JPH03500658A - 安定な医薬組成物 - Google Patents
安定な医薬組成物Info
- Publication number
- JPH03500658A JPH03500658A JP1505939A JP50593989A JPH03500658A JP H03500658 A JPH03500658 A JP H03500658A JP 1505939 A JP1505939 A JP 1505939A JP 50593989 A JP50593989 A JP 50593989A JP H03500658 A JPH03500658 A JP H03500658A
- Authority
- JP
- Japan
- Prior art keywords
- esmolol
- composition
- buffer
- decomposition
- solution
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
-
- 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
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (8)
- 1.有効量のメチル3−〔4−(2−ヒドロキシ−3−イソプロピルアミノ)プ ロポキシ〕フエニルプロピオネート塩酸塩(エスモロール)を含有する、心臓病 状態の治療のための注射しうる水性医薬組成物であって、該組成物は溶液1ml 当たり約1mgから約250mgのエスモロールおよび0.01〜0.04Mの 緩衝剤を含有し、該組成物はpH範囲約4.5〜5.5を有し、該エスモロール は水溶液中で分解して3−〔4−(3−プロピオン酸)−フェノキシ〕−1−イ ソプロピルアミノ−2−プロパノール塩酸塩を生成し、該3−〔4−(3−プロ ピオン酸)−フエノキシ〕−1−イソプロピルアミノ−2−プロパノール塩酸塩 は前記組成物のpH範囲内のpKを有していてそれにより緩衝剤を添加すること なく緩衝容量を高めるための二次緩衝剤として作用しかつ分解が起こる際のpH 変化を最小限に抑え、それにより水性組成物中におけるエスモロールの安定性が 高められるものである組成物。
- 2.緩衝剤が酢酸塩、酒石酸塩、乳酸塩、グルコン酸塩および燐酸塩緩衝剤から なる群から選択される請求項1記載の組成物。
- 3.緩衝剤が酢酸塩緩衝剤である請求項2記載の組成物。
- 4.溶液1ml当たり約10mgを含有する請求項3記載の組成物。
- 5.酢酸塩緩衝剤の濃度が約0.05Mである請求項4記載の組成物。
- 6.pH約4.9〜約5.1を有する請求項5記載の組成物。
- 7.有効量のメチル3−〔4−(2−ヒドロキシ−3−イソプロピルアミノ)プ ロポキシ〕フエニルプロピオネート塩酸塩(エスモロール)を含有する、心臓病 状態の治療のための安定な注射しうる水性医薬組成物であって、該組成物は溶液 1ml当たり約10mgのエスモロールおよび約0.05Mの緩衝剤を含有し、 該組成物はpH範囲約4.5〜5.5を有し、該エスモロールは水溶液中で分解 して3−〔4−(3−プロピオン酸)−フエノキシ〕−1−イソプロピルアミノ −2−プロパノール塩酸塩を生成し、該3−〔4−(3−プロピオン酸)−フエ ノキシ〕−1−イソプロピルアミノ−2−プロパノール塩酸塩は前記組成物のp H範囲内のpKを有していてそれにより緩衝剤を添加することなく緩衝容量を高 めるための二次緩衝剤とし作用しかつ分解が起こる際のpH変化を最小限に抑え 、それにより水性組成物中におけるエスモロールの安定性が高められるものであ る組成物。
- 8.pH約4.9〜約5.1を有する請求項7記載の組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US203836 | 1988-06-08 | ||
US07/203,836 US4857552A (en) | 1988-06-08 | 1988-06-08 | Stable pharmaceutical composition |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH03500658A true JPH03500658A (ja) | 1991-02-14 |
JP2552372B2 JP2552372B2 (ja) | 1996-11-13 |
Family
ID=22755531
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP1505939A Expired - Lifetime JP2552372B2 (ja) | 1988-06-08 | 1989-05-04 | 安定な医薬組成物 |
Country Status (13)
Country | Link |
---|---|
US (1) | US4857552A (ja) |
EP (1) | EP0403578B1 (ja) |
JP (1) | JP2552372B2 (ja) |
AU (1) | AU613196B2 (ja) |
CA (1) | CA1334001C (ja) |
DE (1) | DE68918847T2 (ja) |
DK (1) | DK32490A (ja) |
HU (1) | HUT54041A (ja) |
IL (1) | IL90551A (ja) |
MY (1) | MY104030A (ja) |
NZ (1) | NZ229410A (ja) |
WO (1) | WO1989011855A1 (ja) |
ZA (1) | ZA894344B (ja) |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2004519506A (ja) * | 2001-01-12 | 2004-07-02 | バクスター・インターナショナル・インコーポレイテッド | エスモロール処方物 |
JP2010024249A (ja) * | 2001-01-12 | 2010-02-04 | Baxter Internatl Inc | エスモロール処方物 |
JP2010528001A (ja) * | 2007-05-22 | 2010-08-19 | バクスター・インターナショナル・インコーポレイテッド | 着色されたエスモロール濃縮物 |
JP2010528025A (ja) * | 2007-05-22 | 2010-08-19 | バクスター・インターナショナル・インコーポレイテッド | ベンジルアルコールとの多用量濃縮エスモロール |
JP2010528000A (ja) * | 2007-05-22 | 2010-08-19 | バクスター・インターナショナル・インコーポレイテッド | 濃縮エスモロール |
JP2011506486A (ja) * | 2007-12-21 | 2011-03-03 | エイオーピー オーファン ファーマスーティカルズ アクチエンゲゼルシャフト | 医薬組成物 |
JP2013505231A (ja) * | 2009-09-22 | 2013-02-14 | ヴイライフ サイエンシズ テクノロジーズ プライベート リミテッド | 糖尿病性足潰瘍用の局所用製剤 |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5405376A (en) * | 1993-08-27 | 1995-04-11 | Medtronic, Inc. | Method and apparatus for ablation |
WO1999007354A2 (en) * | 1997-08-08 | 1999-02-18 | Duke University | Compositions, apparatus and methods for facilitating surgical procedures |
US6711436B1 (en) | 1997-08-08 | 2004-03-23 | Duke University | Compositions, apparatus and methods for facilitating surgical procedures |
CA2461349C (en) | 2001-09-26 | 2011-11-29 | Baxter International Inc. | Preparation of submicron sized nanoparticles via dispersion and solvent or liquid phase removal |
EP1417962A1 (de) * | 2002-11-06 | 2004-05-12 | AOP Orphan Pharmaceuticals AG | Verfahren zur Herstellung eines Arzneimittels enthaltend Esmolol |
AU2014203121B2 (en) * | 2007-05-22 | 2016-04-21 | Baxter Healthcare Sa | Concentrate esmolol |
ES2363964B1 (es) | 2009-11-20 | 2012-08-22 | Gp Pharm, S.A. | Cápsulas de principios activos farmacéuticos y ésteres de ácidos grasos poliinsaturados. |
US20120053240A1 (en) * | 2009-12-18 | 2012-03-01 | Metabolic Technologies, Inc. | Method of Administering beta-hydroxy-beta-methylbutyrate (HMB) |
BR112013016701A2 (pt) | 2011-01-27 | 2017-07-04 | Baxter Healthcare Sa | métodos para tratar a taquicardia e/ou controlar a frequência cardíaca enquanto minimiza e/ou controla a hipotensão. |
MX2013008715A (es) | 2011-01-27 | 2013-08-29 | Baxter Healthcare Sa | Uso de (s) -esmolol para controlar la irritacion venosa asociada con el tratamiento de un padecimiento cardiaco. |
US8835505B1 (en) * | 2013-03-15 | 2014-09-16 | Welgrace Research Group | Ready-to-use co-solvents pharmaceutical composition in modified flexible plastic container |
CN104473869A (zh) * | 2014-11-20 | 2015-04-01 | 北京京科泰来科技有限公司 | 一种艾司洛尔脂肪乳及其制备方法 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4454154A (en) * | 1981-06-23 | 1984-06-12 | American Hospital Supply Corporation | Method for treating glaucoma by the topical administration of selectively metabolized beta-blocking agents |
AU575153B2 (en) * | 1984-04-09 | 1988-07-21 | Du Pont Merck Pharmaceutical Company, The | Pharmaceutical compositions and method for treatment for prophylaxis of cardiac disorders |
-
1988
- 1988-06-08 US US07/203,836 patent/US4857552A/en not_active Expired - Fee Related
-
1989
- 1989-05-04 JP JP1505939A patent/JP2552372B2/ja not_active Expired - Lifetime
- 1989-05-04 HU HU892994A patent/HUT54041A/hu unknown
- 1989-05-04 EP EP89905887A patent/EP0403578B1/en not_active Expired - Lifetime
- 1989-05-04 WO PCT/US1989/001834 patent/WO1989011855A1/en active IP Right Grant
- 1989-05-04 AU AU35704/89A patent/AU613196B2/en not_active Ceased
- 1989-05-04 DE DE68918847T patent/DE68918847T2/de not_active Expired - Fee Related
- 1989-06-02 CA CA000601436A patent/CA1334001C/en not_active Expired - Fee Related
- 1989-06-06 MY MYPI89000762A patent/MY104030A/en unknown
- 1989-06-06 NZ NZ229410A patent/NZ229410A/xx unknown
- 1989-06-07 IL IL90551A patent/IL90551A/xx unknown
- 1989-06-08 ZA ZA894344A patent/ZA894344B/xx unknown
-
1990
- 1990-02-07 DK DK032490A patent/DK32490A/da not_active Application Discontinuation
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2004519506A (ja) * | 2001-01-12 | 2004-07-02 | バクスター・インターナショナル・インコーポレイテッド | エスモロール処方物 |
JP2010024249A (ja) * | 2001-01-12 | 2010-02-04 | Baxter Internatl Inc | エスモロール処方物 |
JP2013151572A (ja) * | 2001-01-12 | 2013-08-08 | Baxter Internatl Inc | エスモロール処方物 |
JP2010528001A (ja) * | 2007-05-22 | 2010-08-19 | バクスター・インターナショナル・インコーポレイテッド | 着色されたエスモロール濃縮物 |
JP2010528025A (ja) * | 2007-05-22 | 2010-08-19 | バクスター・インターナショナル・インコーポレイテッド | ベンジルアルコールとの多用量濃縮エスモロール |
JP2010528000A (ja) * | 2007-05-22 | 2010-08-19 | バクスター・インターナショナル・インコーポレイテッド | 濃縮エスモロール |
JP2011506486A (ja) * | 2007-12-21 | 2011-03-03 | エイオーピー オーファン ファーマスーティカルズ アクチエンゲゼルシャフト | 医薬組成物 |
US10660964B2 (en) | 2007-12-21 | 2020-05-26 | Aop Orphan Pharmaceuticals Ag | Pharmaceutical composition for the parenteral administration of ultrashort-effective beta-adrenoreceptor antagonists |
US11517624B2 (en) | 2007-12-21 | 2022-12-06 | Aop Orphan Pharmaceuticals Gmbh | Pharmaceutical composition for the parenteral administration of ultrashort-effective β-adrenoreceptor antagonists |
JP2013505231A (ja) * | 2009-09-22 | 2013-02-14 | ヴイライフ サイエンシズ テクノロジーズ プライベート リミテッド | 糖尿病性足潰瘍用の局所用製剤 |
Also Published As
Publication number | Publication date |
---|---|
DE68918847D1 (de) | 1994-11-17 |
US4857552A (en) | 1989-08-15 |
DK32490D0 (da) | 1990-02-07 |
EP0403578B1 (en) | 1994-10-12 |
CA1334001C (en) | 1995-01-17 |
EP0403578A1 (en) | 1990-12-27 |
DE68918847T2 (de) | 1995-03-16 |
DK32490A (da) | 1990-02-07 |
AU613196B2 (en) | 1991-07-25 |
EP0403578A4 (en) | 1991-07-03 |
JP2552372B2 (ja) | 1996-11-13 |
AU3570489A (en) | 1990-01-05 |
WO1989011855A1 (en) | 1989-12-14 |
MY104030A (en) | 1993-10-30 |
IL90551A (en) | 1992-12-01 |
ZA894344B (en) | 1991-02-27 |
HU892994D0 (en) | 1990-11-28 |
IL90551A0 (en) | 1990-01-18 |
HUT54041A (en) | 1991-01-28 |
NZ229410A (en) | 1991-10-25 |
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