JPS58116414A - ニカルジピン持続性製剤用球形顆粒およびその製造法 - Google Patents
ニカルジピン持続性製剤用球形顆粒およびその製造法Info
- Publication number
- JPS58116414A JPS58116414A JP56208608A JP20860881A JPS58116414A JP S58116414 A JPS58116414 A JP S58116414A JP 56208608 A JP56208608 A JP 56208608A JP 20860881 A JP20860881 A JP 20860881A JP S58116414 A JPS58116414 A JP S58116414A
- Authority
- JP
- Japan
- Prior art keywords
- nicardipine
- composition
- spherular
- salt
- water
- 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 abstract description 35
- ZBBHBTPTTSWHBA-UHFFFAOYSA-N Nicardipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN(C)CC=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ZBBHBTPTTSWHBA-UHFFFAOYSA-N 0.000 title claims abstract description 23
- 229960001783 nicardipine Drugs 0.000 title claims abstract description 23
- 238000002360 preparation method Methods 0.000 title claims description 15
- 230000002035 prolonged effect Effects 0.000 title abstract 3
- 239000008187 granular material Substances 0.000 claims abstract description 21
- 239000000126 substance Substances 0.000 claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 13
- 239000000654 additive Substances 0.000 claims abstract description 11
- 239000004094 surface-active agent Substances 0.000 claims abstract description 10
- 239000003960 organic solvent Substances 0.000 claims abstract description 9
- 238000005507 spraying Methods 0.000 claims abstract description 7
- 229920003169 water-soluble polymer Polymers 0.000 claims description 9
- 230000001419 dependent effect Effects 0.000 claims description 8
- 230000000996 additive effect Effects 0.000 claims description 5
- 239000002245 particle Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000008202 granule composition Substances 0.000 claims 1
- 238000000576 coating method Methods 0.000 abstract description 11
- 239000003814 drug Substances 0.000 abstract description 10
- 239000011248 coating agent Substances 0.000 abstract description 9
- 239000008280 blood Substances 0.000 abstract description 5
- 210000004369 blood Anatomy 0.000 abstract description 5
- 206010002383 Angina Pectoris Diseases 0.000 abstract description 2
- 206010020772 Hypertension Diseases 0.000 abstract description 2
- 208000026106 cerebrovascular disease Diseases 0.000 abstract description 2
- 229920000642 polymer Polymers 0.000 abstract 2
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 239000002775 capsule Substances 0.000 description 11
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 9
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- 229940079593 drug Drugs 0.000 description 8
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 6
- 238000007796 conventional method Methods 0.000 description 6
- 238000001035 drying Methods 0.000 description 5
- 239000012530 fluid Substances 0.000 description 4
- 239000000454 talc Substances 0.000 description 4
- 229910052623 talc Inorganic materials 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 3
- 230000000968 intestinal effect Effects 0.000 description 3
- -1 propatool Substances 0.000 description 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- 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 2
- 239000007788 liquid Substances 0.000 description 2
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 230000002459 sustained effect Effects 0.000 description 2
- 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 1
- 229920003136 Eudragit® L polymer Polymers 0.000 description 1
- 229920003155 Eudragit® RL 100 Polymers 0.000 description 1
- 229920003151 Eudragit® RL polymer Polymers 0.000 description 1
- 229920003134 Eudragit® polymer Polymers 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 1
- 229920003091 Methocel™ Polymers 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 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 1
- 229930006000 Sucrose Natural products 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 150000005215 alkyl ethers Chemical class 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 239000008199 coating composition Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 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 1
- 229920001477 hydrophilic polymer Polymers 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 210000004347 intestinal mucosa Anatomy 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 239000002075 main ingredient Substances 0.000 description 1
- 210000004379 membrane Anatomy 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- DNKKLDKIFMDAPT-UHFFFAOYSA-N n,n-dimethylmethanamine;2-methylprop-2-enoic acid Chemical compound CN(C)C.CC(=C)C(O)=O.CC(=C)C(O)=O DNKKLDKIFMDAPT-UHFFFAOYSA-N 0.000 description 1
- 229960002289 nicardipine hydrochloride Drugs 0.000 description 1
- AIKVCUNQWYTVTO-UHFFFAOYSA-N nicardipine hydrochloride Chemical compound Cl.COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN(C)CC=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 AIKVCUNQWYTVTO-UHFFFAOYSA-N 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 239000005871 repellent Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Priority Applications (10)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP56208608A JPS58116414A (ja) | 1981-12-23 | 1981-12-23 | ニカルジピン持続性製剤用球形顆粒およびその製造法 |
| MX82101116U MX7567E (es) | 1981-12-23 | 1982-12-16 | Procedimiento para recubrir nicardipina de accion prolongada |
| AT0460682A AT386743B (de) | 1981-12-23 | 1982-12-20 | Verfahren zur herstellung einer langwirkenden nicardipinzubereitung |
| CA000418228A CA1200494A (en) | 1981-12-23 | 1982-12-21 | Process of producing composition for long acting nicardipine preparation |
| GR70132A GR77096B (enExample) | 1981-12-23 | 1982-12-21 | |
| PT76023A PT76023B (en) | 1981-12-23 | 1982-12-22 | A process of producing composition for long acting nicardipine preparation |
| IT68503/82A IT1200966B (it) | 1981-12-23 | 1982-12-22 | Composizione per preparati di nicardipina a lunga azione in forma di granuli sferici e procedimento per la produzione della composizione |
| ES518487A ES518487A0 (es) | 1981-12-23 | 1982-12-22 | Un procedimiento para producir una composicion para un preparado de accion prolongada de nicardipina. |
| KR8205782A KR860001147B1 (ko) | 1981-12-23 | 1982-12-23 | 지속성 니카르디핀 제제용 조성물의 제조방법 |
| US07/013,326 US4758437A (en) | 1981-12-23 | 1987-02-11 | Composition for long acting nicardipine preparation and process of producing the composition |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP56208608A JPS58116414A (ja) | 1981-12-23 | 1981-12-23 | ニカルジピン持続性製剤用球形顆粒およびその製造法 |
| US07/013,326 US4758437A (en) | 1981-12-23 | 1987-02-11 | Composition for long acting nicardipine preparation and process of producing the composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS58116414A true JPS58116414A (ja) | 1983-07-11 |
| JPS647047B2 JPS647047B2 (enExample) | 1989-02-07 |
Family
ID=26516929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP56208608A Granted JPS58116414A (ja) | 1981-12-23 | 1981-12-23 | ニカルジピン持続性製剤用球形顆粒およびその製造法 |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS58116414A (enExample) |
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61148114A (ja) * | 1984-11-15 | 1986-07-05 | Teijin Ltd | ニフエジピンの顆粒剤 |
| WO1986005393A1 (fr) * | 1985-03-14 | 1986-09-25 | Teysan Pharmaceuticals Co., Ltd. | Preparation antibiotique granulaire composite stabilisee |
| JPS63310827A (ja) * | 1987-06-15 | 1988-12-19 | Sanwa Kagaku Kenkyusho Co Ltd | ニコチン酸誘導体を主剤とする徐放性製剤 |
| JPS6470414A (en) * | 1987-08-11 | 1989-03-15 | Bayer Ag | Dihydropyridine-containing continuous medicine |
| JPH01249718A (ja) * | 1988-03-30 | 1989-10-05 | Tomoaki Fukuda | マイクロカプセルの製造方法 |
| JPH01313427A (ja) * | 1988-04-29 | 1989-12-18 | Bayer Ag | ジヒドロピリジン類を含有する徐放性製剤 |
| JPH01313431A (ja) * | 1988-04-27 | 1989-12-18 | Sanofi Sa | ジルチアゼム・マイクロビーズ、その製法および徐放性医薬組成物 |
| JPH02705A (ja) * | 1988-01-18 | 1990-01-05 | Lek Tovarna Farmacevtskih | ニカルジピン又はその塩酸塩のβ―シクロデキストリン包接複合体及びそれを含有する医薬製剤 |
| US4938968A (en) * | 1988-07-26 | 1990-07-03 | Norjec Development Associates, Inc. | Controlled release indomethacin |
| EP0164959B1 (en) * | 1984-06-04 | 1992-03-11 | Sterwin Ag. | Pharmaceutical composition in sustained release unit dose form and process for its preparation |
| WO1992018109A1 (en) * | 1991-04-15 | 1992-10-29 | Yamanouchi Pharmaceutical Co., Ltd. | Rapidly soluble solid preparation |
| JP2000080028A (ja) * | 1998-07-17 | 2000-03-21 | Dev Center For Biotechnol | 長持続時間を有するシサプリドの経口剤形 |
| JP2000229888A (ja) * | 1999-02-10 | 2000-08-22 | Pfizer Prod Inc | マトリックス制御放出デバイス |
| JP2003503341A (ja) * | 1999-06-28 | 2003-01-28 | サノフィ−サンテラボ | 少なくとも一つの適時パルスを生ずる制御された放出用の医薬投与形態 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5587717A (en) * | 1978-12-05 | 1980-07-02 | Haessle Ab | Cardiotonic glycoside containing medicine |
| DE3024858A1 (de) * | 1979-07-05 | 1981-01-22 | Yamanouchi Pharma Co Ltd | Anhaltend freigebende pharmazeutische zubereitung eines festen medikamentmaterials |
-
1981
- 1981-12-23 JP JP56208608A patent/JPS58116414A/ja active Granted
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5587717A (en) * | 1978-12-05 | 1980-07-02 | Haessle Ab | Cardiotonic glycoside containing medicine |
| DE3024858A1 (de) * | 1979-07-05 | 1981-01-22 | Yamanouchi Pharma Co Ltd | Anhaltend freigebende pharmazeutische zubereitung eines festen medikamentmaterials |
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0164959B1 (en) * | 1984-06-04 | 1992-03-11 | Sterwin Ag. | Pharmaceutical composition in sustained release unit dose form and process for its preparation |
| JPS61148114A (ja) * | 1984-11-15 | 1986-07-05 | Teijin Ltd | ニフエジピンの顆粒剤 |
| WO1986005393A1 (fr) * | 1985-03-14 | 1986-09-25 | Teysan Pharmaceuticals Co., Ltd. | Preparation antibiotique granulaire composite stabilisee |
| JPS63310827A (ja) * | 1987-06-15 | 1988-12-19 | Sanwa Kagaku Kenkyusho Co Ltd | ニコチン酸誘導体を主剤とする徐放性製剤 |
| JPS6470414A (en) * | 1987-08-11 | 1989-03-15 | Bayer Ag | Dihydropyridine-containing continuous medicine |
| JPH02705A (ja) * | 1988-01-18 | 1990-01-05 | Lek Tovarna Farmacevtskih | ニカルジピン又はその塩酸塩のβ―シクロデキストリン包接複合体及びそれを含有する医薬製剤 |
| JPH01249718A (ja) * | 1988-03-30 | 1989-10-05 | Tomoaki Fukuda | マイクロカプセルの製造方法 |
| JPH01313431A (ja) * | 1988-04-27 | 1989-12-18 | Sanofi Sa | ジルチアゼム・マイクロビーズ、その製法および徐放性医薬組成物 |
| JPH01313427A (ja) * | 1988-04-29 | 1989-12-18 | Bayer Ag | ジヒドロピリジン類を含有する徐放性製剤 |
| US4938968A (en) * | 1988-07-26 | 1990-07-03 | Norjec Development Associates, Inc. | Controlled release indomethacin |
| WO1992018109A1 (en) * | 1991-04-15 | 1992-10-29 | Yamanouchi Pharmaceutical Co., Ltd. | Rapidly soluble solid preparation |
| US5624687A (en) * | 1991-04-15 | 1997-04-29 | Yamanouchi Pharmaceutical Co., Ltd. | Quick-dissolution solid preparation |
| JP2000080028A (ja) * | 1998-07-17 | 2000-03-21 | Dev Center For Biotechnol | 長持続時間を有するシサプリドの経口剤形 |
| JP2000229888A (ja) * | 1999-02-10 | 2000-08-22 | Pfizer Prod Inc | マトリックス制御放出デバイス |
| JP2005320354A (ja) * | 1999-02-10 | 2005-11-17 | Pfizer Prod Inc | マトリックス制御放出デバイス |
| JP2003503341A (ja) * | 1999-06-28 | 2003-01-28 | サノフィ−サンテラボ | 少なくとも一つの適時パルスを生ずる制御された放出用の医薬投与形態 |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS647047B2 (enExample) | 1989-02-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EXPY | Cancellation because of completion of term | ||
| R154 | Certificate of patent or utility model (reissue) |
Free format text: JAPANESE INTERMEDIATE CODE: R154 |