JPS59101422A - 溶出性の優れたニフエジピン固形製剤 - Google Patents
溶出性の優れたニフエジピン固形製剤Info
- Publication number
- JPS59101422A JPS59101422A JP21061882A JP21061882A JPS59101422A JP S59101422 A JPS59101422 A JP S59101422A JP 21061882 A JP21061882 A JP 21061882A JP 21061882 A JP21061882 A JP 21061882A JP S59101422 A JPS59101422 A JP S59101422A
- Authority
- JP
- Japan
- Prior art keywords
- nifedipine
- dissolution
- hydroxypropyl cellulose
- pharmaceutical preparation
- improved dissolution
- 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 37
- 229960001597 nifedipine Drugs 0.000 title claims abstract description 37
- 239000007787 solid Substances 0.000 title claims description 11
- 238000004090 dissolution Methods 0.000 title abstract description 29
- 239000000825 pharmaceutical preparation Substances 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 claims abstract description 19
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 18
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 18
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 18
- 239000000843 powder Substances 0.000 claims description 16
- 238000002360 preparation method Methods 0.000 claims description 9
- 238000010298 pulverizing process Methods 0.000 claims description 8
- 239000000126 substance Substances 0.000 abstract description 4
- 238000002156 mixing Methods 0.000 abstract description 3
- 206010002383 Angina Pectoris Diseases 0.000 abstract description 2
- 206010020772 Hypertension Diseases 0.000 abstract description 2
- RMZQSAMHIQBMLW-UHFFFAOYSA-N 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid Chemical compound OC(=O)C1=C(C)NC(C)=C(C(O)=O)C1C1=CC=CC=C1[N+]([O-])=O RMZQSAMHIQBMLW-UHFFFAOYSA-N 0.000 abstract 1
- 238000004321 preservation Methods 0.000 abstract 1
- 239000000047 product Substances 0.000 description 20
- 238000000034 method Methods 0.000 description 18
- 238000007922 dissolution test Methods 0.000 description 13
- 239000002775 capsule Substances 0.000 description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 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 description 7
- 239000008101 lactose Substances 0.000 description 7
- 238000010828 elution Methods 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- 238000000227 grinding Methods 0.000 description 5
- 239000000546 pharmaceutical excipient Substances 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 4
- 238000010586 diagram Methods 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 230000036470 plasma concentration Effects 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 241000283973 Oryctolagus cuniculus Species 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 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 description 3
- 229930006000 Sucrose Natural products 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000007902 hard capsule Substances 0.000 description 3
- 239000005720 sucrose Substances 0.000 description 3
- 230000007704 transition Effects 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 2
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000011049 filling Methods 0.000 description 2
- 229920001592 potato starch Polymers 0.000 description 2
- 239000012085 test solution Substances 0.000 description 2
- 229940124549 vasodilator Drugs 0.000 description 2
- 239000003071 vasodilator agent Substances 0.000 description 2
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 241000283977 Oryctolagus Species 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920002675 Polyoxyl Polymers 0.000 description 1
- 235000009754 Vitis X bourquina Nutrition 0.000 description 1
- 235000012333 Vitis X labruscana Nutrition 0.000 description 1
- 240000006365 Vitis vinifera Species 0.000 description 1
- 235000014787 Vitis vinifera Nutrition 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000003999 initiator Substances 0.000 description 1
- 229910052742 iron Inorganic materials 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- OJURWUUOVGOHJZ-UHFFFAOYSA-N methyl 2-[(2-acetyloxyphenyl)methyl-[2-[(2-acetyloxyphenyl)methyl-(2-methoxy-2-oxoethyl)amino]ethyl]amino]acetate Chemical compound C=1C=CC=C(OC(C)=O)C=1CN(CC(=O)OC)CCN(CC(=O)OC)CC1=CC=CC=C1OC(C)=O OJURWUUOVGOHJZ-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21061882A JPS59101422A (ja) | 1982-12-02 | 1982-12-02 | 溶出性の優れたニフエジピン固形製剤 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21061882A JPS59101422A (ja) | 1982-12-02 | 1982-12-02 | 溶出性の優れたニフエジピン固形製剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS59101422A true JPS59101422A (ja) | 1984-06-12 |
| JPH0141125B2 JPH0141125B2 (enrdf_load_stackoverflow) | 1989-09-04 |
Family
ID=16592304
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP21061882A Granted JPS59101422A (ja) | 1982-12-02 | 1982-12-02 | 溶出性の優れたニフエジピン固形製剤 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS59101422A (enrdf_load_stackoverflow) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2559064A1 (fr) * | 1984-02-08 | 1985-08-09 | Erba Farmitalia | Composition pharmaceutique a biodisponibilite elevee et procede pour la preparer |
| JPH0215026A (ja) * | 1988-07-01 | 1990-01-18 | Takada Seiyaku Kk | 新規なプロブコール固形製剤 |
| JPH0215027A (ja) * | 1988-07-01 | 1990-01-18 | Takada Seiyaku Kk | 新規なプロブコール固形製剤 |
| JP2001509518A (ja) * | 1997-07-09 | 2001-07-24 | エラン ファーマシューティカル テクノロジーズ | セルロース系表面安定剤を用いたヒト免疫不全ウイルス（ｈｉｖ）プロテアーゼ阻害剤のナノ結晶製剤及びそのような製剤の製造方法 |
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 |
-
1982
- 1982-12-02 JP JP21061882A patent/JPS59101422A/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 (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2559064A1 (fr) * | 1984-02-08 | 1985-08-09 | Erba Farmitalia | Composition pharmaceutique a biodisponibilite elevee et procede pour la preparer |
| JPH0215026A (ja) * | 1988-07-01 | 1990-01-18 | Takada Seiyaku Kk | 新規なプロブコール固形製剤 |
| JPH0215027A (ja) * | 1988-07-01 | 1990-01-18 | Takada Seiyaku Kk | 新規なプロブコール固形製剤 |
| JP2001509518A (ja) * | 1997-07-09 | 2001-07-24 | エラン ファーマシューティカル テクノロジーズ | セルロース系表面安定剤を用いたヒト免疫不全ウイルス（ｈｉｖ）プロテアーゼ阻害剤のナノ結晶製剤及びそのような製剤の製造方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0141125B2 (enrdf_load_stackoverflow) | 1989-09-04 |
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