JPH031288B2 - - Google Patents
Info
- Publication number
- JPH031288B2 JPH031288B2 JP55160952A JP16095280A JPH031288B2 JP H031288 B2 JPH031288 B2 JP H031288B2 JP 55160952 A JP55160952 A JP 55160952A JP 16095280 A JP16095280 A JP 16095280A JP H031288 B2 JPH031288 B2 JP H031288B2
- Authority
- JP
- Japan
- Prior art keywords
- nifedipine
- parts
- fine
- comparative example
- formulation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 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 claims description 71
- 229960001597 nifedipine Drugs 0.000 claims description 69
- 239000010419 fine particle Substances 0.000 claims description 25
- 238000002360 preparation method Methods 0.000 claims description 25
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 23
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 23
- 239000006104 solid solution Substances 0.000 claims description 21
- 239000000243 solution Substances 0.000 claims description 19
- 239000008187 granular material Substances 0.000 claims description 11
- 239000003960 organic solvent Substances 0.000 claims description 9
- 238000001035 drying Methods 0.000 claims description 8
- 239000004503 fine granule Substances 0.000 claims 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 claims description 7
- 239000008101 lactose Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- 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 claims description 6
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 3
- 239000003232 water-soluble binding agent Substances 0.000 claims 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 claims 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 claims 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 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims 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 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 description 31
- 238000009472 formulation Methods 0.000 description 29
- 230000000052 comparative effect Effects 0.000 description 28
- 238000005469 granulation Methods 0.000 description 21
- 230000003179 granulation Effects 0.000 description 21
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 15
- 238000000034 method Methods 0.000 description 13
- 239000002245 particle Substances 0.000 description 13
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 12
- 238000009826 distribution Methods 0.000 description 12
- 239000000047 product Substances 0.000 description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 12
- 238000000576 coating method Methods 0.000 description 11
- 239000008280 blood Substances 0.000 description 10
- 210000004369 blood Anatomy 0.000 description 10
- 238000007796 conventional method Methods 0.000 description 10
- 238000004090 dissolution Methods 0.000 description 10
- 239000011248 coating agent Substances 0.000 description 9
- 229940079593 drug Drugs 0.000 description 8
- 239000003814 drug Substances 0.000 description 8
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- 238000010521 absorption reaction Methods 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 239000007921 spray Substances 0.000 description 5
- 239000013078 crystal Substances 0.000 description 4
- 238000007922 dissolution test Methods 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 238000010828 elution Methods 0.000 description 4
- 238000001125 extrusion Methods 0.000 description 4
- 239000012530 fluid Substances 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 238000004898 kneading Methods 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 206010002383 Angina Pectoris Diseases 0.000 description 2
- 241000282472 Canis lupus familiaris Species 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 239000002244 precipitate Substances 0.000 description 2
- 238000010298 pulverizing process Methods 0.000 description 2
- 238000005096 rolling process Methods 0.000 description 2
- 238000004513 sizing Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 238000005507 spraying Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 1
- 206010025476 Malabsorption Diseases 0.000 description 1
- 208000004155 Malabsorption Syndromes Diseases 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 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
- -1 alkyl sulfate ester Chemical class 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 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 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP16095280A JPS5785316A (en) | 1980-11-14 | 1980-11-14 | Preparation of easily absorbable nifedipine preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP16095280A JPS5785316A (en) | 1980-11-14 | 1980-11-14 | Preparation of easily absorbable nifedipine preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5785316A JPS5785316A (en) | 1982-05-28 |
| JPH031288B2 true JPH031288B2 (ko) | 1991-01-10 |
Family
ID=15725741
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP16095280A Granted JPS5785316A (en) | 1980-11-14 | 1980-11-14 | Preparation of easily absorbable nifedipine preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5785316A (ko) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7432392B2 (en) | 2003-08-29 | 2008-10-07 | Japan Tobacco Inc. | Ester derivatives and medical use thereof |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5846019A (ja) * | 1981-09-14 | 1983-03-17 | Kanebo Ltd | 持続性ニフエジピン製剤 |
| DE3318649A1 (de) * | 1983-05-21 | 1984-11-22 | Bayer Ag, 5090 Leverkusen | Zweiphasenformulierung |
| DE3419129A1 (de) * | 1984-05-23 | 1985-11-28 | Bayer Ag, 5090 Leverkusen | Nifedipinpraeparate und verfahren zu ihrer herstellung |
| EP0175671A1 (de) * | 1984-08-23 | 1986-03-26 | Kuhlemann & Co. | Pharmazeutische Zubereitung sowie Verfahren zum Darreichen dieser pharmazeutischen Zubereitung |
| DE3438830A1 (de) * | 1984-10-23 | 1986-04-30 | Rentschler Arzneimittel | Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung |
| DE3440288A1 (de) * | 1984-11-05 | 1986-05-07 | Gergely, Gerhard, Dr.-Ing., Wien | Pharmazeutische zubereitung mit einem gehalt an mindestens einer schleimhautreizenden substanz oder dergleichen, insbesondere profen, sowie verfahren zu ihrer herstellung |
| JPH0667824B2 (ja) * | 1988-03-30 | 1994-08-31 | 友昭 福田 | マイクロカプセルの製造方法 |
| EP0580860B2 (en) * | 1991-04-16 | 2004-12-15 | Nippon Shinyaku Company, Limited | Method of manufacturing solid dispersion |
| JP4644397B2 (ja) * | 2001-09-05 | 2011-03-02 | 信越化学工業株式会社 | 難溶性薬物を含む医薬用固形製剤の製造方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5283916A (en) * | 1976-01-02 | 1977-07-13 | Beecham Group Ltd | Medical composition for aural administration |
-
1980
- 1980-11-14 JP JP16095280A patent/JPS5785316A/ja active Granted
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5283916A (en) * | 1976-01-02 | 1977-07-13 | Beecham Group Ltd | Medical composition for aural administration |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7432392B2 (en) | 2003-08-29 | 2008-10-07 | Japan Tobacco Inc. | Ester derivatives and medical use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5785316A (en) | 1982-05-28 |
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