JPS5877811A - 安定な易吸収性ニフエジピン製剤の製法 - Google Patents
安定な易吸収性ニフエジピン製剤の製法Info
- Publication number
- JPS5877811A JPS5877811A JP17732381A JP17732381A JPS5877811A JP S5877811 A JPS5877811 A JP S5877811A JP 17732381 A JP17732381 A JP 17732381A JP 17732381 A JP17732381 A JP 17732381A JP S5877811 A JPS5877811 A JP S5877811A
- Authority
- JP
- Japan
- Prior art keywords
- nifedipine
- solution
- coating
- water
- nianidipine
- 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
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 title claims abstract description 19
- 229960001597 nifedipine Drugs 0.000 title claims abstract description 19
- 239000000825 pharmaceutical preparation Substances 0.000 title abstract 4
- 238000002360 preparation method Methods 0.000 title description 9
- 238000000576 coating method Methods 0.000 claims abstract description 27
- 239000011248 coating agent Substances 0.000 claims abstract description 24
- 239000010419 fine particle Substances 0.000 claims abstract description 14
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 11
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 11
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims abstract description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229920000609 methyl cellulose Polymers 0.000 claims abstract description 6
- 239000001923 methylcellulose Substances 0.000 claims abstract description 6
- 235000010981 methylcellulose Nutrition 0.000 claims abstract description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims abstract 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound 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 abstract 3
- 238000000034 method Methods 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 11
- 238000005520 cutting process Methods 0.000 claims description 6
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims 1
- -1 hydroxypropyl Chemical group 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 abstract description 31
- 239000006104 solid solution Substances 0.000 abstract description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 11
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 abstract description 5
- 239000008101 lactose Substances 0.000 abstract description 5
- 238000010521 absorption reaction Methods 0.000 abstract description 4
- 238000005507 spraying Methods 0.000 abstract description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 abstract description 2
- 108010010803 Gelatin Proteins 0.000 abstract description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 abstract description 2
- 229930006000 Sucrose Natural products 0.000 abstract description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 abstract description 2
- 229920000159 gelatin Polymers 0.000 abstract description 2
- 239000008273 gelatin Substances 0.000 abstract description 2
- 235000019322 gelatine Nutrition 0.000 abstract description 2
- 235000011852 gelatine desserts Nutrition 0.000 abstract description 2
- 239000008103 glucose Substances 0.000 abstract description 2
- 239000007864 aqueous solution Substances 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 239000012046 mixed solvent Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 description 20
- 238000004090 dissolution Methods 0.000 description 14
- 230000000052 comparative effect Effects 0.000 description 12
- 238000009472 formulation Methods 0.000 description 9
- 238000005469 granulation Methods 0.000 description 8
- 238000003754 machining Methods 0.000 description 8
- 239000000843 powder Substances 0.000 description 8
- 238000003860 storage Methods 0.000 description 7
- 230000003179 granulation Effects 0.000 description 6
- 239000008187 granular material Substances 0.000 description 4
- 239000003960 organic solvent Substances 0.000 description 4
- 206010002383 Angina Pectoris Diseases 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 3
- 239000001913 cellulose Substances 0.000 description 3
- 238000007922 dissolution test Methods 0.000 description 3
- 238000010828 elution Methods 0.000 description 3
- 230000000474 nursing effect Effects 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 108010076876 Keratins Proteins 0.000 description 2
- 102000011782 Keratins Human genes 0.000 description 2
- 238000011888 autopsy Methods 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- FHHZOYXKOICLGH-UHFFFAOYSA-N dichloromethane;ethanol Chemical compound CCO.ClCCl FHHZOYXKOICLGH-UHFFFAOYSA-N 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000003801 milling Methods 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 239000002023 wood Substances 0.000 description 2
- XINQFOMFQFGGCQ-UHFFFAOYSA-L (2-dodecoxy-2-oxoethyl)-[6-[(2-dodecoxy-2-oxoethyl)-dimethylazaniumyl]hexyl]-dimethylazanium;dichloride Chemical compound [Cl-].[Cl-].CCCCCCCCCCCCOC(=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC(=O)OCCCCCCCCCCCC XINQFOMFQFGGCQ-UHFFFAOYSA-L 0.000 description 1
- 241000252073 Anguilliformes Species 0.000 description 1
- 229910001369 Brass Inorganic materials 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 101100450591 Human adenovirus B serotype 3 PVIII gene Proteins 0.000 description 1
- 206010025476 Malabsorption Diseases 0.000 description 1
- 208000004155 Malabsorption Syndromes Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- ULUAUXLGCMPNKK-UHFFFAOYSA-N Sulfobutanedioic acid Chemical compound OC(=O)CC(C(O)=O)S(O)(=O)=O ULUAUXLGCMPNKK-UHFFFAOYSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 150000008051 alkyl sulfates Chemical class 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000010951 brass Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000002224 dissection Methods 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 238000004898 kneading Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 238000005096 rolling process Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000000304 vasodilatating effect Effects 0.000 description 1
- 230000037303 wrinkles Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP17732381A JPS5877811A (ja) | 1981-11-04 | 1981-11-04 | 安定な易吸収性ニフエジピン製剤の製法 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP17732381A JPS5877811A (ja) | 1981-11-04 | 1981-11-04 | 安定な易吸収性ニフエジピン製剤の製法 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS5877811A true JPS5877811A (ja) | 1983-05-11 |
JPH0328404B2 JPH0328404B2 (enrdf_load_stackoverflow) | 1991-04-19 |
Family
ID=16028964
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP17732381A Granted JPS5877811A (ja) | 1981-11-04 | 1981-11-04 | 安定な易吸収性ニフエジピン製剤の製法 |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS5877811A (enrdf_load_stackoverflow) |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2550444A1 (fr) * | 1983-08-11 | 1985-02-15 | Fujisawa Pharmaceutical Co | Preparation solide capable de liberer rapidement la dihydropyridine a, et son procede d'obtention |
US4562069A (en) * | 1983-05-21 | 1985-12-31 | Bayer Aktiengesellschaft | Two-phase formulation |
US4840799A (en) * | 1986-02-14 | 1989-06-20 | Lejus Medical Aktiebolag | Process for preparing rapidly disintegrating granulates |
JP2002138034A (ja) * | 2000-10-27 | 2002-05-14 | Kyoto Pharmaceutical Industries Ltd | 苦味マスキングチュアブル錠およびその製造方法 |
US6444649B1 (en) | 1998-04-10 | 2002-09-03 | Mitsubishi Chemical Corporation | Solid dispersion containing sialic acid derivative |
US6872336B2 (en) | 2001-09-05 | 2005-03-29 | Shin-Etsu Chemical Co., Ltd. | Process for producing a pharmaceutical solid preparation containing a poorly soluble drug |
JP2018158893A (ja) * | 2017-03-22 | 2018-10-11 | ニプロ株式会社 | トルバプタン製剤およびその製造方法 |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1669345A4 (en) | 2003-08-29 | 2008-02-20 | Japan Tobacco Inc | ESTER DERIVATIVE AND MEDICAL USE THEREOF |
CN105832678A (zh) | 2009-05-27 | 2016-08-10 | 株式会社三养生物制药 | 生物利用度提高的包含难溶性药物的微球及其制备方法 |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS542316A (en) * | 1977-06-07 | 1979-01-09 | Yamanouchi Pharmaceut Co Ltd | Solid pharmaceutical composition containing nifedipene |
-
1981
- 1981-11-04 JP JP17732381A patent/JPS5877811A/ja active Granted
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS542316A (en) * | 1977-06-07 | 1979-01-09 | Yamanouchi Pharmaceut Co Ltd | Solid pharmaceutical composition containing nifedipene |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4562069A (en) * | 1983-05-21 | 1985-12-31 | Bayer Aktiengesellschaft | Two-phase formulation |
FR2550444A1 (fr) * | 1983-08-11 | 1985-02-15 | Fujisawa Pharmaceutical Co | Preparation solide capable de liberer rapidement la dihydropyridine a, et son procede d'obtention |
US4654206A (en) * | 1983-08-11 | 1987-03-31 | Fujisawa Pharmaceutical Co., Ltd. | Fast release solid preparation of dihydropyridine a compound |
AT382779B (de) * | 1983-08-11 | 1987-04-10 | Fujisawa Pharmaceutical Co | Verfahren zur herstellung von festen pharmazeutischen dispersionszusammensetzungen mit rascher wirkstofffreisetzung |
US4840799A (en) * | 1986-02-14 | 1989-06-20 | Lejus Medical Aktiebolag | Process for preparing rapidly disintegrating granulates |
US6444649B1 (en) | 1998-04-10 | 2002-09-03 | Mitsubishi Chemical Corporation | Solid dispersion containing sialic acid derivative |
JP2002138034A (ja) * | 2000-10-27 | 2002-05-14 | Kyoto Pharmaceutical Industries Ltd | 苦味マスキングチュアブル錠およびその製造方法 |
US6872336B2 (en) | 2001-09-05 | 2005-03-29 | Shin-Etsu Chemical Co., Ltd. | Process for producing a pharmaceutical solid preparation containing a poorly soluble drug |
JP2018158893A (ja) * | 2017-03-22 | 2018-10-11 | ニプロ株式会社 | トルバプタン製剤およびその製造方法 |
Also Published As
Publication number | Publication date |
---|---|
JPH0328404B2 (enrdf_load_stackoverflow) | 1991-04-19 |
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