikagel N-100 (manufactured by Sumitomo Chemical Co., Ltd.) was made to absorb 300 times its own weight of distilled water to form a microhydrogel. 50 parts of this microhydrogel was added to the mixture and well dispersed. Next, 4 parts of Alclofenuc dissolved in 5 parts of diisopropyl adipate were added and mixed well for 20 minutes. The resulting mixture was spread on a polybutadiene sheet to a thickness of 100 μm and cured by heating for 20 minutes. The surface was covered with polyethylene film and the product was cut into a desired size. Example 10 X-32- is a diorganopolysiloxane with vinyl end groups at 25°C of 10
465-2A [manufactured by Shin-Etsu Chemical Co., Ltd.] 100 parts of X-32-465-2B, which is an organohydrodiene polysiloxane containing active hydrogen atoms at both end groups and containing platinum, at 602 centipoise at 25°C [manufactured by Shin-Etsu Chemical Co., Ltd.] [manufactured by Shin-Etsu Chemical] was added thereto, and the mixture was stirred and mixed at 30°C for 5 minutes. On the other hand, Sumikagel S-50 (manufactured by Sumitomo Chemical Co., Ltd.) was made to absorb 250 times its own weight of distilled water to form a microhydrogel. 100 parts of this microhydrogel was added to the mixture and well dispersed. Then, 9.7 parts of flurbiprofen dissolved in 15 parts of crotamiton were added and mixed for 15 minutes. The resulting mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, the surface was covered with cellophane, and the product was cut into a desired size. Example 11 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
was made into a microhydrogel by absorbing 250 times its own weight in distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Next, 10 parts of liquid paraffin and 0.2 parts of scopolamine hydrobromide were mixed and dispersed for 20 minutes. The resulting mixture was added to water.
It was spread on an opaque nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, and the surface was covered with cellophane and cut into a desired size to produce a product. Example 12 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
was made into a microhydrogel by absorbing 250 times its own weight in distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Then add 10 parts of liquid paraffin and hydrocortisone butyrate propionate.
Mix and disperse for 20 minutes. The obtained mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, the surface was covered with cellophane, and the product was cut into a desired size. Example 13 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
It was made into a microhydrogel by absorbing 250 times its own weight in distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Next, 10 parts of liquid paraffin and 0.2 parts of clonazepam were mixed and dispersed for 20 minutes. The resulting mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, and
The product was cured by heating for a minute, and the surface was covered with cellophane and cut into a desired size to produce a product. Example 14 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
was made into a microhydrogel by absorbing 250 times its own weight in distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Next, 10 parts of liquid paraffin and 0.8 parts of pindolol were mixed and dispersed for 20 minutes. The obtained mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, the surface was covered with cellophane, and the product was cut into a desired size. Example 15 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
was made into a microhydrogel by absorbing 250 times its own weight in distilled water. 100 parts of this Mikuhydro was added to the mixture and well dispersed. Then liquid paraffin 10
1 part and 1 part of glibenclamide were mixed and dispersed for 20 minutes. The obtained mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, the surface was covered with cellophane, and the product was cut into a desired size. Example 16 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
was made into a microhydrogel by absorbing 250 times its own weight in distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Next, 10 parts of liquid paraffin and 0.2 parts of colchicine were mixed and dispersed for 20 minutes. The resulting mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, and the surface was covered with cellophane and cut into the desired size to form a product. . Example 17 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms as both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30°C for 8 minutes, and then mixed with Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]. ]
was made into a microhydrogel by absorbing 250 times its own weight in distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Next, 10 parts of liquid paraffin and 10 parts of dimethyl were mixed and dispersed for 20 minutes. The obtained mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, the surface was covered with cellophane, and the product was cut to a desired size. Example 18 MDX, a diorganopolysiloxane with vinyl end groups, 80,000 centipoise at 25°C
-4-4210 (manufactured by Dow Corning) 100 parts at 25℃
A 1200 centipoise organohydrodiene polysiloxane having active hydrogen atoms at both end groups and 4 parts of a platinum-containing curing agent were thoroughly mixed at 30° C. for 8 minutes. Next, Sumikagel S-50 [manufactured by Sumitomo Chemical Co., Ltd.]
was made into a microhydrogel by absorbing 250 times its own weight of distilled water. Add this microhydrogel to the mixture
100 parts were added and well dispersed. Next, 10 parts of liquid paraffin and 10 parts of ranitidine were mixed and dispersed for 20 minutes. The obtained mixture was spread on a water-impermeable nonwoven fabric to a thickness of 1 mm, heated for 20 minutes to harden, the surface was covered with cellophane, and the product was cut into a desired size. Reference Example 1 A known poultice with the following formulation was prototyped and designated as Ketoprofen-containing poultice Reference Example 1. Base components Gelatin 7 Carboxymethyl cellulose 2 Polyvinyl alcohol 3 Kaolin clay 20 Titanium oxide 5 Water 35 Ketoprofen 3 Ethylene glycol 5 Glycerin 20 (total 100 parts) Reference example 2 A known poultice was made as a prototype with the following formulation, and a poultice containing indomethacin was used. did. Ingredients Gelatin 10 Polyvinyl alcohol 3 Glycerin 20 Water 38 Kaolin clay 20 Titanium oxide 4 Carboxymethyl cellulose 2 Indomethacin 3 (Total 100 parts)
図1は本願及び市販の貼付薬を放置した時の放
置時間に対する水分残存率を示す。図2は本願及
び参考例の貼付薬を水に浸漬した時の浸漬時間に
対する薬物の放出率を示す。
FIG. 1 shows the moisture residual rate with respect to the standing time when the present application and the commercially available adhesive patch were left. FIG. 2 shows the drug release rate versus immersion time when the patches of the present application and reference examples were immersed in water.
Claims (1)
シロキサンと、両末端基が活性水素原子であるオ
ルガノハイドロジエンポリシロキサンとを、白金
又は白金化合物の存在下反応させて得られるオル
ガノポリシロキサンを基剤成分として、これにミ
クロヒドロゲルを分散させ、薬効成分を配合させ
てなることを特徴とする新規貼付薬。 2 その末端基がビニル基であるジオルガノポリ
シロキサンの粘度が600〜700000センチポイズで
あることを特徴とする特許請求の範囲第1項記載
の新規貼付薬。[Scope of Claims] 1 Obtained by reacting a diorganopolysiloxane whose terminal group is a vinyl group and an organohydrodiene polysiloxane whose terminal groups are active hydrogen atoms in the presence of platinum or a platinum compound. A new adhesive patch comprising organopolysiloxane as a base component, microhydrogel dispersed therein, and a medicinal ingredient added thereto. 2. The novel adhesive patch according to claim 1, wherein the diorganopolysiloxane whose terminal group is a vinyl group has a viscosity of 600 to 700,000 centipoise.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP57198253A JPS59104314A (en) | 1982-11-09 | 1982-11-09 | Novel plaster |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP57198253A JPS59104314A (en) | 1982-11-09 | 1982-11-09 | Novel plaster |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS59104314A JPS59104314A (en) | 1984-06-16 |
JPH0336806B2 true JPH0336806B2 (en) | 1991-06-03 |
Family
ID=16388047
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP57198253A Granted JPS59104314A (en) | 1982-11-09 | 1982-11-09 | Novel plaster |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS59104314A (en) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2632838B2 (en) * | 1986-10-23 | 1997-07-23 | 久光製薬 株式会社 | External patch |
JP2588236B2 (en) * | 1987-02-26 | 1997-03-05 | 亨 山本 | Aromatic composition |
US5429589A (en) * | 1992-04-02 | 1995-07-04 | New Dimensions In Medicine, Inc. | Hydrogel gauze wound dressing |
JP2012518061A (en) * | 2009-02-17 | 2012-08-09 | ダウ コーニング コーポレーション | Silicone gel sealing and method for forming and using the same |
AU2017232433B2 (en) | 2016-03-14 | 2020-01-16 | Trio Healthcare Limited | Skin compatible composition |
GB201616223D0 (en) * | 2016-09-23 | 2016-11-09 | University College Cardiff Consultants Limited | Topical treatment patch |
GB201904403D0 (en) * | 2019-03-29 | 2019-05-15 | Trio Healthcare Ltd | Skin compatible silicone composition |
-
1982
- 1982-11-09 JP JP57198253A patent/JPS59104314A/en active Granted
Also Published As
Publication number | Publication date |
---|---|
JPS59104314A (en) | 1984-06-16 |
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