JPH0529008B2 - - Google Patents
Info
- Publication number
- JPH0529008B2 JPH0529008B2 JP60102165A JP10216585A JPH0529008B2 JP H0529008 B2 JPH0529008 B2 JP H0529008B2 JP 60102165 A JP60102165 A JP 60102165A JP 10216585 A JP10216585 A JP 10216585A JP H0529008 B2 JPH0529008 B2 JP H0529008B2
- Authority
- JP
- Japan
- Prior art keywords
- weight
- urea
- external preparation
- oil
- hydrogenated
- 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
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 30
- 238000002360 preparation method Methods 0.000 description 30
- 239000000203 mixture Substances 0.000 description 20
- 239000004202 carbamide Substances 0.000 description 15
- 238000009472 formulation Methods 0.000 description 11
- 239000003921 oil Substances 0.000 description 10
- 235000019198 oils Nutrition 0.000 description 10
- 230000001225 therapeutic effect Effects 0.000 description 10
- -1 liquid paraffin Chemical class 0.000 description 9
- 150000003904 phospholipids Chemical class 0.000 description 9
- 235000014113 dietary fatty acids Nutrition 0.000 description 8
- 229930195729 fatty acid Natural products 0.000 description 8
- 239000000194 fatty acid Substances 0.000 description 8
- 239000007788 liquid Substances 0.000 description 8
- 238000002845 discoloration Methods 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 238000003860 storage Methods 0.000 description 6
- 150000004665 fatty acids Chemical class 0.000 description 5
- 239000012071 phase Substances 0.000 description 5
- 239000002270 dispersing agent Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 150000002148 esters Chemical class 0.000 description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 3
- 150000001298 alcohols Chemical class 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 235000011187 glycerol Nutrition 0.000 description 3
- 229910052740 iodine Inorganic materials 0.000 description 3
- 239000011630 iodine Substances 0.000 description 3
- 229940057995 liquid paraffin Drugs 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 239000008347 soybean phospholipid Substances 0.000 description 3
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 3
- 239000004094 surface-active agent Substances 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
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-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
- 201000004624 Dermatitis Diseases 0.000 description 2
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 description 2
- 206010020649 Hyperkeratosis Diseases 0.000 description 2
- 208000001126 Keratosis Diseases 0.000 description 2
- 206010040880 Skin irritation Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 235000006708 antioxidants Nutrition 0.000 description 2
- LVTYICIALWPMFW-UHFFFAOYSA-N diisopropanolamine Chemical compound CC(O)CNCC(C)O LVTYICIALWPMFW-UHFFFAOYSA-N 0.000 description 2
- 229940043276 diisopropanolamine Drugs 0.000 description 2
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 description 2
- 201000006549 dyspepsia Diseases 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 229930184727 ginkgolide Natural products 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-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
- 206010021198 ichthyosis Diseases 0.000 description 2
- 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 2
- 239000004310 lactic acid Substances 0.000 description 2
- 235000014655 lactic acid Nutrition 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 235000019271 petrolatum Nutrition 0.000 description 2
- 230000000750 progressive effect Effects 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 230000036556 skin irritation Effects 0.000 description 2
- 231100000475 skin irritation Toxicity 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 235000015112 vegetable and seed oil Nutrition 0.000 description 2
- 239000008158 vegetable oil Substances 0.000 description 2
- 239000003871 white petrolatum Substances 0.000 description 2
- JQWAHKMIYCERGA-UHFFFAOYSA-N (2-nonanoyloxy-3-octadeca-9,12-dienoyloxypropoxy)-[2-(trimethylazaniumyl)ethyl]phosphinate Chemical class CCCCCCCCC(=O)OC(COP([O-])(=O)CC[N+](C)(C)C)COC(=O)CCCCCCCC=CCC=CCCCCC JQWAHKMIYCERGA-UHFFFAOYSA-N 0.000 description 1
- RDEIXVOBVLKYNT-VQBXQJRRSA-N (2r,3r,4r,5r)-2-[(1s,2s,3r,4s,6r)-4,6-diamino-3-[(2r,3r,6s)-3-amino-6-(1-aminoethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol;(2r,3r,4r,5r)-2-[(1s,2s,3r,4s,6r)-4,6-diamino-3-[(2r,3r,6s)-3-amino-6-(aminomethyl)oxan-2-yl]o Chemical compound OS(O)(=O)=O.O1C[C@@](O)(C)[C@H](NC)[C@@H](O)[C@H]1O[C@@H]1[C@@H](O)[C@H](O[C@@H]2[C@@H](CC[C@@H](CN)O2)N)[C@@H](N)C[C@H]1N.O1C[C@@](O)(C)[C@H](NC)[C@@H](O)[C@H]1O[C@@H]1[C@@H](O)[C@H](O[C@@H]2[C@@H](CC[C@H](O2)C(C)N)N)[C@@H](N)C[C@H]1N.O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N RDEIXVOBVLKYNT-VQBXQJRRSA-N 0.000 description 1
- YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 description 1
- ALSTYHKOOCGGFT-KTKRTIGZSA-N (9Z)-octadecen-1-ol Chemical compound CCCCCCCC\C=C/CCCCCCCCO ALSTYHKOOCGGFT-KTKRTIGZSA-N 0.000 description 1
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical class CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 description 1
- RZRNAYUHWVFMIP-KTKRTIGZSA-N 1-oleoylglycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-KTKRTIGZSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- FKOKUHFZNIUSLW-UHFFFAOYSA-N 2-Hydroxypropyl stearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(C)O FKOKUHFZNIUSLW-UHFFFAOYSA-N 0.000 description 1
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 1
- ZVTDEEBSWIQAFJ-KHPPLWFESA-N 2-hydroxypropyl (z)-octadec-9-enoate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(C)O ZVTDEEBSWIQAFJ-KHPPLWFESA-N 0.000 description 1
- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 235000019489 Almond oil Nutrition 0.000 description 1
- 206010003645 Atopy Diseases 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- WJLVQTJZDCGNJN-UHFFFAOYSA-N Chlorhexidine hydrochloride Chemical compound Cl.Cl.C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 WJLVQTJZDCGNJN-UHFFFAOYSA-N 0.000 description 1
- 239000004287 Dehydroacetic acid Substances 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 235000016623 Fragaria vesca Nutrition 0.000 description 1
- 240000009088 Fragaria x ananassa Species 0.000 description 1
- 235000011363 Fragaria x ananassa Nutrition 0.000 description 1
- DCXXMTOCNZCJGO-UHFFFAOYSA-N Glycerol trioctadecanoate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 1
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 description 1
- 244000215562 Heliotropium arborescens Species 0.000 description 1
- 244000178870 Lavandula angustifolia Species 0.000 description 1
- 235000010663 Lavandula angustifolia Nutrition 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 206010033554 Palmoplantar keratoderma Diseases 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 241000220317 Rosa Species 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- BHEOSNUKNHRBNM-UHFFFAOYSA-N Tetramethylsqualene Natural products CC(=C)C(C)CCC(=C)C(C)CCC(C)=CCCC=C(C)CCC(C)C(=C)CCC(C)C(C)=C BHEOSNUKNHRBNM-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 1
- 229930003316 Vitamin D Natural products 0.000 description 1
- 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 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 206010048218 Xeroderma Diseases 0.000 description 1
- FPVRUILUEYSIMD-RPRRAYFGSA-N [(8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] acetate 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(C)=O)[C@@]1(C)C[C@@H]2O FPVRUILUEYSIMD-RPRRAYFGSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 125000001931 aliphatic group Chemical group 0.000 description 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 1
- 239000008168 almond oil Substances 0.000 description 1
- 229940072049 amyl acetate Drugs 0.000 description 1
- PGMYKACGEOXYJE-UHFFFAOYSA-N anhydrous amyl acetate Natural products CCCCCOC(C)=O PGMYKACGEOXYJE-UHFFFAOYSA-N 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 229960004311 betamethasone valerate Drugs 0.000 description 1
- 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 1
- PXGPQCBSBQOPLZ-UHFFFAOYSA-N butanoic acid;propanoic acid Chemical compound CCC(O)=O.CCCC(O)=O PXGPQCBSBQOPLZ-UHFFFAOYSA-N 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 229960003333 chlorhexidine gluconate Drugs 0.000 description 1
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 1
- 229960004504 chlorhexidine hydrochloride Drugs 0.000 description 1
- ALSTYHKOOCGGFT-UHFFFAOYSA-N cis-oleyl alcohol Natural products CCCCCCCCC=CCCCCCCCCO ALSTYHKOOCGGFT-UHFFFAOYSA-N 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 229940061632 dehydroacetic acid Drugs 0.000 description 1
- 235000019258 dehydroacetic acid Nutrition 0.000 description 1
- JEQRBTDTEKWZBW-UHFFFAOYSA-N dehydroacetic acid Chemical compound CC(=O)C1=C(O)OC(C)=CC1=O JEQRBTDTEKWZBW-UHFFFAOYSA-N 0.000 description 1
- PGRHXDWITVMQBC-UHFFFAOYSA-N dehydroacetic acid Natural products CC(=O)C1C(=O)OC(C)=CC1=O PGRHXDWITVMQBC-UHFFFAOYSA-N 0.000 description 1
- 229960001378 dequalinium chloride Drugs 0.000 description 1
- LTNZEXKYNRNOGT-UHFFFAOYSA-N dequalinium chloride Chemical compound [Cl-].[Cl-].C1=CC=C2[N+](CCCCCCCCCC[N+]3=C4C=CC=CC4=C(N)C=C3C)=C(C)C=C(N)C2=C1 LTNZEXKYNRNOGT-UHFFFAOYSA-N 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 229960003657 dexamethasone acetate Drugs 0.000 description 1
- 229960000520 diphenhydramine Drugs 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000008344 egg yolk phospholipid Substances 0.000 description 1
- 229940068998 egg yolk phospholipid Drugs 0.000 description 1
- 229960003720 enoxolone Drugs 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 239000003925 fat Chemical class 0.000 description 1
- 229960001347 fluocinolone acetonide Drugs 0.000 description 1
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000000417 fungicide Substances 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- MNWFXJYAOYHMED-UHFFFAOYSA-M heptanoate Chemical compound CCCCCCC([O-])=O MNWFXJYAOYHMED-UHFFFAOYSA-M 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 229960000905 indomethacin Drugs 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 description 1
- 229960003517 isothipendyl Drugs 0.000 description 1
- OQJBSDFFQWMKBQ-UHFFFAOYSA-N isothipendyl Chemical compound C1=CN=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 OQJBSDFFQWMKBQ-UHFFFAOYSA-N 0.000 description 1
- 239000001102 lavandula vera Substances 0.000 description 1
- 235000018219 lavender Nutrition 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 1
- 239000013081 microcrystal Substances 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- OIXVKQDWLFHVGR-WQDIDPJDSA-N neomycin B sulfate Chemical compound OS(O)(=O)=O.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 OIXVKQDWLFHVGR-WQDIDPJDSA-N 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 201000008743 palmoplantar keratosis Diseases 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229940093625 propylene glycol monostearate Drugs 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- 239000012177 spermaceti Substances 0.000 description 1
- 229940084106 spermaceti Drugs 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 229940031439 squalene Drugs 0.000 description 1
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- YZMCKZRAOLZXAZ-UHFFFAOYSA-N sulfisomidine Chemical compound CC1=NC(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 YZMCKZRAOLZXAZ-UHFFFAOYSA-N 0.000 description 1
- 229960001975 sulfisomidine Drugs 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
Description
(産業上の利用分野)
本発明は外用製剤に関し、更に詳しくは皮膚角
化異常症の治療に用いる外用製剤に関する。
(従来の技術)
魚鱗癬、老人性乾皮症、アトピー皮膚、進行性
指掌角皮症(乾燥タイプの主婦湿疹)、足蹠部皹
裂性皮膚炎、掌蹠角化症、毛孔性苔癬などの皮膚
角化異常症の治療には尿素含有外用剤が有効であ
る。尿素は水溶性であるため、従来は尿素水溶液
を合成界面活性剤で油脂成分に分散した乳剤性軟
膏、クリーム、ローシヨンとして使用されてい
た。
(発明が解決しようとする問題点)
しかしながら、これらの製剤中に含有されてい
る合成界面活性剤は、皮膚からの水分蒸散を促進
し、尿素含有外用剤の治療効果を著しく減少させ
てしまう。
(問題点を解決するための手段)
本発明者らは、従来の尿素含有外用剤の欠点を
解消すべく鋭意研究を重さねた結果、分散剤とし
て水素添加リン脂質を用いることにより皮膚角化
異常症に対する尿素含有外用剤の治療効果が著し
く増大することを見出し、本発明を完成した。
(問題点を解決するための手段)
本発明者らは、従来の尿素含有外用剤の欠点を
解消すべく鋭意研究を重さねた結果、分散剤とし
て水素添加リン脂質を用いることにより皮膚角化
異常症に対する尿素含有外用剤の治療効果を増大
するとともに長期保存による製剤の変質をおこさ
ないことを見出して本発明を完成した。
本発明の目的物は尿素、水素添加リン脂質、水
および油脂成分を含有してなる外用製剤である。
本発明において、尿素は全量の2〜30重量%、
好ましくは5〜20重量%を配合する。この範囲以
下の配合量では治療効果は期待し難く、この範囲
以上の配合量では皮膚に対する刺激が強すぎて実
用的ではない。
水素添加リン脂質は大豆リン脂質、卵黄リン脂
質などのリン脂質に水素添加したもの、好ましく
はヨウ素価が15以下のものを用い、全量の0.2〜
30重量%、好ましくは1〜20重量%を配合する。
水は精製水を用い、全量の5〜80重量%、好ま
しくはO/Wタイプの製剤では30〜80重量%、
W/Oタイプの製剤では5〜15重量%を配合す
る。
油脂成分は液状〜固体状の炭化水素(たとえ
ば、流動パラフイン、白色ワセリン、固形パラフ
イン、ミクロクリスタルワツクス、スクラワン、
スクワレンなど)、脂肪族高級アルコール(たと
えば、セチルアルコール、ヘキサデシルアルコー
ル、ステアリルアルコール、オレインアルコール
など)、高級脂肪酸と高級アルコールのエステル
(たとえば、ミツロウ、鯨ロウなど)、高級脂肪酸
と低級アルコールのエステル(たとえば、ミリス
チン酸イソプロピル、パルミチン酸イソプロピル
など)、植物油(たとえば、オリーブ油、アーモ
ンド油、落花生油など)、改質植物油(たとえば、
硬化ヒマシ油、中鎖脂肪酸グリセライドなど)、
脂肪酸とグリセリンのエステル(たとえば、グリ
セリンモノステアレート、グリセリンモノオレー
トなど)、脂肪酸とプロピレングリコールのエス
テル(たとえば、プロピレングリコールモノステ
アレート、プロピレングリコールモノオレートな
ど)、高級脂肪酸(たとえば、パルミチン酸、ス
テアリン酸など)を用い、O/Wタイプの製剤に
おいては全量の5〜60重量%、好ましくは10〜30
重量%、W/Oタイプの製剤においては全量の70
〜90重量%、好ましくは80〜88重量%を配合す
る。
この他必要に応じて、ゲル化剤〔製剤の保存安
定性を増大;全量の0.01〜2重量%、好ましくは
0.02〜0.5重量%を配合;たとえば、カルボキシ
メチルセルロース、カルボキシビニルポリマー
(ハイビスワコー:商品名、和光純薬(株)製)、ポリ
ビニルアルコールなど〕、湿潤剤(製剤の湿潤作
用を増大;全量の0.1〜20重量%、好ましくは0.5
〜10重量%を配合;たとえば、プロピレングリコ
ール、グリセリン、ソルビツトなど)、キレート
剤(製剤の保存安定性を増大;たとえば、エチレ
ンジアミンテトラ酢酸ジナトリウムなど)、防腐
剤(たとえば、パラオキシ安息香酸メチル、同エ
チル、同プロピル、同ブチル、デヒドロ酢酸およ
びその塩など)、PH調整剤(たとえば、クエン酸、
乳酸、酒石酸およびその塩並びにジイソプロパノ
ールアミンなど:調整すべきPHは製剤の安定性に
基づいて決定され、製剤は通常弱酸性ないし弱ア
ルカリ性に保たれるのが好ましい。)などを配合
することができる。
また必要があれば、抗生物質(たとえば、硫酸
ゲンタマイシン、硫酸フラジオマイシンなど)、
抗ヒスタミン剤(たとえば、ジフエンヒドラミ
ン、塩酸イソチペンジルなど)、殺菌剤(たとえ
ば、塩化デカリニウム、塩酸クロルヘキシジン、
グルコン酸クロルヘキシジン、スルフイソミジン
など)、抗炎症剤(たとえば、グリチルレチン酸、
インドメタシン、酢酸デキサメタゾン、フルオシ
ノロンアセトニド、吉草酸ベタメタゾン、酪酸プ
ロピオン酸ヒドロコルチゾンなど)、ビタミン酸
(たとえば、ビタミンA、ビタミンD、ビタミン
Eなど)などの薬効成分および香料(たとえば、
ラベンダー、ネロリー、ストロベリー、ヘリオト
ロープ、ローズ、アミルアセテートなど)を適宜
組み合わせて配合することができる。
さらにまた必要があれば、皮膚に対する刺激が
少ない非イオン界面活性剤(たとえば、脂肪酸モ
ノグリセライド類、ソルビタン脂肪酸エステル
類、ポリオキシエチレン高級脂肪酸エステル類な
ど)を尿素の効果を低下させない程度に少量配合
することができる。
本発明の外用製剤は、たとえば下記の方法によ
り製造することができる。
すなわち、加温した油脂成分に水素添加リン脂
質を溶解し、これに加温した尿素水溶液を加えて
撹拌しながら冷却するか、または全成分をすべて
混合し、加温撹拌後冷却する。
製造上特に注意すべき点はないが、加温時撹拌
の際にホモミキサーなどを用いてエマルジヨンの
粒子を微細化することにより保存安定性が大きい
外用製剤を得ることができる。
(作用)
リン脂質を配合した製剤は、長期保存によつて
ときには変色するなどの不都合を生ずることがあ
る。
しかしながら、本発明の外用製剤は、分散剤と
して水素添加リン脂質、特にヨウ素価15以下の水
素添加リン脂質を用いることにより、抗酸化剤を
用いることがなくても保存中に製剤の変色をおこ
さず、分散剤として合成界面活性剤を用いた尿素
含有外用剤よりも皮膚角化異常症に対する治療効
果が著しく増大する。
以下、試験例を挙げて本発明の外用製剤の作用
を示す。
試験例 1
ヨウ素価の異なる大豆リン脂質または水素添加
大豆リン脂質にそれぞれ10重量%用いて、後記実
施例1に従つてクリーム状の各種試料を調製し
た。
この各種試料50gを内容量60gの透明ガラスビ
ンにいれ、40℃恒温室に保存してその経時変化を
調べた。
その結果を第1表に示す。
(Industrial Application Field) The present invention relates to an external preparation, and more particularly to an external preparation used for the treatment of skin dyskeratosis. (Conventional technology) Ichthyosis, senile xeroderma, atopic skin, progressive digital palmar keratoderma (dry type of housewife's eczema), footpad fissuring dermatitis, palmoplantar keratosis, lichen pilaris External preparations containing urea are effective for the treatment of skin dyskeratosis such as. Since urea is water-soluble, it has conventionally been used in emulsion ointments, creams, and lotions in which an aqueous urea solution is dispersed in oil and fat components using a synthetic surfactant. (Problems to be Solved by the Invention) However, the synthetic surfactants contained in these preparations promote water evaporation from the skin, significantly reducing the therapeutic effect of urea-containing external preparations. (Means for Solving the Problems) As a result of extensive research in order to eliminate the drawbacks of conventional urea-containing topical preparations, the present inventors have developed a solution to skin irritation by using hydrogenated phospholipids as a dispersant. The present invention has been completed based on the discovery that the therapeutic effect of a urea-containing external preparation for dyspepsia is significantly increased. (Means for Solving the Problems) As a result of extensive research in order to eliminate the drawbacks of conventional urea-containing topical preparations, the present inventors have developed a solution to skin irritation by using hydrogenated phospholipids as a dispersant. The present invention was completed based on the discovery that the therapeutic effect of a urea-containing external preparation for dyspepsia is increased and that the preparation does not deteriorate during long-term storage. The object of the present invention is an external preparation containing urea, hydrogenated phospholipids, water, and oil and fat components. In the present invention, urea is 2 to 30% by weight of the total amount,
Preferably, it is blended in an amount of 5 to 20% by weight. If the amount is less than this range, no therapeutic effect can be expected, and if the amount is more than this range, the irritation to the skin will be too strong to be practical. Hydrogenated phospholipids are hydrogenated phospholipids such as soybean phospholipids and egg yolk phospholipids, preferably those with an iodine value of 15 or less, and 0.2 to 0.2 of the total amount.
30% by weight, preferably 1 to 20% by weight. For water, use purified water, 5 to 80% by weight of the total amount, preferably 30 to 80% by weight for O/W type formulations,
In W/O type preparations, the amount is 5 to 15% by weight. The oil and fat components are liquid to solid hydrocarbons (e.g., liquid paraffin, white petrolatum, solid paraffin, microcrystal wax, squalane,
(e.g., squalene), aliphatic higher alcohols (e.g., cetyl alcohol, hexadecyl alcohol, stearyl alcohol, oleic alcohol, etc.), esters of higher fatty acids and higher alcohols (e.g., beeswax, spermaceti, etc.), esters of higher fatty acids and lower alcohols. (e.g., isopropyl myristate, isopropyl palmitate, etc.), vegetable oils (e.g., olive oil, almond oil, peanut oil, etc.), modified vegetable oils (e.g.,
hydrogenated castor oil, medium chain fatty acid glycerides, etc.)
Esters of fatty acids and glycerin (e.g., glycerin monostearate, glycerin monooleate, etc.), esters of fatty acids and propylene glycol (e.g., propylene glycol monostearate, propylene glycol monooleate, etc.), higher fatty acids (e.g., palmitic acid, stearin, etc.) acids, etc.), and in O/W type preparations, 5 to 60% by weight of the total amount, preferably 10 to 30% by weight of the total amount.
% by weight, 70% of the total amount in W/O type formulations
~90% by weight, preferably 80-88% by weight. In addition, if necessary, a gelling agent [increases the storage stability of the preparation; 0.01 to 2% by weight of the total amount, preferably
Contains 0.02 to 0.5% by weight; for example, carboxymethylcellulose, carboxyvinyl polymer (Hibis Wako: trade name, manufactured by Wako Pure Chemical Industries, Ltd.), polyvinyl alcohol, etc.), wetting agent (increases the wetting effect of the preparation; 0.1% of the total amount) ~20% by weight, preferably 0.5
~10% by weight; e.g., propylene glycol, glycerin, sorbitate, etc.), chelating agents (increases storage stability of the formulation; e.g., disodium ethylenediaminetetraacetate), preservatives (e.g., methyl paraoxybenzoate, ethyl, propyl, butyl, dehydroacetic acid and its salts), PH regulators (e.g. citric acid,
Lactic acid, tartaric acid and its salts, diisopropanolamine, etc.: The pH to be adjusted is determined based on the stability of the formulation, and the formulation is usually preferably kept weakly acidic to weakly alkaline. ) etc. can be blended. If necessary, antibiotics (e.g., gentamicin sulfate, fradiomycin sulfate, etc.)
Antihistamines (e.g., diphenhydramine, isothipendyl hydrochloride, etc.), fungicides (e.g., dequalinium chloride, chlorhexidine hydrochloride, etc.)
chlorhexidine gluconate, sulfisomidine), anti-inflammatory agents (e.g. glycyrrhetinic acid,
medicinal ingredients such as indomethacin, dexamethasone acetate, fluocinolone acetonide, betamethasone valerate, hydrocortisone propionate butyrate), vitamin acids (e.g. vitamin A, vitamin D, vitamin E, etc.) and fragrances (e.g.
lavender, neroli, strawberry, heliotrope, rose, amyl acetate, etc.) can be blended in appropriate combinations. Furthermore, if necessary, add a small amount of nonionic surfactant that is less irritating to the skin (for example, fatty acid monoglycerides, sorbitan fatty acid esters, polyoxyethylene higher fatty acid esters, etc.) to the extent that it does not reduce the effectiveness of urea. be able to. The external preparation of the present invention can be produced, for example, by the method described below. That is, a hydrogenated phospholipid is dissolved in a heated fat or oil component, a heated aqueous urea solution is added thereto, and the mixture is cooled while stirring, or all components are mixed together, heated and stirred, and then cooled. Although there are no particular precautions to be taken during production, a preparation for external use with high storage stability can be obtained by making the emulsion particles finer using a homomixer or the like during stirring during heating. (Effect) Preparations containing phospholipids may sometimes cause problems such as discoloration when stored for a long period of time. However, by using a hydrogenated phospholipid, especially a hydrogenated phospholipid with an iodine value of 15 or less, as a dispersant, the external preparation of the present invention does not cause discoloration of the preparation during storage even without using an antioxidant. First, the therapeutic effect on skin dyskeratosis is significantly greater than that of a urea-containing external preparation that uses a synthetic surfactant as a dispersant. Hereinafter, the effects of the external preparation of the present invention will be illustrated by giving test examples. Test Example 1 Various creamy samples were prepared according to Example 1 described below using 10% by weight of soybean phospholipids or hydrogenated soybean phospholipids having different iodine values. 50g of each sample was placed in a transparent glass bottle with a content of 60g and stored in a constant temperature room at 40°C to examine changes over time. The results are shown in Table 1.
【表】
△:僅かに変色する
×:著しく変色する
試験例 2
後記実施例1に準じて第2表に示す処方の試料
1〜3を調製した。
中程度の症状を示す進行性指掌角皮症の主婦
(23〜35才)10名を1群として3群を用意し、毎
日水仕事および就寝前に前記各試料をそれぞれ別
個の群の主婦の患部に適量塗布し、1週間後およ
び2週間後の症状の改善度を調べ、それを該当人
数で表わした。
その結果を第3表に示す。[Table] △: Slight discoloration ×: Significant discoloration Test Example 2 Samples 1 to 3 of the formulations shown in Table 2 were prepared according to Example 1 described later. Three groups were prepared, each consisting of 10 housewives (23-35 years old) with progressive digital palmar keratoderma exhibiting moderate symptoms, and each sample was administered to separate groups of housewives each day before washing and before going to bed. An appropriate amount was applied to the affected area, and the degree of improvement in symptoms was examined one week and two weeks later, and the results were expressed in terms of the number of people affected. The results are shown in Table 3.
【表】【table】
【表】
(発明の効果)
本発明の外用製剤は、皮膚角化異常症に対する
治療効果が高く、抗酸化剤を使用することなしに
保存中の製剤の変色、変質を避けることができ、
医薬として利用するができる。
(実施例)
以下、実施例を挙げて本発明を具体的に説明す
る。
実施例 1
水素添加大豆リン脂質100gを流動パラフイン
300gに加温溶解し、これにパラオキシ安息香酸
エチル2gを加えて溶解し、油相液を調製した。
また、尿素100gを精製水394.5gに溶解し、こ
れに乳酸2g、乳酸ナトリウム1g、エチレンジ
アミンテトラ酢酸エチルジナトリウム0.5gを加
えて溶解した後、更にグリセリン100gを加えて
加温、溶解して水相液を調製した。
75℃に加温した前記油相液にほぼ同温度に加温
した水相液を加え、ホモミキサーを用い、
5000rpmで20分間撹拌し、その後撹拌しながら室
温まで冷却してクリーム状の外用製剤1000gを得
た。
本品を40℃3個月間保存してその状態を調べた
が、変色、異臭は認められなかつた。
実施例 2
水素添加卵黄レシチン10g、白色ワセリン10
g、流動パラフイン100g、パラオキシ安息香酸
メチル4gを加温、溶解し、油相液を調製した。
また尿素100gを精製水773.8gに溶解し、これ
にハイビスワコー2gを添加して分散させた後、
ジイソプロパノールアミン0.2gを添加して水相
液を調製した。
70℃に加温した前記油相液にほぼ同温度に加温
した前記水相液を加え、ホモミキサーを用いて
5000rpmで15分間撹拌し、その後撹拌しながら室
温まで冷却してローシヨン状の外用製剤1000gを
得た。
本品を40℃で3個月間保存してその状態を調べ
たが、変色、異臭は認められなかつた。
実施例 3
実施例1に準じて、下記処方のクリーム状外用
製剤を調製した。[Table] (Effects of the invention) The external preparation of the present invention has a high therapeutic effect on skin dyskeratosis, and can avoid discoloration and deterioration of the preparation during storage without using antioxidants.
It can be used as a medicine. (Example) Hereinafter, the present invention will be specifically described with reference to Examples. Example 1 100g of hydrogenated soybean phospholipid was added to liquid paraffin.
300 g was heated and dissolved, and 2 g of ethyl paraoxybenzoate was added and dissolved to prepare an oil phase liquid. In addition, 100 g of urea was dissolved in 394.5 g of purified water, 2 g of lactic acid, 1 g of sodium lactate, and 0.5 g of ethyl disodium ethylenediaminetetraacetate were added and dissolved, and then 100 g of glycerin was added, heated, dissolved, and water was added. A phase solution was prepared. The aqueous phase liquid heated to approximately the same temperature is added to the oil phase liquid heated to 75°C, and using a homomixer,
The mixture was stirred at 5000 rpm for 20 minutes, and then cooled to room temperature while stirring to obtain 1000 g of a creamy external preparation. This product was stored at 40°C for 3 months and its condition was examined, but no discoloration or unusual odor was observed. Example 2 Hydrogenated egg yolk lecithin 10g, white petrolatum 10g
g, 100 g of liquid paraffin, and 4 g of methyl p-oxybenzoate were heated and dissolved to prepare an oil phase liquid. In addition, 100 g of urea was dissolved in 773.8 g of purified water, and 2 g of Hibis Wako was added to it to disperse it.
An aqueous phase liquid was prepared by adding 0.2 g of diisopropanolamine. Add the aqueous phase liquid heated to approximately the same temperature to the oil phase liquid heated to 70°C, and mix using a homomixer.
The mixture was stirred at 5,000 rpm for 15 minutes, and then cooled to room temperature while stirring to obtain 1,000 g of a lotion-like external preparation. This product was stored at 40℃ for 3 months and its condition was examined, but no discoloration or unusual odor was observed. Example 3 According to Example 1, a cream-like external preparation having the following formulation was prepared.
【表】
実施例 4
実施例1に準じて下記処方のクリーム状外用製
剤を調製した。[Table] Example 4 According to Example 1, a cream-like external preparation with the following formulation was prepared.
【表】
実施例 5
実施例1に準じて下記処方のクリーム状外用製
剤を調製した。[Table] Example 5 According to Example 1, a cream-like external preparation with the following formulation was prepared.
【表】
実施例 6
実施例1に準じて下記処方の油性軟膏状外用製
剤を調製した。[Table] Example 6 According to Example 1, an oil-based ointment-like external preparation with the following formulation was prepared.
【表】
実施例 7
実施例1に準じて下記処方の油性溶液状の外用
製剤を得た。[Table] Example 7 According to Example 1, an oil-based solution for external use having the following formulation was obtained.
【表】【table】
1 有効量のギンゴーライド又はギンゴーライド
誘導体及び薬学的に許容し得る担体を含有してな
る血小板活性化因子によつて誘発される病気の治
療用組成物。
2 ギンゴーライドはギンゴーライドA、ギンゴ
ーライドB、ギンゴーライドC及びギンゴーライ
ドMからなる群から選ばれる特許請求の範囲第1
項記載の治療用組成物。
3 ギンゴーライドとしてギンゴーライドBを10
〜150mgの量で含有する経口用投与に適する形態
の特許請求の範囲第1項記載の治療用組成物。
4 ギンゴーライドとしてギンゴーライドBを1
〜20mgの量で含有する静脈内投与に適する形態の
特許請求の範囲第1項記載の治療用組成物。
5 ギンゴーライドとしてギンゴーライドBをス
プレー式1用量当り約1mgの量で含有するスプレ
ー吸入用投与に適する形態の特許請求の範囲第1
項記載の治療用組成物。
1. A composition for treating diseases induced by platelet activating factors, comprising an effective amount of ginkgolide or a ginkgolide derivative and a pharmaceutically acceptable carrier. 2. Gingoride is selected from the group consisting of Gingoride A, Gingoride B, Gingoride C, and Gingoride M. Claim 1
Therapeutic compositions described in Section. 3 Gingo Ride B as Gingo Ride 10
A therapeutic composition according to claim 1 in a form suitable for oral administration containing in an amount of 150 mg. 4 Gingo Ride B as Gingo Ride 1
A therapeutic composition according to claim 1 in a form suitable for intravenous administration containing in an amount of ~20 mg. 5 Claim 1 in a form suitable for spray inhalation administration containing Gingolide B as Gingolide in an amount of about 1 mg per spray dose
Therapeutic compositions described in Section.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP60102165A JPS61260016A (en) | 1985-05-14 | 1985-05-14 | Pharmaceutical preparation for external use |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP60102165A JPS61260016A (en) | 1985-05-14 | 1985-05-14 | Pharmaceutical preparation for external use |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS61260016A JPS61260016A (en) | 1986-11-18 |
JPH0529008B2 true JPH0529008B2 (en) | 1993-04-28 |
Family
ID=14320096
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP60102165A Granted JPS61260016A (en) | 1985-05-14 | 1985-05-14 | Pharmaceutical preparation for external use |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS61260016A (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002167328A (en) * | 2000-11-29 | 2002-06-11 | Toyo Aerosol Ind Co Ltd | Composition and aerosol composition for external skin preparation |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS58201708A (en) * | 1982-05-18 | 1983-11-24 | Asahi Chem Ind Co Ltd | Cosmetic composition |
-
1985
- 1985-05-14 JP JP60102165A patent/JPS61260016A/en active Granted
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS58201708A (en) * | 1982-05-18 | 1983-11-24 | Asahi Chem Ind Co Ltd | Cosmetic composition |
Also Published As
Publication number | Publication date |
---|---|
JPS61260016A (en) | 1986-11-18 |
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