JPH06511255A - 微結晶性セルローススフェロニゼーション組成物 - Google Patents
微結晶性セルローススフェロニゼーション組成物Info
- Publication number
- JPH06511255A JPH06511255A JP5511647A JP51164793A JPH06511255A JP H06511255 A JPH06511255 A JP H06511255A JP 5511647 A JP5511647 A JP 5511647A JP 51164793 A JP51164793 A JP 51164793A JP H06511255 A JPH06511255 A JP H06511255A
- Authority
- JP
- Japan
- Prior art keywords
- composition
- drug
- spheronization
- microcrystalline cellulose
- hydrocolloid
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims description 65
- 229920000168 Microcrystalline cellulose Polymers 0.000 title claims description 43
- 239000008108 microcrystalline cellulose Substances 0.000 title claims description 42
- 235000019813 microcrystalline cellulose Nutrition 0.000 title claims description 42
- 229940016286 microcrystalline cellulose Drugs 0.000 title claims description 42
- 238000005563 spheronization Methods 0.000 title claims description 26
- 229940079593 drug Drugs 0.000 claims description 39
- 239000003814 drug Substances 0.000 claims description 39
- 239000000416 hydrocolloid Substances 0.000 claims description 32
- 235000010980 cellulose Nutrition 0.000 claims description 28
- 229920002678 cellulose Polymers 0.000 claims description 28
- 239000001913 cellulose Substances 0.000 claims description 28
- 238000004519 manufacturing process Methods 0.000 claims description 19
- 238000000034 method Methods 0.000 claims description 18
- 239000002002 slurry Substances 0.000 claims description 12
- 239000007787 solid Substances 0.000 claims description 12
- 229920000609 methyl cellulose Polymers 0.000 claims description 11
- 239000001923 methylcellulose Substances 0.000 claims description 11
- 235000010981 methylcellulose Nutrition 0.000 claims description 11
- 239000008187 granular material Substances 0.000 claims description 9
- 239000007909 solid dosage form Substances 0.000 claims description 7
- 239000002245 particle Substances 0.000 claims description 6
- 238000001694 spray drying Methods 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 8
- 238000005516 engineering process Methods 0.000 description 7
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 6
- 235000012970 cakes Nutrition 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 238000001125 extrusion Methods 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 230000003993 interaction Effects 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 230000008569 process Effects 0.000 description 4
- 229960000278 theophylline Drugs 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 239000012736 aqueous medium Substances 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 239000013081 microcrystal Substances 0.000 description 3
- 229960005489 paracetamol Drugs 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 229920002301 cellulose acetate Polymers 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000013270 controlled release Methods 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 238000009826 distribution Methods 0.000 description 2
- 238000012377 drug delivery Methods 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 238000011068 loading method Methods 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
- 239000012798 spherical particle Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 229920002554 vinyl polymer Polymers 0.000 description 2
- UOTMYNBWXDUBNX-UHFFFAOYSA-N 1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxyisoquinolin-2-ium;chloride Chemical compound Cl.C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 UOTMYNBWXDUBNX-UHFFFAOYSA-N 0.000 description 1
- GJHKWLSRHNWTAN-UHFFFAOYSA-N 1-ethoxy-4-(4-pentylcyclohexyl)benzene Chemical compound C1CC(CCCCC)CCC1C1=CC=C(OCC)C=C1 GJHKWLSRHNWTAN-UHFFFAOYSA-N 0.000 description 1
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical class CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 description 1
- WYUYEJNGHIOFOC-VVTVMFAVSA-N 2-[(z)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridine;hydrochloride Chemical compound Cl.C1=CC(C)=CC=C1C(\C=1N=CC=CC=1)=C\CN1CCCC1 WYUYEJNGHIOFOC-VVTVMFAVSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 229930186147 Cephalosporin Natural products 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Natural products 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 1
- 241000116710 Ferula foetidissima Species 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 1
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 description 1
- 241000282320 Panthera leo Species 0.000 description 1
- CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 description 1
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical compound [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 1
- 238000005903 acid hydrolysis reaction Methods 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 229940057282 albuterol sulfate Drugs 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 229960003556 aminophylline Drugs 0.000 description 1
- FQPFAHBPWDRTLU-UHFFFAOYSA-N aminophylline Chemical compound NCCN.O=C1N(C)C(=O)N(C)C2=C1NC=N2.O=C1N(C)C(=O)N(C)C2=C1NC=N2 FQPFAHBPWDRTLU-UHFFFAOYSA-N 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000012752 auxiliary agent Substances 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229940124587 cephalosporin Drugs 0.000 description 1
- 150000001780 cephalosporins Chemical class 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 229960002155 chlorothiazide Drugs 0.000 description 1
- 229940124579 cold medicine Drugs 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000004020 conductor Substances 0.000 description 1
- 238000013267 controlled drug release Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 235000013367 dietary fats Nutrition 0.000 description 1
- -1 dilthia Zem Chemical compound 0.000 description 1
- MZNZKBJIWPGRID-UHFFFAOYSA-N diphenylphosphorylmethyl(diphenyl)phosphane Chemical compound C=1C=CC=CC=1P(C=1C=CC=CC=1)(=O)CP(C=1C=CC=CC=1)C1=CC=CC=C1 MZNZKBJIWPGRID-UHFFFAOYSA-N 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 235000021463 dry cake Nutrition 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 229960004842 ephedrine sulfate Drugs 0.000 description 1
- 229960003276 erythromycin Drugs 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 230000009969 flowable effect Effects 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 239000004083 gastrointestinal agent Substances 0.000 description 1
- 239000010520 ghee Substances 0.000 description 1
- 239000004519 grease Substances 0.000 description 1
- 239000008240 homogeneous mixture Substances 0.000 description 1
- 229960002003 hydrochlorothiazide Drugs 0.000 description 1
- 229920001477 hydrophilic polymer Polymers 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229960001680 ibuprofen Drugs 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 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 1
- 229960000991 ketoprofen Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- YLGXILFCIXHCMC-JHGZEJCSSA-N methyl cellulose Chemical compound COC1C(OC)C(OC)C(COC)O[C@H]1O[C@H]1C(OC)C(OC)C(OC)OC1COC YLGXILFCIXHCMC-JHGZEJCSSA-N 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- DYKFCLLONBREIL-KVUCHLLUSA-N minocycline Chemical compound C([C@H]1C2)C3=C(N(C)C)C=CC(O)=C3C(=O)C1=C(O)[C@@]1(O)[C@@H]2[C@H](N(C)C)C(O)=C(C(N)=O)C1=O DYKFCLLONBREIL-KVUCHLLUSA-N 0.000 description 1
- 229960004023 minocycline Drugs 0.000 description 1
- VWPOSFSPZNDTMJ-UCWKZMIHSA-N nadolol Chemical compound C1[C@@H](O)[C@@H](O)CC2=C1C=CC=C2OCC(O)CNC(C)(C)C VWPOSFSPZNDTMJ-UCWKZMIHSA-N 0.000 description 1
- 229960004255 nadolol Drugs 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 238000011017 operating method Methods 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 229960003207 papaverine hydrochloride Drugs 0.000 description 1
- 239000013618 particulate matter Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 235000021110 pickles Nutrition 0.000 description 1
- 239000011295 pitch Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 229960003447 pseudoephedrine hydrochloride Drugs 0.000 description 1
- BALXUFOVQVENIU-KXNXZCPBSA-N pseudoephedrine hydrochloride Chemical compound [H+].[Cl-].CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 BALXUFOVQVENIU-KXNXZCPBSA-N 0.000 description 1
- XHKUDCCTVQUHJQ-LCYSNFERSA-N quinidine D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@H]2[C@@H](O)C1=CC=NC2=CC=C(OC)C=C21 XHKUDCCTVQUHJQ-LCYSNFERSA-N 0.000 description 1
- 229960002454 quinidine gluconate Drugs 0.000 description 1
- 229960004482 quinidine sulfate Drugs 0.000 description 1
- 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 1
- 229960000620 ranitidine Drugs 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 238000007790 scraping Methods 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000010902 straw Substances 0.000 description 1
- 230000009967 tasteless effect Effects 0.000 description 1
- 229910052719 titanium Inorganic materials 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- 229960001593 triprolidine hydrochloride Drugs 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J3/00—Processes of treating or compounding macromolecular substances
- C08J3/005—Processes for mixing polymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L1/00—Compositions of cellulose, modified cellulose or cellulose derivatives
- C08L1/02—Cellulose; Modified cellulose
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J2300/00—Characterised by the use of unspecified polymers
- C08J2300/14—Water soluble or water swellable polymers, e.g. aqueous gels
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J2301/00—Characterised by the use of cellulose, modified cellulose or cellulose derivatives
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L1/00—Compositions of cellulose, modified cellulose or cellulose derivatives
- C08L1/08—Cellulose derivatives
- C08L1/26—Cellulose ethers
- C08L1/28—Alkyl ethers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Polymers & Plastics (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Abstract
Description
Claims (20)
- 1.ともに処理される非摩擦微結晶性セルロース及び非イオン性ヒドロコロイド の乾燥した粒状粒子であり、2種の成分の比が99:1−70:30の微結晶性 セルロース:ヒドロコロイドの重量比であり、該成分が互いに緊密に結合してい ることを特徴とするスフェロニゼーションによりスフェロイドを製造するのに有 用な組成物。
- 2.ヒドロコロイドがメチルセルロースであり、2種の成分の重量比が97.5 :2.5−90:10の微結晶性セルロース:ヒドロコロイドの範囲内であるこ とを特徴とする請求項1の組成物。
- 3.ヒドロコロイドがメチルセルロースであり、2種の成分の重量比が96:4 −94:6の微結晶性セルロース:ヒドロコロイドの範囲内であることを特徴と する請求項1の組成物。
- 4.微結晶性セルロース成分の源が湿ったケーキであることを特徴とする請求項 1の組成物。
- 5.ヒドロコロイドがメチルセルロースであることを特徴とする請求項1の組成 物。
- 6.ヒドロコロイド成分がヒドロキシプロピルメチルセルロースであることを特 徴とする請求項1の組成物。
- 7.非イオン性ヒドロコロイドの水溶液中の非摩擦微結晶性セルロースの十分に 分散したスラリーを形成し、微結晶性セルロース及びヒドロコロイドの成分の量 が粒状のともに処理される生成物に関する以下に示される範囲内に成分の比をも たらすようなものであり、そして 水性スラリーを乾燥して非摩擦微結晶性セルロース対ヒドロコロイドの重量比が 99:1−70:30の範囲にある粒状のともに処理される生成物を生ずること を特徴とする、スフェロニゼーションによりスフェロイドを製造するのに有用な 粒状物質を製造する方法。
- 8.水性スラリーが噴霧乾燥により乾燥されることを特徴とする請求項7の方法 。
- 9.微結晶性セルロースが湿ったケーキであることを特徴とする請求項7の方法 。
- 10.噴霧乾燥が230°F−240°F(110℃−115,6℃)の乾燥機 出口温度で行われることを特徴とする請求項8の方法。
- 11.薬剤及び請求項1の組成物のブレンドをスフェロニゼーションにかけるこ とを特徴とする粒状のスフェロニゼーション化固体投与物を製造する方法。
- 12.薬剤及び請求項2の組成物のブレンドをスフェロニゼーションにかけるこ とを特徴とする粒状のスフェロニゼーション化固体投与物を製造する方法。
- 13.薬剤及び請求項3の組成物のブレンドをスフェロニゼーションにかけるこ とを特徴とする粒状のスフェロニゼーション化固体投与物を製造する方法。
- 14.薬剤及び請求項4の組成物のブレンドをスフェロニゼーションにかけるこ とを特徴とする粒状のスフェロニゼーシヨン化固体投与物を製造する方法。
- 15.薬剤及び請求項5の組成物のブレンドをスフェロニゼーションにかけるこ とを特徴とする粒状のスフェロニゼーション化固体投与物を製造する方法。
- 16.薬剤及び請求項6の組成物のブレンドをスフェロニゼーションにかけるこ とを特徴とする粒状のスフェロニゼーション化固体投与物を製造する方法。
- 17.請求項1の組成物並びに製薬上有効な量の少なくとも1種の薬剤を組合せ て含む球を特徴とする固体の投与物。
- 18.請求項2の組成物並びに製薬上有効な量の少なくとも1種の薬剤を組合せ て含む球を特徴とする固体の投与物。
- 19.請求項3の組成物並びに製薬上有効な量の少なくとも1種の薬剤を粗合せ て含む球を特徴とする固体の投与物。
- 20.請求項6の組成物並びに製薬上有効な量の少なくとも1種の薬剤を組合せ て含む球を特徴とする固体の投与物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US81602791A | 1991-12-30 | 1991-12-30 | |
US816.027 | 1991-12-30 |
Publications (2)
Publication Number | Publication Date |
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JPH06511255A true JPH06511255A (ja) | 1994-12-15 |
JP2628230B2 JP2628230B2 (ja) | 1997-07-09 |
Family
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JP5511647A Expired - Fee Related JP2628230B2 (ja) | 1991-12-30 | 1992-11-18 | 微結晶性セルローススフェロニゼーション組成物 |
Country Status (16)
Country | Link |
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US (1) | US5725886A (ja) |
EP (1) | EP0619731B1 (ja) |
JP (1) | JP2628230B2 (ja) |
CN (1) | CN1074228A (ja) |
AT (1) | ATE196733T1 (ja) |
AU (1) | AU663146B2 (ja) |
BR (1) | BR9206996A (ja) |
CA (1) | CA2126441C (ja) |
DE (1) | DE69231499T2 (ja) |
ES (1) | ES2150438T3 (ja) |
FI (1) | FI943121A (ja) |
IL (1) | IL104087A (ja) |
MX (1) | MX9207438A (ja) |
NO (1) | NO942457D0 (ja) |
WO (1) | WO1993012768A1 (ja) |
ZA (1) | ZA929161B (ja) |
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-
1992
- 1992-11-18 WO PCT/US1992/009983 patent/WO1993012768A1/en active IP Right Grant
- 1992-11-18 BR BR9206996A patent/BR9206996A/pt not_active Application Discontinuation
- 1992-11-18 JP JP5511647A patent/JP2628230B2/ja not_active Expired - Fee Related
- 1992-11-18 AT AT93900553T patent/ATE196733T1/de not_active IP Right Cessation
- 1992-11-18 ES ES93900553T patent/ES2150438T3/es not_active Expired - Lifetime
- 1992-11-18 DE DE69231499T patent/DE69231499T2/de not_active Expired - Fee Related
- 1992-11-18 EP EP93900553A patent/EP0619731B1/en not_active Expired - Lifetime
- 1992-11-18 CA CA002126441A patent/CA2126441C/en not_active Expired - Fee Related
- 1992-11-18 AU AU31793/93A patent/AU663146B2/en not_active Ceased
- 1992-11-25 ZA ZA929161A patent/ZA929161B/xx unknown
- 1992-12-14 IL IL10408792A patent/IL104087A/en not_active IP Right Cessation
- 1992-12-18 MX MX9207438A patent/MX9207438A/es unknown
- 1992-12-21 CN CN92115100A patent/CN1074228A/zh active Pending
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1994
- 1994-06-29 FI FI943121A patent/FI943121A/fi not_active Application Discontinuation
- 1994-06-29 NO NO942457A patent/NO942457D0/no unknown
- 1994-09-26 US US08/311,800 patent/US5725886A/en not_active Expired - Lifetime
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2012509329A (ja) * | 2008-11-19 | 2012-04-19 | アバントール パフォーマンス マテリアルズ, インコーポレイテッド | 直接圧縮可能で高機能性な顆粒状の微結晶性セルロースベース賦形剤、それらの製造プロセスおよび使用 |
Also Published As
Publication number | Publication date |
---|---|
CN1074228A (zh) | 1993-07-14 |
ATE196733T1 (de) | 2000-10-15 |
AU663146B2 (en) | 1995-09-28 |
ZA929161B (en) | 1993-05-25 |
EP0619731B1 (en) | 2000-10-04 |
IL104087A (en) | 1998-10-30 |
BR9206996A (pt) | 1995-12-05 |
EP0619731A4 (en) | 1995-05-03 |
EP0619731A1 (en) | 1994-10-19 |
CA2126441A1 (en) | 1993-07-08 |
DE69231499D1 (de) | 2000-11-09 |
NO942457L (no) | 1994-06-29 |
CA2126441C (en) | 1999-12-21 |
FI943121A0 (fi) | 1994-06-29 |
US5725886A (en) | 1998-03-10 |
AU3179393A (en) | 1993-07-28 |
JP2628230B2 (ja) | 1997-07-09 |
ES2150438T3 (es) | 2000-12-01 |
NO942457D0 (no) | 1994-06-29 |
DE69231499T2 (de) | 2001-05-03 |
FI943121A (fi) | 1994-06-29 |
IL104087A0 (en) | 1993-05-13 |
WO1993012768A1 (en) | 1993-07-08 |
MX9207438A (es) | 1993-06-01 |
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