RU97108682A - Новые лекарственные формы циклоспорина для орального применения с простым составом и с высокой биоготовностью и способ их получения - Google Patents
Новые лекарственные формы циклоспорина для орального применения с простым составом и с высокой биоготовностью и способ их полученияInfo
- Publication number
- RU97108682A RU97108682A RU97108682/14A RU97108682A RU97108682A RU 97108682 A RU97108682 A RU 97108682A RU 97108682/14 A RU97108682/14 A RU 97108682/14A RU 97108682 A RU97108682 A RU 97108682A RU 97108682 A RU97108682 A RU 97108682A
- Authority
- RU
- Russia
- Prior art keywords
- cyclosporin
- simple composition
- solution
- drinking
- oral use
- Prior art date
Links
- PMATZTZNYRCHOR-CGLBZJNRSA-N (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17 Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 title claims 7
- 108010036949 Cyclosporine Proteins 0.000 title claims 7
- 229960001265 ciclosporin Drugs 0.000 title claims 7
- 239000000203 mixture Substances 0.000 title claims 3
- 238000004519 manufacturing process Methods 0.000 title 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 4
- 239000002775 capsule Substances 0.000 claims 3
- 230000035622 drinking Effects 0.000 claims 3
- 235000021271 drinking Nutrition 0.000 claims 3
- 230000004634 feeding behavior Effects 0.000 claims 3
- 238000003756 stirring Methods 0.000 claims 3
- CYAMZYIUAHNTBO-UHFFFAOYSA-N 11-hydroxy-17-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]heptadecanoic acid Chemical compound OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCCCCCC(O)CCCCCCCCCC(O)=O CYAMZYIUAHNTBO-UHFFFAOYSA-N 0.000 claims 2
- 230000036912 Bioavailability Effects 0.000 claims 2
- 229940119017 Cyclosporine Drugs 0.000 claims 2
- 230000035514 bioavailability Effects 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- ZMKGDQSIRSGUDJ-IMVLJIQESA-N 33-[(E)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-30-propyl-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone Chemical compound CCCC1NC(=O)C(C(O)C(C)C\C=C\C)N(C)C(=O)C(C(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(C)NC(=O)C(C)NC(=O)C(CC(C)C)N(C)C(=O)C(C(C)C)NC(=O)C(CC(C)C)N(C)C(=O)CN(C)C1=O ZMKGDQSIRSGUDJ-IMVLJIQESA-N 0.000 claims 1
- 108010036941 Cyclosporins Proteins 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 150000001298 alcohols Chemical class 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 108010019249 cyclosporin G Proteins 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- -1 hydroxy fatty acids Chemical class 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
Claims (3)
1. Новые лекарственные формы введения циклоспорина для орального применения с простым составом и с высокой биоготовностью в виде раствора для питья или капсул, отличающиеся тем, что содержат а) от 0,5 до 2, предпочтительно 1 вес. ч. одного или нескольких аморфных циклоспоринов в качестве активного вещества; б) от 6 до 9, предпочтительно 7,5 вес. ч. одного или нескольких сложных полиэтиленгликолевых моноэфиров насыщенных C10-C22 - оксижирных кислот, предпочтительно Солутола® HS15; с) 1 - 3, предпочтительно 2 вес. ч. одного или нескольких одноатомных или многоатомных спиртов в качестве сорастворителей, предпочтительно этанол и пропиленгликоль, и их получение.
2. Формы введения по п.1, отличающиеся тем, что в качестве активного вещества применяют циклоспорин A или циклоспорин G в аморфной форме.
3. Способ получения новых лекарственных форм циклоспорина для орального применения с простым составом и с высокой биоготовностью в форме раствора для питья или капсул по пп.1 и 2, отличающийся тем, что сначала при перемешивании и при комнатной температуре а) 100 г аморфного циклоспорина, особенно циклоспорина A растворяют в 127 мл этанола; б) также при перемешивании и при комнатной температуре производят добавку 96 мл пропиленгликоля и в заключение также при перемешивании и при комнатной температуре; с) добавляют 750 г Солутола® HS15, причем образуется прозрачный, вязкий раствор циклоспорина A, который известным способом расфасовывается как раствор для питья или как капсулы.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4438861 | 1994-11-03 | ||
| DEP4438861.6 | 1994-11-03 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU97108682A true RU97108682A (ru) | 1999-05-10 |
| RU2158601C2 RU2158601C2 (ru) | 2000-11-10 |
Family
ID=6532126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU97108682/14A RU2158601C2 (ru) | 1994-11-03 | 1995-07-19 | Новые лекарственные формы циклоспорина для орального применения с простым составом и высокой биодоступностью и способ их получения |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US6486124B2 (ru) |
| EP (1) | EP0789580B1 (ru) |
| JP (1) | JP3833248B2 (ru) |
| KR (1) | KR970704464A (ru) |
| CN (1) | CN1121238C (ru) |
| AT (1) | ATE218359T1 (ru) |
| AU (1) | AU715165B2 (ru) |
| BG (1) | BG62955B1 (ru) |
| BR (1) | BR9509550A (ru) |
| CA (1) | CA2231404C (ru) |
| CZ (1) | CZ287806B6 (ru) |
| DE (2) | DE59510233D1 (ru) |
| DK (1) | DK0789580T3 (ru) |
| EE (1) | EE03425B1 (ru) |
| ES (1) | ES2177652T3 (ru) |
| FI (1) | FI118722B (ru) |
| HU (1) | HUT77283A (ru) |
| LT (1) | LT4306B (ru) |
| LV (1) | LV11884B (ru) |
| NO (1) | NO970741D0 (ru) |
| PL (1) | PL183579B1 (ru) |
| PT (1) | PT789580E (ru) |
| RU (1) | RU2158601C2 (ru) |
| SK (1) | SK164796A3 (ru) |
| TR (1) | TR199501361A2 (ru) |
| TW (1) | TW492876B (ru) |
| WO (1) | WO1996014079A1 (ru) |
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| US5766629A (en) * | 1995-08-25 | 1998-06-16 | Sangstat Medical Corporation | Oral cyclosporin formulations |
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| DE19821951A1 (de) * | 1998-05-15 | 1999-11-18 | Basf Ag | Cyclosporin-Zubereitungen |
| AUPP627498A0 (en) | 1998-10-02 | 1998-10-22 | University Of Queensland, The | Novel peptides - i |
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| US9839667B2 (en) | 2005-10-14 | 2017-12-12 | Allergan, Inc. | Prevention and treatment of ocular side effects with a cyclosporin |
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-
1995
- 1995-07-19 PT PT95925707T patent/PT789580E/pt unknown
- 1995-07-19 WO PCT/DE1995/000951 patent/WO1996014079A1/de not_active Application Discontinuation
- 1995-07-19 RU RU97108682/14A patent/RU2158601C2/ru active
- 1995-07-19 CA CA002231404A patent/CA2231404C/en not_active Expired - Fee Related
- 1995-07-19 EE EE9700112A patent/EE03425B1/xx not_active IP Right Cessation
- 1995-07-19 HU HU9702144A patent/HUT77283A/hu unknown
- 1995-07-19 ES ES95925707T patent/ES2177652T3/es not_active Expired - Lifetime
- 1995-07-19 SK SK1647-96A patent/SK164796A3/sk unknown
- 1995-07-19 KR KR1019970700361A patent/KR970704464A/ko not_active Application Discontinuation
- 1995-07-19 CZ CZ19963616A patent/CZ287806B6/cs not_active IP Right Cessation
- 1995-07-19 AT AT95925707T patent/ATE218359T1/de not_active IP Right Cessation
- 1995-07-19 CN CN95196010A patent/CN1121238C/zh not_active Expired - Fee Related
- 1995-07-19 JP JP51493496A patent/JP3833248B2/ja not_active Expired - Fee Related
- 1995-07-19 DE DE59510233T patent/DE59510233D1/de not_active Expired - Fee Related
- 1995-07-19 AU AU29751/95A patent/AU715165B2/en not_active Ceased
- 1995-07-19 DK DK95925707T patent/DK0789580T3/da active
- 1995-07-19 EP EP95925707A patent/EP0789580B1/de not_active Expired - Lifetime
- 1995-07-19 BR BR9509550A patent/BR9509550A/pt not_active Application Discontinuation
- 1995-08-08 TW TW084108225A patent/TW492876B/zh active
- 1995-10-26 DE DE19539860A patent/DE19539860A1/de not_active Withdrawn
- 1995-11-02 TR TR95/01361A patent/TR199501361A2/xx unknown
-
1997
- 1997-01-06 BG BG101117A patent/BG62955B1/bg unknown
- 1997-01-09 LT LT97-002A patent/LT4306B/lt not_active IP Right Cessation
- 1997-02-14 FI FI970634A patent/FI118722B/fi active IP Right Grant
- 1997-02-18 NO NO970741A patent/NO970741D0/no not_active Application Discontinuation
- 1997-05-14 LV LVP-97-94A patent/LV11884B/lv unknown
-
1998
- 1998-03-09 PL PL95318560A patent/PL183579B1/pl unknown
-
2001
- 2001-10-17 US US09/981,929 patent/US6486124B2/en not_active Expired - Fee Related
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