JP2000503655A - 医薬組成物 - Google Patents
医薬組成物Info
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- JP2000503655A JP2000503655A JP9525704A JP52570497A JP2000503655A JP 2000503655 A JP2000503655 A JP 2000503655A JP 9525704 A JP9525704 A JP 9525704A JP 52570497 A JP52570497 A JP 52570497A JP 2000503655 A JP2000503655 A JP 2000503655A
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- 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
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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- A61K9/0048—Eye, e.g. artificial tears
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- 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
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.有効成分としてサイクロスポリン、ラパマイシンまたはアスコマイシンま たはその誘導体を含有するエマルション組成物の調製法であって、かかる方法は 、 a)有効成分 b)リン脂質、糖脂質、スフィンゴ脂質、ジアシルホスファチジルグリセロール 、卵−ホスファチジルグリセロール、大豆−ホスファチジルグリセロール、ジア シル−ホスファチジルグリセロール、またはその塩;または飽和、モノ−または ジ−不飽和(C12-24)脂肪酸またはその塩から選択される安定化剤、および c)有機溶媒 (ただし、有効成分と安定化剤との重量比は400:1ないし0.5:1である ) を含有する濃縮液をプラセボ脂肪エマルションに混合する段階を含む。 2.有機溶媒がエタノールおよびプロピレングリコールを含むものである請求 項1に記載の方法。 3.安定化剤がオレイン酸ナトリウムまたはNaPOPGである請求項1また は請求項2に記載の方法。 4.有効成分であるサイクロスポリン、ラパマイシンまたはアスコマイシンま たはその誘導体の既使用型脂肪エマルション中の濃度を、プラセボ脂肪エマルシ ョン中の濃度よりも増加させ、および/または既使用型エマルションの形成を促 進する、請求項1または請求項3に記載の安定化剤の使用。 5.a)プラセボ脂肪エマルション、および b)安定化剤であるオレイン酸ナトリウムまたはNaPOPGを含む有効成分の 有機溶媒溶液 (ただし、有効成分と安定化剤の重量比は400:1〜10:1である) を含有する、有効成分[3'−デソキシ−3−オキソ−MeBmt]1−[Val]2−シクロ スポリンの静脈内投与用エマルション。 6.有機溶媒がエタノールおよび/またはプロピレングリコールを含むもので ある請求項5に記載のエマルション。 7.有効成分[3'−デソキシ−3−オキソ−MeBmt]1−[Val]2−シクロスポリ ンの静脈内投与用エマルションの調製法であって、かかる工程は、 a)有効成分および b)安定化剤であるオレイン酸ナトリウムまたはNaPOPG c)有機溶媒 (ただし、有効成分と安定化剤の重量比は400:1〜10:1である) を含有する濃縮液をプラセボ脂肪エマルションに混合する段階を含む。 8.有機溶媒がエタノールおよび/またはプロピレングリコールを含むもので ある請求項7に記載の方法。 9.既使用型エマルションを形成するために、医薬的に安全な粒子サイズの有 効成分の必要量に関して患者の要求に合致する割合に内容物を混合するのに適当 な、請求項1に記載の濃縮液が入るアンプルおよびプラセボ脂肪エマルションが 入るビン組合せ。 10.実施例のいずれか1つに関して本明細書に実質的に前記した方法、濃縮 液またはエマルション。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9601120.0 | 1996-01-19 | ||
GBGB9601120.0A GB9601120D0 (en) | 1996-01-19 | 1996-01-19 | Organic compounds |
PCT/EP1997/000252 WO1997025977A1 (en) | 1996-01-19 | 1997-01-20 | Pharmaceutical compositions |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2003337458A Division JP4077386B2 (ja) | 1996-01-19 | 2003-09-29 | 医薬組成物 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2000503655A true JP2000503655A (ja) | 2000-03-28 |
JP3763581B2 JP3763581B2 (ja) | 2006-04-05 |
JP3763581B6 JP3763581B6 (ja) | 2007-12-12 |
Family
ID=
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2005529851A (ja) * | 2002-03-04 | 2005-10-06 | ノバルティス アクチエンゲゼルシャフト | アスコマイシンを含む眼用組成物 |
JP2006522007A (ja) * | 2002-11-15 | 2006-09-28 | ノバルティス アクチエンゲゼルシャフト | ドラッグ・デリバリー・システム |
JP2010047601A (ja) * | 2000-10-31 | 2010-03-04 | Pharma Mar Sa | カハラリドf |
JP2010515062A (ja) * | 2006-12-29 | 2010-05-06 | アボット・ラボラトリーズ | 非変性細胞溶解試薬 |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2010047601A (ja) * | 2000-10-31 | 2010-03-04 | Pharma Mar Sa | カハラリドf |
JP2005529851A (ja) * | 2002-03-04 | 2005-10-06 | ノバルティス アクチエンゲゼルシャフト | アスコマイシンを含む眼用組成物 |
JP4740542B2 (ja) * | 2002-03-04 | 2011-08-03 | ノバルティス アーゲー | アスコマイシンを含む眼用組成物 |
JP2006522007A (ja) * | 2002-11-15 | 2006-09-28 | ノバルティス アクチエンゲゼルシャフト | ドラッグ・デリバリー・システム |
JP2010515062A (ja) * | 2006-12-29 | 2010-05-06 | アボット・ラボラトリーズ | 非変性細胞溶解試薬 |
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