JPH04124126A - Durable capsule - Google Patents
Durable capsuleInfo
- Publication number
- JPH04124126A JPH04124126A JP24148290A JP24148290A JPH04124126A JP H04124126 A JPH04124126 A JP H04124126A JP 24148290 A JP24148290 A JP 24148290A JP 24148290 A JP24148290 A JP 24148290A JP H04124126 A JPH04124126 A JP H04124126A
- Authority
- JP
- Japan
- Prior art keywords
- hydrochloride
- capsule
- weight
- parts
- capsules
- 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.)
- Pending
Links
- 239000002775 capsule Substances 0.000 title claims abstract description 28
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 28
- 239000003814 drug Substances 0.000 claims abstract description 16
- 229940079593 drug Drugs 0.000 claims abstract description 15
- -1 fatty acid ester Chemical class 0.000 claims abstract description 14
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 8
- 239000000194 fatty acid Substances 0.000 claims abstract description 8
- 229930195729 fatty acid Natural products 0.000 claims abstract description 8
- 239000000126 substance Substances 0.000 claims abstract description 8
- 230000001079 digestive effect Effects 0.000 claims abstract description 6
- 235000011389 fruit/vegetable juice Nutrition 0.000 claims abstract description 5
- 229920000642 polymer Polymers 0.000 claims abstract description 5
- 150000001875 compounds Chemical class 0.000 claims abstract description 4
- 150000004665 fatty acids Chemical class 0.000 claims abstract description 4
- 230000005923 long-lasting effect Effects 0.000 claims description 6
- 150000001298 alcohols Chemical class 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 abstract description 7
- 239000007902 hard capsule Substances 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 3
- 239000004094 surface-active agent Substances 0.000 abstract description 2
- 239000003925 fat Substances 0.000 abstract 1
- 239000003921 oil Substances 0.000 abstract 1
- 238000012856 packing Methods 0.000 abstract 1
- 230000008961 swelling Effects 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 17
- 238000000034 method Methods 0.000 description 11
- 239000003607 modifier Substances 0.000 description 7
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 6
- 239000008187 granular material Substances 0.000 description 6
- 239000001856 Ethyl cellulose Substances 0.000 description 5
- 108010010803 Gelatin Proteins 0.000 description 5
- 230000000052 comparative effect Effects 0.000 description 5
- 229920001249 ethyl cellulose Polymers 0.000 description 5
- 235000019325 ethyl cellulose Nutrition 0.000 description 5
- 229920000159 gelatin Polymers 0.000 description 5
- 239000008273 gelatin Substances 0.000 description 5
- 235000019322 gelatine Nutrition 0.000 description 5
- 235000011852 gelatine desserts Nutrition 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- 229920001577 copolymer Polymers 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 3
- 230000002459 sustained effect Effects 0.000 description 3
- AKNNEGZIBPJZJG-MSOLQXFVSA-N (-)-noscapine Chemical compound CN1CCC2=CC=3OCOC=3C(OC)=C2[C@@H]1[C@@H]1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-MSOLQXFVSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- OHXPGWPVLFPUSM-KLRNGDHRSA-N 3,7,12-trioxo-5beta-cholanic acid Chemical compound C1CC(=O)C[C@H]2CC(=O)[C@H]3[C@@H]4CC[C@H]([C@@H](CCC(O)=O)C)[C@@]4(C)C(=O)C[C@@H]3[C@]21C OHXPGWPVLFPUSM-KLRNGDHRSA-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
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 2
- RKWGIWYCVPQPMF-UHFFFAOYSA-N Chloropropamide Chemical compound CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1 RKWGIWYCVPQPMF-UHFFFAOYSA-N 0.000 description 2
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-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
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 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
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-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
- BZKPWHYZMXOIDC-UHFFFAOYSA-N acetazolamide Chemical compound CC(=O)NC1=NN=C(S(N)(=O)=O)S1 BZKPWHYZMXOIDC-UHFFFAOYSA-N 0.000 description 2
- 229960000571 acetazolamide Drugs 0.000 description 2
- CUFNKYGDVFVPHO-UHFFFAOYSA-N azulene Chemical compound C1=CC=CC2=CC=CC2=C1 CUFNKYGDVFVPHO-UHFFFAOYSA-N 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
- 235000019438 castor oil Nutrition 0.000 description 2
- 229940046978 chlorpheniramine maleate Drugs 0.000 description 2
- 229960001761 chlorpropamide Drugs 0.000 description 2
- 229960002997 dehydrocholic acid Drugs 0.000 description 2
- 238000007922 dissolution test Methods 0.000 description 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 2
- CHNXZKVNWQUJIB-CEGNMAFCSA-N ethisterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 CHNXZKVNWQUJIB-CEGNMAFCSA-N 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 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 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
- 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
- 239000004615 ingredient Substances 0.000 description 2
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 229960004708 noscapine Drugs 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 230000002688 persistence Effects 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 239000011118 polyvinyl acetate Substances 0.000 description 2
- 238000007789 sealing Methods 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 229940083542 sodium Drugs 0.000 description 2
- 239000007901 soft capsule Substances 0.000 description 2
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 2
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 description 1
- DNXIKVLOVZVMQF-UHFFFAOYSA-N (3beta,16beta,17alpha,18beta,20alpha)-17-hydroxy-11-methoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]-yohimban-16-carboxylic acid, methyl ester Natural products C1C2CN3CCC(C4=CC=C(OC)C=C4N4)=C4C3CC2C(C(=O)OC)C(O)C1OC(=O)C1=CC(OC)=C(OC)C(OC)=C1 DNXIKVLOVZVMQF-UHFFFAOYSA-N 0.000 description 1
- RUDATBOHQWOJDD-UHFFFAOYSA-N (3beta,5beta,7alpha)-3,7-Dihydroxycholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 RUDATBOHQWOJDD-UHFFFAOYSA-N 0.000 description 1
- YQSHYGCCYVPRDI-UHFFFAOYSA-N (4-propan-2-ylphenyl)methanamine Chemical compound CC(C)C1=CC=C(CN)C=C1 YQSHYGCCYVPRDI-UHFFFAOYSA-N 0.000 description 1
- DKSZLDSPXIWGFO-BLOJGBSASA-N (4r,4ar,7s,7ar,12bs)-9-methoxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-ol;phosphoric acid;hydrate Chemical compound O.OP(O)(O)=O.OP(O)(O)=O.C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC.C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC DKSZLDSPXIWGFO-BLOJGBSASA-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
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- YDDUMTOHNYZQPO-UHFFFAOYSA-N 1,3-bis{[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy}-4,5-dihydroxycyclohexanecarboxylic acid Natural products OC1C(O)CC(C(O)=O)(OC(=O)C=CC=2C=C(O)C(O)=CC=2)CC1OC(=O)C=CC1=CC=C(O)C(O)=C1 YDDUMTOHNYZQPO-UHFFFAOYSA-N 0.000 description 1
- FLNXBVJLPJNOSI-UHFFFAOYSA-N 1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine Chemical compound C1=CC(Cl)=CC=C1C(C=1C=CC=CC=1)OCCN1CCCCC1 FLNXBVJLPJNOSI-UHFFFAOYSA-N 0.000 description 1
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 1
- FRPZMMHWLSIFAZ-UHFFFAOYSA-N 10-undecenoic acid Chemical compound OC(=O)CCCCCCCCC=C FRPZMMHWLSIFAZ-UHFFFAOYSA-N 0.000 description 1
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 description 1
- GCKMFJBGXUYNAG-UHFFFAOYSA-N 17alpha-methyltestosterone Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C)(O)C1(C)CC2 GCKMFJBGXUYNAG-UHFFFAOYSA-N 0.000 description 1
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-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
- 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
- FSSICIQKZGUEAE-UHFFFAOYSA-N 2-[benzyl(pyridin-2-yl)amino]ethyl-dimethylazanium;chloride Chemical compound Cl.C=1C=CC=NC=1N(CCN(C)C)CC1=CC=CC=C1 FSSICIQKZGUEAE-UHFFFAOYSA-N 0.000 description 1
- QCXJFISCRQIYID-IAEPZHFASA-N 2-amino-1-n-[(3s,6s,7r,10s,16s)-3-[(2s)-butan-2-yl]-7,11,14-trimethyl-2,5,9,12,15-pentaoxo-10-propan-2-yl-8-oxa-1,4,11,14-tetrazabicyclo[14.3.0]nonadecan-6-yl]-4,6-dimethyl-3-oxo-9-n-[(3s,6s,7r,10s,16s)-7,11,14-trimethyl-2,5,9,12,15-pentaoxo-3,10-di(propa Chemical compound C[C@H]1OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C(=O)[C@@H]2CCCN2C(=O)[C@H](C(C)C)NC(=O)[C@H]1NC(=O)C1=C(N=C2C(C(=O)N[C@@H]3C(=O)N[C@H](C(N4CCC[C@H]4C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]3C)=O)[C@@H](C)CC)=C(N)C(=O)C(C)=C2O2)C2=C(C)C=C1 QCXJFISCRQIYID-IAEPZHFASA-N 0.000 description 1
- HCMKRGSDKVVWKX-UHFFFAOYSA-N 2-cyclohexyl-2-hydroxybutanoic acid Chemical compound CCC(O)(C(O)=O)C1CCCCC1 HCMKRGSDKVVWKX-UHFFFAOYSA-N 0.000 description 1
- GKNPSSNBBWDAGH-UHFFFAOYSA-N 2-hydroxy-2,2-diphenylacetic acid (1,1-dimethyl-3-piperidin-1-iumyl) ester Chemical compound C1[N+](C)(C)CCCC1OC(=O)C(O)(C=1C=CC=CC=1)C1=CC=CC=C1 GKNPSSNBBWDAGH-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- CDOUZKKFHVEKRI-UHFFFAOYSA-N 3-bromo-n-[(prop-2-enoylamino)methyl]propanamide Chemical compound BrCCC(=O)NCNC(=O)C=C CDOUZKKFHVEKRI-UHFFFAOYSA-N 0.000 description 1
- WTJXVDPDEQKTCV-UHFFFAOYSA-N 4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide;hydron;chloride Chemical compound Cl.C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2C1CC1C(N(C)C)C(=O)C(C(N)=O)=C(O)C1(O)C2=O WTJXVDPDEQKTCV-UHFFFAOYSA-N 0.000 description 1
- PBBGSZCBWVPOOL-HDICACEKSA-N 4-[(1r,2s)-1-ethyl-2-(4-hydroxyphenyl)butyl]phenol Chemical compound C1([C@H](CC)[C@H](CC)C=2C=CC(O)=CC=2)=CC=C(O)C=C1 PBBGSZCBWVPOOL-HDICACEKSA-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
- LZCBNYVJTNCPDR-UHFFFAOYSA-N 4-methoxy-n-[5-(2-methylpropyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide Chemical compound C1=CC(OC)=CC=C1S(=O)(=O)NC1=NN=C(CC(C)C)S1 LZCBNYVJTNCPDR-UHFFFAOYSA-N 0.000 description 1
- PJJGZPJJTHBVMX-UHFFFAOYSA-N 5,7-Dihydroxyisoflavone Chemical compound C=1C(O)=CC(O)=C(C2=O)C=1OC=C2C1=CC=CC=C1 PJJGZPJJTHBVMX-UHFFFAOYSA-N 0.000 description 1
- PUHLHLQBIFRKRD-CSKARUKUSA-N 5-methyl-2-[(E)-2-phenylethenyl]-1,3-benzoxazole Chemical compound N=1C2=CC(C)=CC=C2OC=1\C=C\C1=CC=CC=C1 PUHLHLQBIFRKRD-CSKARUKUSA-N 0.000 description 1
- QMNAQPMXDMLOLD-UHFFFAOYSA-N 6-methyl-4-oxo-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfonamide Chemical compound S1C(C)CC(=O)C2=C1SC(S(N)(=O)=O)=C2 QMNAQPMXDMLOLD-UHFFFAOYSA-N 0.000 description 1
- VCCNKWWXYVWTLT-CYZBKYQRSA-N 7-[(2s,3r,4s,5s,6r)-4,5-dihydroxy-6-(hydroxymethyl)-3-[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-2-yl]oxy-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)chromen-4-one Chemical compound C1=C(O)C(OC)=CC=C1C(OC1=C2)=CC(=O)C1=C(O)C=C2O[C@H]1[C@H](O[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 VCCNKWWXYVWTLT-CYZBKYQRSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
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- 229920002126 Acrylic acid copolymer Polymers 0.000 description 1
- RMMXTBMQSGEXHJ-UHFFFAOYSA-N Aminophenazone Chemical compound O=C1C(N(C)C)=C(C)N(C)N1C1=CC=CC=C1 RMMXTBMQSGEXHJ-UHFFFAOYSA-N 0.000 description 1
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- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 1
- SITQVDJAXQSXSA-CEZRHVESSA-N Cynarin Natural products O[C@@H]1C[C@@](C[C@H](O)[C@H]1OC(=O)C=Cc2ccc(O)c(O)c2)(OC(=O)C=Cc3cccc(O)c3O)C(=O)O SITQVDJAXQSXSA-CEZRHVESSA-N 0.000 description 1
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- PLPRGLOFPNJOTN-UHFFFAOYSA-N narcotine Natural products COc1ccc2C(OC(=O)c2c1OC)C3Cc4c(CN3C)cc5OCOc5c4OC PLPRGLOFPNJOTN-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 235000021313 oleic acid Nutrition 0.000 description 1
- BARWIPMJPCRCTP-UHFFFAOYSA-N oleic acid oleyl ester Natural products CCCCCCCCC=CCCCCCCCCOC(=O)CCCCCCCC=CCCCCCCCC BARWIPMJPCRCTP-UHFFFAOYSA-N 0.000 description 1
- 229940055577 oleyl alcohol Drugs 0.000 description 1
- XMLQWXUVTXCDDL-UHFFFAOYSA-N oleyl alcohol Natural products CCCCCCC=CCCCCCCCCCCO XMLQWXUVTXCDDL-UHFFFAOYSA-N 0.000 description 1
- BARWIPMJPCRCTP-CLFAGFIQSA-N oleyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCCOC(=O)CCCCCCC\C=C/CCCCCCCC BARWIPMJPCRCTP-CLFAGFIQSA-N 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 229960005489 paracetamol Drugs 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 229960001753 phenformin hydrochloride Drugs 0.000 description 1
- MRBDMNSDAVCSSF-UHFFFAOYSA-N phentolamine Chemical compound C1=CC(C)=CC=C1N(C=1C=C(O)C=CC=1)CC1=NCCN1 MRBDMNSDAVCSSF-UHFFFAOYSA-N 0.000 description 1
- 229960001999 phentolamine Drugs 0.000 description 1
- OCYSGIYOVXAGKQ-FVGYRXGTSA-N phenylephrine hydrochloride Chemical compound [H+].[Cl-].CNC[C@H](O)C1=CC=CC(O)=C1 OCYSGIYOVXAGKQ-FVGYRXGTSA-N 0.000 description 1
- 229960003733 phenylephrine hydrochloride Drugs 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229920006122 polyamide resin Polymers 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
- 229960005205 prednisolone Drugs 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[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 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- DBABZHXKTCFAPX-UHFFFAOYSA-N probenecid Chemical compound CCCN(CCC)S(=O)(=O)C1=CC=C(C(O)=O)C=C1 DBABZHXKTCFAPX-UHFFFAOYSA-N 0.000 description 1
- 229960003081 probenecid Drugs 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 229940093625 propylene glycol monostearate Drugs 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 238000003908 quality control method Methods 0.000 description 1
- BJOIZNZVOZKDIG-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C([C]5C=CC(OC)=CC5=N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 BJOIZNZVOZKDIG-MDEJGZGSSA-N 0.000 description 1
- 229960003147 reserpine Drugs 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
- 206010039083 rhinitis Diseases 0.000 description 1
- MDMGHDFNKNZPAU-UHFFFAOYSA-N roserpine Natural products C1C2CN3CCC(C4=CC=C(OC)C=C4N4)=C4C3CC2C(OC(C)=O)C(OC)C1OC(=O)C1=CC(OC)=C(OC)C(OC)=C1 MDMGHDFNKNZPAU-UHFFFAOYSA-N 0.000 description 1
- 229960000581 salicylamide Drugs 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
- 229940079841 sodium copper chlorophyllin Drugs 0.000 description 1
- 235000013758 sodium copper chlorophyllin Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 229940012831 stearyl alcohol Drugs 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 229960004989 tetracycline hydrochloride Drugs 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
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- DZKXJUASMGQEMA-UHFFFAOYSA-N tetradecyl tetradecanoate Chemical compound CCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCC DZKXJUASMGQEMA-UHFFFAOYSA-N 0.000 description 1
- 229960000278 theophylline Drugs 0.000 description 1
- 229960000896 tipepidine Drugs 0.000 description 1
- 229960002649 tolazoline hydrochloride Drugs 0.000 description 1
- 229960005371 tolbutamide Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 description 1
- LMJSLTNSBFUCMU-UHFFFAOYSA-N trichlormethiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NC(C(Cl)Cl)NS2(=O)=O LMJSLTNSBFUCMU-UHFFFAOYSA-N 0.000 description 1
- 229960004813 trichlormethiazide Drugs 0.000 description 1
- FAPSXSAPXXJTOU-UHFFFAOYSA-L trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;dibromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C FAPSXSAPXXJTOU-UHFFFAOYSA-L 0.000 description 1
- 229960001593 triprolidine hydrochloride Drugs 0.000 description 1
- 229960002703 undecylenic acid Drugs 0.000 description 1
- RUDATBOHQWOJDD-UZVSRGJWSA-N ursodeoxycholic acid Chemical compound C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-UZVSRGJWSA-N 0.000 description 1
- 229960001661 ursodiol Drugs 0.000 description 1
- AQTQHPDCURKLKT-JKDPCDLQSA-N vincristine sulfate Chemical compound OS(O)(=O)=O.C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C=O)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 AQTQHPDCURKLKT-JKDPCDLQSA-N 0.000 description 1
- 229960002110 vincristine sulfate Drugs 0.000 description 1
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明は、持続性のカプセル剤に関し、さらに詳しくは
、内層した際に一部の薬剤が速やかに放出され、残った
薬剤が持続的に放出される速効性かつ持続性のカプセル
剤に関する。DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to a long-acting capsule, and more particularly, it is a long-acting capsule that, when filled with an inner layer, releases part of the drug quickly and releases the remaining drug in a sustained manner. The present invention relates to a fast-acting and long-lasting capsule formulation.
従沫１１１４
従来から、薬効を持続的に発揮する製剤方法としては、
以下のものが知られている。Cong. 1114 Traditionally, the formulation methods that achieve sustained medicinal efficacy include:
The following are known:
（１）トローチ、火剤などのように製剤の崩壊性を悪く
する方法。(1) Methods that make the disintegration of the preparation worse, such as troches and gunpowder.
（２）外層は普通の錠剤で糖衣を施し、内層はフィルム
コーティングにより腸溶性にして複効錠とする方法。(2) A method in which the outer layer is an ordinary tablet coated with sugar, and the inner layer is made enteric-coated by film coating to make a double-acting tablet.
（３）崩壊時間の異なる顆粒をカプセル等に充填し、ス
パンスルカプセルとする方法。(3) A method in which granules with different disintegration times are filled into capsules, etc. to make spansle capsules.
（４）崩壊時間の異なる顆粒を錠剤に成形してスパンタ
ブ型とする方法。(4) A method of forming granules with different disintegration times into tablets into a spun tab type.
（５）速放出性の顆粒と徐放８性の顆粒とに分けて、二
層または三層に打錠してスパンタブ型多層錠とする方法
。(5) A method of separating the immediate-release granules and sustained-release granules into two- or three-layer tablets to form span tab-type multilayer tablets.
（６）高分子マトリックスにより薬剤の放出をコントロ
ールした錠剤とする方法。(6) A method of making tablets with controlled drug release using a polymer matrix.
しかしながら従来の持続型内服剤は、持続性の点では改
善されているが。However, conventional long-acting oral preparations have been improved in terms of sustainability.
■ 速効性が十分でない
１＋ 薬剤の崩壊をコントロールする方法であるため
、食事の種類に影響される
・、■ 製造工程が複雑である
などの欠点があった。■ Not fast-acting enough 1+ Since it is a method of controlling the disintegration of the drug, it is affected by the type of meal, and ■ The manufacturing process is complicated.
発明が解決しようとする課
本発明は、薬効の持続性はもちろんのこと、速効性に優
れたカプセル剤を提供するものである。Problems to be Solved by the Invention The present invention provides capsules that are excellent in immediate efficacy as well as long-lasting medicinal efficacy.
月１４１１戊
本発明の持続性カプセル剤は、消化液に不溶ないし難溶
性の物質をエタノールに溶解または膨潤せしめ、内服に
より有効性を発揮する薬物とともに、カプセルに充填し
たことを特徴とする。The long-acting capsule of the present invention is characterized in that a substance that is insoluble or poorly soluble in digestive fluids is dissolved or swollen in ethanol and filled into a capsule along with a drug that is effective when taken orally.
以下、本発明についてさらに詳細に説明する。The present invention will be explained in more detail below.
本発明では放出性調整剤として、消化液に不溶ないし難
溶性の物質が用いられ、この物質はエタノールに溶解ま
たは膨潤し、一般に水に不溶ないし難溶性である。In the present invention, a substance that is insoluble or sparingly soluble in digestive juices is used as the release modifier, and this substance dissolves or swells in ethanol and is generally insoluble or sparingly soluble in water.
放出性調整剤としては、高分子化合物、脂肪酸類、高級
アルコール類、脂肪酸エステル類などが好適に使用され
る。As the release modifier, polymer compounds, fatty acids, higher alcohols, fatty acid esters, etc. are preferably used.
高分子化合物としては、エチルセルロース、酢酸フタル
酸セルロース、ヒドロキシプロピルメチルセルロースフ
タレート、カルボキシメチルエチルセルロース、ポリビ
ニルピロリドン、メチルビニルエーテル／無水マレイン
酸共重合体、メタアクリル酸・アクリル酸エチルコポリ
マー、メタクリル酸・メタアクリル酸メチルコポリマー
、酢酸酸ビニル樹脂、ポリアミド樹脂などがある。Examples of polymer compounds include ethyl cellulose, cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate, carboxymethyl ethyl cellulose, polyvinyl pyrrolidone, methyl vinyl ether/maleic anhydride copolymer, methacrylic acid/ethyl acrylate copolymer, methacrylic acid/methacrylic acid Examples include methyl copolymers, vinyl acetate resins, and polyamide resins.
脂肪酸類としては、ラウリン酸、ミリスチン酸、パルミ
チン酸、ステアリン酸、オレイン酸、ウンデシレン酸、
イソステアリン酸、ロジンなどがある。Fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, undecylenic acid,
These include isostearic acid and rosin.
高級アルコール類としては、セタノール、ステアリルア
ルコール、オレイルアルコール、ラウリルアルコール、
ヘキサデシルアルコール、インステアリルアルコールな
どがある。Higher alcohols include cetanol, stearyl alcohol, oleyl alcohol, lauryl alcohol,
Examples include hexadecyl alcohol and instearyl alcohol.
脂肪酸エステル類としては、ミリスチン酸イソプロピル
、パルミチン酸イソプロピル、ラウリン酸ヘキシル、ミ
リスチン酸ミリスチル、オレイン酸オレイル、オレイン
酸デシル、乳酸ミリスチルなどがある。Examples of fatty acid esters include isopropyl myristate, isopropyl palmitate, hexyl laurate, myristyl myristate, oleyl oleate, decyl oleate, myristyl lactate, and the like.
これら放出性調整剤は、単独で用いても２種以上用いて
もよく、また、配合量は使用する調整剤、配合する薬物
、目的とする持続性の程度等により異なるが、通常エタ
ノール中に１〜７０重量％、好ましくは５〜３０重量％
の量で配合することが望ましい。These release modifiers may be used alone or in two or more types, and the amount of the release modifier varies depending on the modifier used, the drug to be mixed, the desired degree of persistence, etc., but is usually added to ethanol. 1-70% by weight, preferably 5-30% by weight
It is desirable to mix it in an amount of .
さらに本発明では放出をコントロールする目的で、各種
の油脂類、界面活性剤などをエタノールに配合すること
ができる。Furthermore, in the present invention, various oils and fats, surfactants, etc. can be blended with ethanol for the purpose of controlling release.
本発明のカプセル剤中には、内服により各種の疾病を予
防ないしは治療する薬物が配合される。これら薬物を例
示すれば以下の通りである。The capsules of the present invention contain drugs that can be taken internally to prevent or treat various diseases. Examples of these drugs are as follows.
使途等に応して必要量配合される。The required amount is mixed according to the intended use.
（１）解熱鎮痛消炎剤
アセトアミノフェン、ブセチン、サリチルアミド、アミ
ノピリン、フェニルブタシン、メフェナム酸、フルフェ
ナム酸５ジクロフエナツクナトリウム、イブフェナック
、イブプロフェン、インドメタシン、ケトプロフェン、
プロベネシッドなど
（２）自律神経用剤
塩酸ノルフェネフリン、塩酸メタンフェタミン、フェニ
ルプロパツールアミン、塩酸フェキシベンザミン、酒石
酸エルゴタミン、塩酸トラゾリン、硫酸アトロピン、ア
ンプロトロピン、塩酸ジサイクロミン、臭化ブトロピウ
ム、塩酸ピペリドレート、塩酸ベナクチジン、臭化オキ
シピロニウム、塩酸ピメタネート、臭化メペンゾレート
。(1) Antipyretic analgesic anti-inflammatory agent acetaminophen, busetin, salicylamide, aminopyrine, phenylbutacin, mefenamic acid, flufenamic acid 5-diclofenac sodium, ibufenac, ibuprofen, indomethacin, ketoprofen,
Probenecid, etc. (2) Autonomic nerve agents norphenephrine hydrochloride, methamphetamine hydrochloride, phenylpropaturamine, fexibenzamine hydrochloride, ergotamine tartrate, tolazoline hydrochloride, atropine sulfate, amprotropin, dicyclomine hydrochloride, butropium bromide, piperidlate hydrochloride, hydrochloric acid Benactidine, oxypyronium bromide, pimethanate hydrochloride, mepenzolate bromide.
臭化メチルスコポラミン、臭化メチルベナクチジウムな
ど
（３）感覚器管用剤
ジクロツェナミド、アセタゾラミド、メタシラミドなど
（４）抗ヒスタミン剤
塩酸ジフェンヒドラミン、塩酸クロルフ二ツキサミン、
マレイン酸カルビノキサミン、マレイン酸クロルフェニ
ラミン、マレイン酸プロムフェニラミン、塩酸トリペレ
ナミン、塩酸トンジルアミン、塩酸プロメタシン、塩酸
インチベンジル、塩酸トリプロリジン、塩酸クレミゾー
ル、マレイン酸ジメチンデン、タレマスチン、塩酸イソ
プロピルアミノメチルへブタンなど
（５）降圧利尿剤
ヘキサメソニウムプロミド、ベントリニウム、塩化クロ
ルプロパミド、塩酸メカミルアミン、硫酸グアネチジン
、フェントールアミンメタンスルフォネート、塩酸ヒト
ララジン、レセルピン、レシナミン、硫酸ベタニシン、
メブタノート、ペンドロフルチチアジド、トリクロルメ
チアジド、アセタゾラミド、グロフェナミドなど
（６）呼吸促進・鎮咳去痰剤
ジメフリン塩酸塩、リン酸コデイン、リン酸ビヒドロコ
デイン、塩酸エフェドリン、ｄＱ−塩酸メチルエフェド
リン、塩酸ノスカピン、ノスカピン、クエン酸カルへタ
ペンタン、塩酸アクロラマイド、臭化水Ｓ酸デキストロ
メトルファン、ヒベンズ酸チペピジン、オキシメテハノ
ール、クエン酸イソアミル、グアヤコールグリセリンエ
ーテル、クロペラスチン、塩酸エチルシスティン、塩酸
メトキシフェナミン、硫酸イソプロテレノール、塩酸ク
ロルブレナリン、塩酸トリメトキノールなど
（７）消化器管用剤
アズレン、ゲファルナート、カルベノキサロン、塩酸ク
ロルベンゾキサミン、銅クロロフイリンナトリウム、ウ
ルソデオキシコール酸、デヒドロコール酸、デヒドロコ
ール酸ナトリウム、ヒドロキシシクロヘキシル酪酸、フ
ェニルプロパツール、サイナリン、ジオクチルソジウム
スルホサクシネートなど
（８）副腎ホルモン剤
ヒドロコルチゾン、酢酸ヒドロコルチゾン、プレドニゾ
ロン、トリアニシンロン、デキサメタシン、ベタメタシ
ン、フルオコートロンなど
（９）性ホルモン剤
テストステロン、メチルテストステロン。Methylscopolamine bromide, methylbenactidium bromide, etc. (3) Sensory agents diclozenamide, acetazolamide, metasilamide, etc. (4) Antihistamines diphenhydramine hydrochloride, chlorfnituxamine hydrochloride,
Carbinoxamine maleate, chlorpheniramine maleate, prompheniramine maleate, tripelenamine hydrochloride, tonzylamine hydrochloride, promethacin hydrochloride, inchibenzyl hydrochloride, triprolidine hydrochloride, clemizole hydrochloride, dimethindene maleate, talemastine, isopropylaminomethylhebutane hydrochloride, etc. 5) Antihypertensive diuretics hexamethonium bromide, ventolinium, chlorpropamide chloride, mecamylamine hydrochloride, guanethidine sulfate, fentolamine methanesulfonate, hydralazine hydrochloride, reserpine, recinamine, betanisin sulfate,
Mebutanot, pendroflutithiazide, trichlormethiazide, acetazolamide, glofenamide, etc. (6) Respiratory promoting/antitussive expectorant Dimefrine hydrochloride, codeine phosphate, bihydrocodeine phosphate, ephedrine hydrochloride, dQ-methylephedrine hydrochloride, noscapine hydrochloride, Noscapine, carhetapentane citrate, acrolamide hydrochloride, dextromethorphan hydrobromide, tipepidine hibenzate, oxymethehanol, isoamyl citrate, guaiacol glycerin ether, cloperastine, ethyl cysteine hydrochloride, methoxyphenamine hydrochloride, isoprotere sulfate (7) Gastrointestinal agents azulene, gefarnate, carbenoxalone, chlorbenzoxamine hydrochloride, sodium copper chlorophyllin, ursodeoxycholic acid, dehydrocholic acid, sodium dehydrocholic acid, Hydroxycyclohexylbutyric acid, phenylpropatur, Cynarin, dioctyl sodium sulfosuccinate, etc. (8) Adrenal hormones hydrocortisone, hydrocortisone acetate, prednisolone, trianisinlone, dexamethacin, betamethacin, fluocortorone, etc. (9) Sex hormones testosterone, Methyltestosterone.
フルオキシメステロン、フォスフニストロール、エスト
ロン、エチニルエストラジオール、ヘキセストロール、
エチステロンなと
（１０）糖尿病治療剤
スルフオブタミド、トルブタミド、クロルプロパミド、
アセトヘキサミド、メラザミド、グリクロピラミド、イ
ソブゾール、グリベンクラミド、グリミジンナトリウム
、グリブゾール、塩酸フェンフォルミン、メトフォルミ
ン、塩酸ブフオルミンなど
（１１）抗悪性腫瘍剤
ティトロジエンマスタード−Ｎ−オキシド、シクロフォ
スフアミド、カルボコン、インブロクオン、チオテバ、
フトラフール。fluoxymesterone, fosfunistrol, estrone, ethinylestradiol, hexestrol,
Ethisterone (10) Antidiabetic agents sulfobutamide, tolbutamide, chlorpropamide,
Acetohexamide, melazamide, glyclopyramide, isobuzole, glibenclamide, glymidine sodium, glybuzol, phenformin hydrochloride, metformin, buformin hydrochloride, etc. (11) Anti-cancer agents Titrodiene mustard-N-oxide, cyclophosphamide , carbocon, imbroquone, thioteva,
Futrafur.
６−メルカプトプリン、硫酸ビングラスチン、硫酸ビン
クリスチン、アクチノマイシンＣ，マイトマイシンＣな
ど
（１２）抗生物質
ペニシリン、タロキサシリンナトリウム。6-mercaptopurine, vingrastine sulfate, vincristine sulfate, actinomycin C, mitomycin C, etc. (12) Antibiotics penicillin, taroxacillin sodium.
ジクロキサシリンナトリウム、セファレキシン、エリス
ロマイシン、キタサマイシン。Dicloxacillin sodium, cephalexin, erythromycin, kitasamycin.
ジョサマイシン、クロラムフェニコール、テトラサイク
リン、塩酸テトラサイクリン、塩酸ミノサイクリンなど
本発明では、放出性調整剤をエタノールに溶解または膨
潤せしめ、薬物とともにカプセルに充填して使用される
。カプセルとしては、エタノールに対して不溶性であれ
ば硬カプセル、軟カプセルのいずれでもよい。ただし、
硬カプセルを使用する際は、カプセル本体とキャップを
シールするなどして、液もれを防止する処置を施して製
造される。In the present invention, release modifiers such as josamycin, chloramphenicol, tetracycline, tetracycline hydrochloride, minocycline hydrochloride, etc. are dissolved or swollen in ethanol and used by being filled into capsules with the drug. The capsule may be either a hard capsule or a soft capsule as long as it is insoluble in ethanol. however,
When hard capsules are used, they are manufactured by sealing the capsule body and cap to prevent fluid leakage.
本発明のカプセル剤では、内服後にカプセルの崩壊によ
り内容物が放出され、薬物の一部は速やかに吸収されて
必要な速効性を示す。また、一部の薬物は消化器系にお
ける消化液や水に不溶化ないし電溶化した放出性調整剤
に被覆され、その後論々に放出、吸収されて持続性を示
すと考えられる。In the capsule of the present invention, the contents are released by disintegration of the capsule after internal administration, and a portion of the drug is quickly absorbed to exhibit the necessary rapid efficacy. Further, it is thought that some drugs are coated with a release modifier that is insolubilized or electrosolubilized in digestive juices or water in the digestive system, and are then spontaneously released and absorbed to exhibit persistence.
発明の効果
本発明のカプセル剤によれば、カプセルが崩壊するとと
もに、一部の薬物が一部に放出され、残りが持続的に放
出されるため、速効性と持続性の２つの目的が１つのカ
プセル剤で一挙に達成される。Effects of the Invention According to the capsule of the present invention, when the capsule disintegrates, part of the drug is released into a portion and the rest is released continuously, so that the two objectives of quick-acting and long-lasting effects are achieved. Achieved all at once with one capsule.
また、本発明によれば、従来製剤の如き崩壊遅延による
持続性とは異なるため、持続性に対する食事の影響が少
なく、常に安定した持続効果が得られる。Further, according to the present invention, since the sustainability is different from that due to delayed disintegration as in conventional preparations, there is little influence of food on sustainability, and a stable sustained effect can always be obtained.
さらに本発明によれば、液剤またはペーストをカプセル
に充填するだけで製造できるため、製造工程が簡単で品
質管理が容易である。Furthermore, according to the present invention, the capsule can be manufactured by simply filling the capsule with a liquid or paste, so the manufacturing process is simple and quality control is easy.
実験例１
下記に示す処方の本発明品と、スパンスル型持続性カプ
セル剤である比較品を製造し、モデル薬物である塩酸フ
ェニルプロパツールアミンの溶出率を測定した。Experimental Example 1 A product of the present invention having the formulation shown below and a comparative product in the form of spanned long-lasting capsules were manufactured, and the dissolution rate of phenylpropaturamine hydrochloride, a model drug, was measured.
（１）本発明品の調製
塩酸フェニルプロパツールアミン ５．０重量部エチル
セルロース（１００ｃｐ） １０．０重量部エ
チルセルロース（１０ｃｐ） ３．０重量部
ヒマシ油 ８．０重量部エタノ
ール ７０６０重量部精製水
４．０重量部上記成分を溶解混
合したものを、ゼラチンハードカプセル（１号）に充填
し、シール加工を施して本発明品を得た。(1) Preparation of the product of the present invention Phenylpropaturamine hydrochloride 5.0 parts by weight Ethyl cellulose (100 cp) 10.0 parts by weight Ethyl cellulose (10 cp) 3.0 parts by weight Castor oil 8.0 parts by weight Ethanol 7060 parts by weight Purified water
A solution of 4.0 parts by weight of the above components was filled into gelatin hard capsules (No. 1) and sealed to obtain a product of the present invention.
（２）比較品の調製
塩酸フェニルプロパツールアミン
グラニユー糖
コーンスターチ
ヒドロキシプロピルセルロース
ポリ酢酸ビニル
５．０重量部
４０．０重量部
４０．０重量部
１０．０重量部
５．０重量部
遠心流動造粒機により球形造粒した顆粒に、ヒドロキシ
エチルセルロースおよびポリ酢酸ビニルをコーティング
した顆粒を。(2) Preparation of comparative product Phenylpropaturamine hydrochloride Granulated sugar Corn starch Hydroxypropyl cellulose Polyvinyl acetate 5.0 parts by weight 40.0 parts by weight 40.0 parts by weight 10.0 parts by weight 5.0 parts by weight Centrifugal fluid production Granules are made into spherical granules using a granulator and coated with hydroxyethyl cellulose and polyvinyl acetate.
ゼラチンハートカプセル（１号）に充填し、比較品を得
た。A comparative product was obtained by filling gelatin heart capsules (No. 1).
（３）測定結果
日本薬局方記載の「一般試験法、溶出試験法、第一法」
に従って溶出試験をした結果、第１図に示したように、
比較品では実験開始６０分で約２０％の放出を示し、そ
の後一定の速度で放出されたのに対し、本発明品では開
始２０分後に約４０％の放出を示し、その後、一定の速
度で放出された。(3) Measurement results "General test method, dissolution test method, method 1" described in the Japanese Pharmacopoeia
As a result of the dissolution test according to the following, as shown in Figure 1,
The comparative product showed about 20% release 60 minutes after the start of the experiment and then released at a constant rate, whereas the inventive product showed about 40% release 20 minutes after the start of the experiment and then released at a constant rate. released.
この結果から、本発明品は持続性に加えて、速効性も期
待できることが示された。This result showed that the product of the present invention can be expected to have immediate effect in addition to sustainability.
（以下余白）
実施例１
塩酸フェニルプロパツールアミン ５．０重を部マ
レイン酸クロルフェニラミン ０．５重量部塩
酸フェニレフリン ０．５重量部無水
カフェイン ５．０重量部エチル
セルロース １０．０重量部ヒマシ
油 ５．０重量部エタノー
ル ６０．０重量部上記成
分を溶解混合し、常法によりゼラチンソフトカプセルに
充填し、本発明品を得る。本市は持続性の鼻炎薬として
用いられる。(Leaving space below) Example 1 Phenylpropaturamine hydrochloride 5.0 parts by weight Chlorpheniramine maleate 0.5 parts by weight Phenylephrine hydrochloride 0.5 parts by weight Anhydrous caffeine 5.0 parts by weight Ethyl cellulose 10.0 parts by weight Castor Oil: 5.0 parts by weight Ethanol: 60.0 parts by weight The above components are dissolved and mixed and filled into gelatin soft capsules by a conventional method to obtain the product of the present invention. Motoichi is used as a persistent rhinitis medicine.
実施例２
臭化水素酸デキストロメトロファン １．０重量部メ
タアクリル酸・アクリル酸コポリマー１５．０重量部オ
リーブ油 ５．０重量部ス
テアリン酸モノグリセリン ５．０重量部エ
タノール ６４．０重量部
精製水 １０．０重量部
上記成分を溶解混合し、ゼラチンハードヵプセルに充填
後、シール加工を施し、本発明品を得る。本塁は持続性
の鎮咳薬として使用される実施例３
テオフィリン １０．０重量部
モノステアリン酸プロピレングリコール４０，０重量部
グリセリン ５．０重量部エ
タノール ４５．０重量部上
記成分を溶解混合し、常法によりゼラチンハードカプセ
ルに充填後、シール加工を施し、本発明品を得る。本発
明品は持続性の気管支抗張剤として使用される。Example 2 Dextrometrophane hydrobromide 1.0 parts by weight Methacrylic acid/acrylic acid copolymer 15.0 parts by weight Olive oil 5.0 parts by weight Monoglyceryl stearate 5.0 parts by weight Ethanol 64.0 parts by weight Purification Water: 10.0 parts by weight The above ingredients are dissolved and mixed, filled into gelatin hard capsules, and then sealed to obtain the product of the present invention. Example 3 Theophylline 10.0 parts by weight Propylene glycol monostearate 40.0 parts by weight Glycerin 5.0 parts by weight Ethanol 45.0 parts by weight The above ingredients were dissolved and mixed, and the After filling gelatin hard capsules by the method, sealing is performed to obtain the product of the present invention. The product of the present invention is used as a long-acting bronchial tensile agent.
第１図は、本発明品および比較品について服用後の時開
と、塩酸フェニルプロパツールアミンの溶出率との関係
を示すグラフである。FIG. 1 is a graph showing the relationship between the time release after administration and the elution rate of phenylpropaturamine hydrochloride for the products of the present invention and comparative products.
Claims (1)
解または膨潤せしめ、内服により有効性を発揮する薬物
とともに、カプセルに充填したことを特徴とする持続性
カプセル剤。 ２、上記消化液に不溶ないし難溶性の物質が、高分子化
合物、脂肪酸類、高級アルコール類および脂肪酸エステ
ル類から選ばれる１種または２種以上の物質である請求
項１記載の持続性カプセル剤。[Scope of Claims] 1. A long-lasting capsule, characterized in that a substance that is insoluble or poorly soluble in digestive juices is dissolved or swollen in ethanol and filled into a capsule along with a drug that is effective when taken orally. 2. The long-lasting capsule according to claim 1, wherein the substance insoluble or sparingly soluble in digestive juices is one or more substances selected from polymer compounds, fatty acids, higher alcohols, and fatty acid esters. .
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP24148290A JPH04124126A (en) | 1990-09-12 | 1990-09-12 | Durable capsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP24148290A JPH04124126A (en) | 1990-09-12 | 1990-09-12 | Durable capsule |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04124126A true JPH04124126A (en) | 1992-04-24 |
Family
ID=17074972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP24148290A Pending JPH04124126A (en) | 1990-09-12 | 1990-09-12 | Durable capsule |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH04124126A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008534591A (en) * | 2005-03-29 | 2008-08-28 | マクニール−ピーピーシー・インコーポレーテツド | Composition having a hydrophilic drug in a hydrophobic solvent |
| US8931508B2 (en) | 2008-08-26 | 2015-01-13 | Eaton Corporation | Piloted fuel tank vapor isolation valve |
-
1990
- 1990-09-12 JP JP24148290A patent/JPH04124126A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008534591A (en) * | 2005-03-29 | 2008-08-28 | マクニール−ピーピーシー・インコーポレーテツド | Composition having a hydrophilic drug in a hydrophobic solvent |
| US8931508B2 (en) | 2008-08-26 | 2015-01-13 | Eaton Corporation | Piloted fuel tank vapor isolation valve |
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