JPH10508306A - 簡単な組成及び高い生物有効性を有する経口投与のためのシクロスポリンの新規処方物及びその製造法 - Google Patents
簡単な組成及び高い生物有効性を有する経口投与のためのシクロスポリンの新規処方物及びその製造法Info
- Publication number
- JPH10508306A JPH10508306A JP8514934A JP51493496A JPH10508306A JP H10508306 A JPH10508306 A JP H10508306A JP 8514934 A JP8514934 A JP 8514934A JP 51493496 A JP51493496 A JP 51493496A JP H10508306 A JPH10508306 A JP H10508306A
- Authority
- JP
- Japan
- Prior art keywords
- cyclosporin
- weight
- parts
- oral administration
- high bioavailability
- 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
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 次のもの: a)活性成分としての1つ又はそれ以上の非晶質シクロスポリン0.5〜2 重量部、有利に1重量部 b)C10〜C22の飽和ヒドロキシ脂肪酸の1つ又はそれ以上のポリエチレン グリコールモノエステル、有利にソルトール(SOLUTOL) HS 15 6〜9 重量部、有利に7.5重量部 c)共溶剤としての1つ又はそれ以上の一価又は多価アルコール、有利にエ タノール及びプロピレングリコール1〜3重量部、有利に2重量部 を含有する飲用可能な溶液又はカプセル剤の形で簡単な組成及び高い生物有 効性を有する経口投与のためのシクロスポリンの新規処方物及びその製造。 2. シクロスポリンA又はシクロスポリンGが非晶質の形で活性成分としてが 使用されている、請求項1記載の投与形。 3. 飲用可能な溶液又はカプセル剤の形で簡単な組成及び高い生物有効性を有 する経口投与のための請求項1又は2に記載のシクロスポリンの新規処方物を製 造する方法において、最初に室温で撹拌しながら a)非晶質シクロスポリン、殊にシクロスポリンA100gをエタノール1 27mlに溶解させ、 b)同様に室温で撹拌しながら、プロピレングリコ ール96mlを添加し、その後に同様に室温で撹拌しながら c)ソルトール(SOLUTOL) HS 15 750gを添加し、シクロスポ リンAの粘稠な澄明溶液を生じさせ、自体公知の方法で飲用可能な溶液として瓶 詰めするか、あるいはカプセルに詰めることを特徴とする、請求項1又は2に記 載のシクロスポリンの新規処方物の製造法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE4438861 | 1994-11-03 | ||
DE4438861.6 | 1994-11-03 | ||
PCT/DE1995/000951 WO1996014079A1 (de) | 1994-11-03 | 1995-07-19 | Neue zubereitungsformen des cyclosporins zur oralen applikation mit einfacher zusammensetzung und hoher bioverfügbarkeit und verfahren zu deren herstellung |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH10508306A true JPH10508306A (ja) | 1998-08-18 |
JP3833248B2 JP3833248B2 (ja) | 2006-10-11 |
Family
ID=6532126
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP51493496A Expired - Fee Related JP3833248B2 (ja) | 1994-11-03 | 1995-07-19 | 簡単な組成及び高い生物有効性を有する経口投与のためのシクロスポリンの新規処方物及びその製造法 |
Country Status (27)
Country | Link |
---|---|
US (1) | US6486124B2 (ja) |
EP (1) | EP0789580B1 (ja) |
JP (1) | JP3833248B2 (ja) |
KR (1) | KR970704464A (ja) |
CN (1) | CN1121238C (ja) |
AT (1) | ATE218359T1 (ja) |
AU (1) | AU715165B2 (ja) |
BG (1) | BG62955B1 (ja) |
BR (1) | BR9509550A (ja) |
CA (1) | CA2231404C (ja) |
CZ (1) | CZ287806B6 (ja) |
DE (2) | DE59510233D1 (ja) |
DK (1) | DK0789580T3 (ja) |
EE (1) | EE03425B1 (ja) |
ES (1) | ES2177652T3 (ja) |
FI (1) | FI118722B (ja) |
HU (1) | HUT77283A (ja) |
LT (1) | LT4306B (ja) |
LV (1) | LV11884B (ja) |
NO (1) | NO970741D0 (ja) |
PL (1) | PL183579B1 (ja) |
PT (1) | PT789580E (ja) |
RU (1) | RU2158601C2 (ja) |
SK (1) | SK164796A3 (ja) |
TR (1) | TR199501361A2 (ja) |
TW (1) | TW492876B (ja) |
WO (1) | WO1996014079A1 (ja) |
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RU2158601C2 (ru) | 1994-11-03 | 2000-11-10 | Новартис Аг | Новые лекарственные формы циклоспорина для орального применения с простым составом и высокой биодоступностью и способ их получения |
US5962019A (en) * | 1995-08-25 | 1999-10-05 | Sangstat Medical Corporation | Oral cyclosporin formulations |
US5766629A (en) * | 1995-08-25 | 1998-06-16 | Sangstat Medical Corporation | Oral cyclosporin formulations |
US5834017A (en) * | 1995-08-25 | 1998-11-10 | Sangstat Medical Corporation | Oral cyclopsporin formulations |
PL319898A1 (en) * | 1995-08-25 | 1997-09-01 | Sangstat Medical Corp | Cyclosporines containing compositions for oral administration |
DE19544507B4 (de) * | 1995-11-29 | 2007-11-15 | Novartis Ag | Cyclosporin enthaltende Präparate |
AU762247B2 (en) * | 1997-01-30 | 2003-06-19 | Novartis Ag | Oil-free pharmaceutical compositions containing cyclosporin A |
NZ336900A (en) * | 1997-01-30 | 2001-06-29 | Novartis Ag | Hard gelatine capsules containing pharmaceutical compositions comprising cyclosporin A and being substantially free of any oil |
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 |
US6656504B1 (en) * | 1999-09-09 | 2003-12-02 | Elan Pharma International Ltd. | Nanoparticulate compositions comprising amorphous cyclosporine and methods of making and using such compositions |
US6506742B2 (en) | 1999-12-13 | 2003-01-14 | Ortho-Mcneil Pharmaceutical, Inc. | Soluble contraceptive liquid formulation |
WO2004050688A1 (en) | 2002-12-02 | 2004-06-17 | Xenome Ltd | NOVEL χ-CONOTOXIN PEPTIDES (-II) |
ATE547424T1 (de) | 2002-12-02 | 2012-03-15 | Xenome Ltd | Chi-conotoxinpeptide mit einer n-terminalen pyroglutaminsäure |
SE0301119D0 (sv) * | 2003-04-14 | 2003-04-14 | Astrazeneca Ab | New non-ionic surfactants for solubilizing poorly soluble molecules |
CN102552917A (zh) | 2003-08-13 | 2012-07-11 | 比奥孔有限公司 | 用于治疗剂的微-粒子脂肪酸盐固体剂量制剂 |
US20050059583A1 (en) | 2003-09-15 | 2005-03-17 | Allergan, Inc. | Methods of providing therapeutic effects using cyclosporin components |
US7135455B2 (en) * | 2004-11-15 | 2006-11-14 | Allergan, Inc | Methods for the therapeutic use of cyclosporine components |
US7151085B2 (en) * | 2004-11-15 | 2006-12-19 | Allergan, Inc. | Therapeutic methods using cyclosporine components |
AU2006235478B2 (en) | 2005-04-12 | 2011-07-21 | Elan Pharma International Limited | Nanoparticulate and controlled release compositions comprising cyclosporine |
US7276476B2 (en) * | 2005-07-13 | 2007-10-02 | Allergan, Inc. | Cyclosporin compositions |
US7297679B2 (en) | 2005-07-13 | 2007-11-20 | Allergan, Inc. | Cyclosporin compositions |
US20070015691A1 (en) | 2005-07-13 | 2007-01-18 | Allergan, Inc. | Cyclosporin compositions |
US7202209B2 (en) | 2005-07-13 | 2007-04-10 | Allergan, Inc. | Cyclosporin compositions |
US7288520B2 (en) * | 2005-07-13 | 2007-10-30 | Allergan, Inc. | Cyclosporin compositions |
US20070015693A1 (en) * | 2005-07-13 | 2007-01-18 | Allergan, Inc. | Cyclosporin compositions |
US7501393B2 (en) * | 2005-07-27 | 2009-03-10 | Allergan, Inc. | Pharmaceutical compositions comprising cyclosporins |
US9839667B2 (en) | 2005-10-14 | 2017-12-12 | Allergan, Inc. | Prevention and treatment of ocular side effects with a cyclosporin |
US7745400B2 (en) * | 2005-10-14 | 2010-06-29 | Gregg Feinerman | Prevention and treatment of ocular side effects with a cyclosporin |
CN104080442B (zh) * | 2011-11-15 | 2018-01-05 | 阿勒根公司 | 环孢菌素a形式2的悬浮液 |
RU2635547C2 (ru) * | 2011-11-15 | 2017-11-14 | Аллерган, Инк. | Форма 2 циклоспорина а и способ ее получения |
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-
1995
- 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 PT PT95925707T patent/PT789580E/pt unknown
- 1995-07-19 DK DK95925707T patent/DK0789580T3/da active
- 1995-07-19 AT AT95925707T patent/ATE218359T1/de not_active IP Right Cessation
- 1995-07-19 EP EP95925707A patent/EP0789580B1/de not_active Expired - Lifetime
- 1995-07-19 WO PCT/DE1995/000951 patent/WO1996014079A1/de not_active Application Discontinuation
- 1995-07-19 EE EE9700112A patent/EE03425B1/xx not_active IP Right Cessation
- 1995-07-19 AU AU29751/95A patent/AU715165B2/en not_active Ceased
- 1995-07-19 SK SK1647-96A patent/SK164796A3/sk unknown
- 1995-07-19 CN CN95196010A patent/CN1121238C/zh not_active Expired - Fee Related
- 1995-07-19 ES ES95925707T patent/ES2177652T3/es not_active Expired - Lifetime
- 1995-07-19 HU HU9702144A patent/HUT77283A/hu unknown
- 1995-07-19 CZ CZ19963616A patent/CZ287806B6/cs not_active IP Right Cessation
- 1995-07-19 DE DE59510233T patent/DE59510233D1/de not_active Expired - Fee Related
- 1995-07-19 KR KR1019970700361A patent/KR970704464A/ko not_active Application Discontinuation
- 1995-07-19 BR BR9509550A patent/BR9509550A/pt not_active Application Discontinuation
- 1995-07-19 JP JP51493496A patent/JP3833248B2/ja not_active Expired - Fee Related
- 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
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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
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1998
- 1998-03-09 PL PL95318560A patent/PL183579B1/pl unknown
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2001
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