JP2007126485A - マグネシウム・オメプラゾール(omeprazole) - Google Patents
マグネシウム・オメプラゾール(omeprazole) Download PDFInfo
- Publication number
- JP2007126485A JP2007126485A JP2007038953A JP2007038953A JP2007126485A JP 2007126485 A JP2007126485 A JP 2007126485A JP 2007038953 A JP2007038953 A JP 2007038953A JP 2007038953 A JP2007038953 A JP 2007038953A JP 2007126485 A JP2007126485 A JP 2007126485A
- Authority
- JP
- Japan
- Prior art keywords
- magnesium
- omeprazole
- methanol
- solution
- composition
- 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.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Abstract
【解決手段】50%未満の結晶化度、及び7重量%未満の残留有機溶媒含量をもつマグネシウム・オメプラゾールを含む組成物を提供する。
【選択図】なし
Description
本発明は、マグネシウム・オメプラゾールの改良された形態、その製法、及びその医薬組成物に関する。
オメプラゾールの一般名で知られる化合物は欧州特許第0005129号に記載されている。
本発明のマグネシウム・オメプラゾールはマグネシウムを低級アルコール中で反応させてマグネシウム・アルコキシドを形成し、オメプラゾールをマグネシウム1モル当たり約2モルの量で加え、そして許容できないレベルでアルコールを閉じ込める結晶又は粒子の成長を許すことなく固体沈殿を形成するために、上記アルコールをフラッシュ蒸発させる。得られる物質は実質的に非晶質(非結晶性)である。
本発明によるマグネシウム・オメプラゾールの製法において、マグネシウムを低級アルコール、好ましくはメタノール中で反応させてアルコールによるマグネシウム・アルコキシド溶液を形成する。
結晶化度=100+C/(A+C)
C=回折図におけるピークの面積(「結晶体面積」)
A=ピークの間及びバックグラウンドの面積(「非晶質面積」)
により計算される。
1.76gの純粋なマグネシウムを1000mL容ガラス・フラスコ中の800gのメタノールに加えた。そのフラスコを緩く取り付けた栓により閉じ(水素ガスの流出を許す緩さ)、そしてそのフラスコを一晩放置した。
従来技術(すなわちEP0124495の実施例6)によるマグネシウム・オメプラゾール無水和物の基準サンプルを製造するために、ステップ2から約20%の前記溶液を1000mL容ビーカーに移した。次にそのビーカーを、減圧下、50℃で4時間乾かすために減圧オーブン内に置いた。この期間終了時、残留メタノールのはっきりとした臭いのない固形物質が残った。この固形物質を試験し、残留メタノールのレベルを決定すると、そのレベルは7.2重量%であることがわかった。
本発明のマグネシウム・オメプラゾールを作製するために、実施例1の溶液の残りを、約140℃の噴射口空気温度、及び約70℃の出口空気温度を用いて、Yamato(商標)スプレー・ドライヤーによりスプレー・ドライした。
次の材料を、以下に示す割合で一緒に混合した:
マグネシウム・オメプラゾール 21.
無水ラクトース 131.
クロスカルメロース・ナトリウム 6.4
マグネシウム・ステアレート 1.6
160.
Claims (8)
- 50%未満の結晶化度、及び7重量%未満の残留有機溶媒含量をもつマグネシウム・オメプラゾールを含む組成物。
- 5重量%未満の残留有機溶媒含量をもつ、請求項1に記載の組成物。
- 2重量%未満の残留有機溶媒含量をもつ、請求項1に記載の組成物。
- 1重量%未満の残留有機溶媒含量をもつ、請求項1に記載の組成物。
- 25%未満の結晶化度をもつ、請求項1〜4のいずれか1項に記載の組成物。
- 請求項1〜5のいずれか1項に記載の組成物を含む経口投与のための固形医薬組成物。
- 錠剤の形態をなす、請求項6に記載の組成物。
- 前記錠剤が腸溶性コートされている、請求項7に記載の組成物。
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CA002290893A CA2290893C (en) | 1999-11-16 | 1999-11-16 | Magnesium omeprazole |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2001538898A Division JP3971187B2 (ja) | 1999-11-16 | 2000-08-04 | マグネシウム・オメプラゾール(omeprazole) |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2007126485A true JP2007126485A (ja) | 2007-05-24 |
Family
ID=4164727
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2001538898A Expired - Fee Related JP3971187B2 (ja) | 1999-11-16 | 2000-08-04 | マグネシウム・オメプラゾール(omeprazole) |
JP2007038953A Pending JP2007126485A (ja) | 1999-11-16 | 2007-02-20 | マグネシウム・オメプラゾール(omeprazole) |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2001538898A Expired - Fee Related JP3971187B2 (ja) | 1999-11-16 | 2000-08-04 | マグネシウム・オメプラゾール(omeprazole) |
Country Status (8)
Country | Link |
---|---|
US (1) | US6713495B1 (ja) |
EP (1) | EP1230237B2 (ja) |
JP (2) | JP3971187B2 (ja) |
AT (1) | ATE265450T1 (ja) |
AU (1) | AU782651B2 (ja) |
CA (1) | CA2290893C (ja) |
DE (1) | DE60010316T3 (ja) |
WO (1) | WO2001036409A1 (ja) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2290893C (en) * | 1999-11-16 | 2007-05-01 | Bernard Charles Sherman | Magnesium omeprazole |
CN1437593A (zh) * | 2000-05-15 | 2003-08-20 | 兰贝克赛实验室有限公司 | 新颖的无定形奥美拉唑盐 |
CA2386716C (en) * | 2002-05-17 | 2012-07-24 | Bernard Charles Sherman | Magnesium salt of s-omeprazole |
US6894066B2 (en) * | 2002-05-09 | 2005-05-17 | Bernard Charles Sherman | Magnesium salt of S-omeprazole |
AU2003262992A1 (en) | 2002-08-30 | 2004-03-19 | Reddy's Laboratories Limited | Amorphous hydrates of esomeprazole magnesium and process for the preparation thereof |
CA2502219C (en) | 2002-10-16 | 2012-05-29 | Takeda Pharmaceutical Company Limited | A process for producing an amorphous isomer of lansoprazole |
US20040235903A1 (en) * | 2002-10-22 | 2004-11-25 | Khanna Mahavir Singh | Amorphous form of esomeprazole salts |
US20060094762A1 (en) * | 2003-01-07 | 2006-05-04 | Yatendra Kumar | Magnesium salt of imidazole derivative |
CN100364987C (zh) | 2003-03-24 | 2008-01-30 | 卫材R&D管理有限公司 | 亚砜衍生物或其盐的非定形态的制备方法 |
CA2591983A1 (en) * | 2004-12-20 | 2006-06-29 | Dr. Reddy's Laboratories Ltd. | Pharmaceutical compositions comprising amorphous benzimidazole compounds |
EP1830823A2 (en) | 2004-12-23 | 2007-09-12 | Ranbaxy Laboratories Limited | Stable oral benzimidazole compositions and process of preparation thereof |
US20080279951A1 (en) * | 2005-02-02 | 2008-11-13 | Rajesh Gandhi | Stable Oral Benzimidazole Compositions Prepared by Non-Aqueous Layering Process |
CA2600456A1 (en) * | 2005-03-08 | 2006-09-14 | Dr. Reddy's Laboratories Ltd. | Process for preparing amorphous salts |
EP1801110A1 (en) | 2005-12-22 | 2007-06-27 | KRKA, tovarna zdravil, d.d., Novo mesto | Esomeprazole arginine salt |
US7553857B2 (en) * | 2005-12-23 | 2009-06-30 | Lek Pharmaceuticals D.D. | S-omeprazole magnesium |
EP1947099A1 (en) * | 2007-01-18 | 2008-07-23 | LEK Pharmaceuticals D.D. | Process for solvent removal from omeprazole salts |
US8911787B2 (en) | 2008-02-26 | 2014-12-16 | Ranbaxy Laboratories Limited | Stable oral benzimidazole compositions and process of preparation thereof |
US20090280173A1 (en) * | 2008-05-09 | 2009-11-12 | Ishwar Chauhan | Multilayer Omeprazole Tablets |
EP2147918A1 (en) | 2008-07-21 | 2010-01-27 | LEK Pharmaceuticals D.D. | Process for the preparation of S-omeprazole magnesium in a stable form |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH05194225A (ja) * | 1991-11-07 | 1993-08-03 | Yoshitomi Pharmaceut Ind Ltd | 安定化された抗潰瘍剤含有製剤 |
JPH08134101A (ja) * | 1994-11-15 | 1996-05-28 | Daicel Chem Ind Ltd | 粉粒状セルロースエステルの製造方法 |
WO1997041114A1 (en) * | 1996-04-26 | 1997-11-06 | Astra Aktiebolag | Process for the preparation of a magnesium salt of a substituted sulphinyl heterocycle |
WO2001036409A1 (en) * | 1999-11-16 | 2001-05-25 | Bernard Charles Sherman | Magnesium omeprazole |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE7804231L (sv) | 1978-04-14 | 1979-10-15 | Haessle Ab | Magsyrasekretionsmedel |
SE8301182D0 (sv) * | 1983-03-04 | 1983-03-04 | Haessle Ab | Novel compounds |
SE9302396D0 (sv) | 1993-07-09 | 1993-07-09 | Ab Astra | A novel compound form |
ES2100142T3 (es) | 1994-07-08 | 2002-03-01 | Astrazeneca Ab | Forma de dosificacion en tabletas i constituida por unidades multiples. |
US6048981A (en) | 1998-04-22 | 2000-04-11 | Torcan Chemical Ltd. | Magnesium omeprazole and process for its preparation |
SE9804003D0 (sv) * | 1998-11-23 | 1998-11-23 | Astra Ab | A method of producing drug particles |
CN1437593A (zh) * | 2000-05-15 | 2003-08-20 | 兰贝克赛实验室有限公司 | 新颖的无定形奥美拉唑盐 |
-
1999
- 1999-11-16 CA CA002290893A patent/CA2290893C/en not_active Expired - Fee Related
-
2000
- 2000-08-04 WO PCT/CA2000/000901 patent/WO2001036409A1/en active IP Right Grant
- 2000-08-04 AT AT00952815T patent/ATE265450T1/de not_active IP Right Cessation
- 2000-08-04 EP EP00952815A patent/EP1230237B2/en not_active Expired - Lifetime
- 2000-08-04 AU AU65511/00A patent/AU782651B2/en not_active Ceased
- 2000-08-04 JP JP2001538898A patent/JP3971187B2/ja not_active Expired - Fee Related
- 2000-08-04 US US10/129,622 patent/US6713495B1/en not_active Expired - Fee Related
- 2000-08-04 DE DE60010316T patent/DE60010316T3/de not_active Expired - Lifetime
-
2007
- 2007-02-20 JP JP2007038953A patent/JP2007126485A/ja active Pending
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH05194225A (ja) * | 1991-11-07 | 1993-08-03 | Yoshitomi Pharmaceut Ind Ltd | 安定化された抗潰瘍剤含有製剤 |
JPH08134101A (ja) * | 1994-11-15 | 1996-05-28 | Daicel Chem Ind Ltd | 粉粒状セルロースエステルの製造方法 |
WO1997041114A1 (en) * | 1996-04-26 | 1997-11-06 | Astra Aktiebolag | Process for the preparation of a magnesium salt of a substituted sulphinyl heterocycle |
WO2001036409A1 (en) * | 1999-11-16 | 2001-05-25 | Bernard Charles Sherman | Magnesium omeprazole |
Also Published As
Publication number | Publication date |
---|---|
AU6551100A (en) | 2001-05-30 |
JP2003514813A (ja) | 2003-04-22 |
EP1230237B2 (en) | 2011-07-20 |
US6713495B1 (en) | 2004-03-30 |
DE60010316D1 (de) | 2004-06-03 |
EP1230237B1 (en) | 2004-04-28 |
CA2290893C (en) | 2007-05-01 |
DE60010316T2 (de) | 2005-05-04 |
DE60010316T3 (de) | 2012-01-26 |
CA2290893A1 (en) | 2001-05-16 |
AU782651B2 (en) | 2005-08-18 |
EP1230237A1 (en) | 2002-08-14 |
JP3971187B2 (ja) | 2007-09-05 |
WO2001036409A1 (en) | 2001-05-25 |
ATE265450T1 (de) | 2004-05-15 |
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