CN101616668A - 新的药用组合物 - Google Patents
新的药用组合物 Download PDFInfo
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- CN101616668A CN101616668A CN200880001668A CN200880001668A CN101616668A CN 101616668 A CN101616668 A CN 101616668A CN 200880001668 A CN200880001668 A CN 200880001668A CN 200880001668 A CN200880001668 A CN 200880001668A CN 101616668 A CN101616668 A CN 101616668A
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
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Abstract
Description
Claims (12)
- 权利要求1、 一种药用组合物, 含有药理活性成分 2-丁基 -4-氯 -1-[2'-(1 H -四唑 -5-基) 1,1'-联苯 基-甲基]咪唑 -5-羧酸, 1- [(异丙氧基)羰氧基]甲基酯和药学上可接受的载体材料。
- 2、如权利要求 1所述的药用组合物, 其特征在于, 所述药理活性成分在组合物中的 重量百分比为 1%~50%。
- 3、 如权利要求 2所述的药用组合物, 其特征在于, 所述载体材料包括填充剂、 崩解 剂、 润湿剂、 粘合剂、 润滑剂、 表面活性剂、 助流剂、 矫味剂、 矫嗅剂和着色剂中一种 或几种。
- 4、如权利要求 3所述的药用组合物, 其特征在于, 所述填充剂选自以下物质一种或 几种的组合: 碳酸钙、 碳酸镁、 磷酸钙、 硫酸钙、 氧化镁、 羧甲基纤维素钙、 羧甲基纤 维素钠、 蔗糖、 乳糖、 果糖、 木糖醇、 甘露醇、 淀粉或其衍生物、 糊精和微晶纤维素; 崩解剂可选自以下物质一种或几种的组合: 淀粉、 藻酸、 羧甲基纤维素钙、 羧甲基纤维 素钠、 交联羧甲基纤维素钠、 交联聚乙烯吡咯烷酮、 低取代羟丙基甲基纤维素、 微晶纤 维素和甲基纤维素; 润湿剂可选自以下物质一种或几种的组合: 蒸馏水、 乙醇和淀粉浆; 粘合剂可选自以下物质一种或几种的组合: 阿拉伯胶、 明胶、 黄蓍胶、 糊精、 聚乙烯吡 咯烷酮、 淀粉及其衍生物、 藻酸钠、 山梨醇、 糖浆、 羟丙基甲基纤维素、 甲基纤维素、 羟丙基纤维素、 羟乙基纤维素、 乙基纤维素、 羧甲基纤维素钠、 羧甲基纤维素钙、 葡萄 糖和聚甲基丙烯酸酯; 润滑剂可选自以下物质一种或几种的组合: 硬脂酸钙、 单硬脂酸 甘油酯、 棕榈硬脂酸甘油酯、 硬脂酸镁、 微晶纤维素、 苯甲酸钠、 氯化钠、 十二烷基硫 酸钠、 硬脂酸镁、 硬脂基富马酸钠、 滑石粉、 硬脂酸锌和聚乙二醇; 表面活性剂可选自 以下物质一种或几种的组合: 十二烷基硫酸钠、 泊洛沙姆、 吐温类、 溴化十六垸三甲胺、 月桂醇硫酸钠、 硬脂醇磺酸钠、 聚氧乙烯高级脂肪醇、 蔗糖酯、 山梨醇脂肪酯和大豆磷 脂; 助流剂可选自以下物质一种或几种的组合: '胶体二氧化硅、粉状纤维素、三硅酸镁、 二氧化硅和滑石粉。
- 5、如权利要求 3所述的药用组合物,其特征在于,所述载体材料进一步包括泡腾剂, 所述泡腾剂选自碳酸氢钠、 磷酸盐、 有机酸类和有机酸酐类。
- 6、 如权利要求 1至 5任一所述的药用组合物, 其特征在于, 所述载体材料进一步包 含增溶载体, 药理活性成分分散在增溶载体中, 所述增溶载体选自聚乙二醇类、 聚维酮 类、 含有聚氧乙烯基的表面活性剂、 水溶性纤维素衍生物、 有机酸和糖类、 固醇类和脂 类物质中之一种或几种。
- 7、如权利要求 6所述的药用组合物, 其特征在于, 所述增溶载体材料选自聚乙二醇 类、 聚维酮类、 含有聚氧乙烯基的表面活性剂和水溶性纤维素衍生物中之一种或几种。
- 8、如权利要求 7所述的药用组合物, 其特征在于, 药理活性成分与增溶载体的重量 比例为 1:1 1:100。
- 9、包含如权利要求 1至 8任一所述的药用组合物的制剂, 含有药理活性成分的重量 为 5mg~180mg。10、 如权利要求 9所述的制剂, 其特征在于, 所述制剂含有的药理活性成分选自如 下重量: 5mg, 10mg, 20mg, 30mg, 40mg, 50mg, 60mg, 70mg, 80mg, 90mg, lOOmg, 120mg, 140mg, 160mg和 180mg。
- 11、 如权利要求 9所述的制剂, 其特征在于, 其形式为散剂、 颗粒剂、 微丸、 片剂、 胶囊剂、 滴丸剂或锭剂。
- 12、 如权利要求 1至 8任一所述的组合物用于制备心血管药物的用途。
- 13、 如权利要求 1至 8任一所述的组合物用于制备降血压药物的用途。14、 一种治疗人类心血管疾病的方法, 包括给患者施以含有有效剂量 2-丁基 -4-氯 小 [2'-(1 H -四唑 -5-基) 1,1'-联苯基-甲基]咪唑 -5-羧酸, H (异丙氧基)羰氧基]甲基酯的如权 利要求 9至 11任一所述的制剂。15、 一种治疗人类高血压疾病的方法, 包括给高血压患者施以含有有效剂量 2-丁基 -4-氯小 [2'-(1 H -四唑 -5-基) Ι,Γ-联苯基-甲基]咪唑 -5-羧酸, 1- [(异丙氧基)羰氧基]甲基酯的 如权利要求 9至 11任一所述的制剂。16、如权利要求 15所述的治疗人类高血压疾病的方法, 包括给高血压患者施以含有 有效剂量 2-丁基 -4-氯 -1-[2'-(1 Η -四唑 -5-基) Ι,Γ-联苯基-甲基]咪唑 -5-羧酸, 1- [(异丙氧基) 羰氧基]甲基酯的如权利要求 9至 11任一所述的制剂, 和其他的降压药物, 其他降压药 物选自利尿剂、 血管紧张素转换酶抑制剂、 钙离子拮抗剂中之一种或多种。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CN2008800016680A CN101616668B (zh) | 2007-01-05 | 2008-01-07 | 药用组合物 |
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CN200710036237.5 | 2007-01-05 | ||
CNA2007100362375A CN101214242A (zh) | 2007-01-05 | 2007-01-05 | 新的药用组合物 |
PCT/CN2008/000048 WO2008086733A1 (fr) | 2007-01-05 | 2008-01-07 | Nouvelle composition pharmaceutique |
CN2008800016680A CN101616668B (zh) | 2007-01-05 | 2008-01-07 | 药用组合物 |
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CN101616668A true CN101616668A (zh) | 2009-12-30 |
CN101616668B CN101616668B (zh) | 2013-01-09 |
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CNA2007100362375A Pending CN101214242A (zh) | 2007-01-05 | 2007-01-05 | 新的药用组合物 |
CN2008800016680A Active CN101616668B (zh) | 2007-01-05 | 2008-01-07 | 药用组合物 |
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US (1) | US8138214B2 (zh) |
EP (1) | EP2116242B1 (zh) |
JP (1) | JP5295123B2 (zh) |
CN (2) | CN101214242A (zh) |
WO (1) | WO2008086733A1 (zh) |
Families Citing this family (14)
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CN101024643A (zh) | 2006-02-20 | 2007-08-29 | 上海艾力斯医药科技有限公司 | 咪唑-5-羧酸类衍生物、制备方法及其应用 |
CN101317842A (zh) | 2007-06-07 | 2008-12-10 | 上海艾力斯医药科技有限公司 | 一种咪唑-5-羧酸衍生物的治疗用途 |
US9205577B2 (en) * | 2010-02-05 | 2015-12-08 | Allergan, Inc. | Porogen compositions, methods of making and uses |
US9138309B2 (en) | 2010-02-05 | 2015-09-22 | Allergan, Inc. | Porous materials, methods of making and uses |
US11202853B2 (en) * | 2010-05-11 | 2021-12-21 | Allergan, Inc. | Porogen compositions, methods of making and uses |
CN103263395A (zh) * | 2013-06-10 | 2013-08-28 | 南京正宽医药科技有限公司 | 一种替米沙坦片剂及其制备方法 |
CN104610232B (zh) | 2013-11-01 | 2019-09-20 | 深圳信立泰药业股份有限公司 | 阿利沙坦酯无定形及其制备方法及含所述无定形的药物组合物 |
CN105078974A (zh) * | 2014-05-23 | 2015-11-25 | 深圳信立泰药业股份有限公司 | 一种阿利沙坦酯固体分散体及药物组合物 |
CN105232489B (zh) * | 2014-07-01 | 2019-06-11 | 深圳信立泰药业股份有限公司 | 一种阿利沙坦酯固体分散体及含有该固体分散体的药物组合物 |
CN106539690B (zh) * | 2015-09-18 | 2020-08-04 | 天士力医药集团股份有限公司 | 一种液体冷却滴丸的连续智能制备方法 |
US20180168932A1 (en) * | 2016-12-20 | 2018-06-21 | Apotex Technologies Inc. | Meloxicam Dosage Forms |
CN112245396B (zh) * | 2020-09-28 | 2022-11-15 | 北京华氏开元医药科技有限公司 | 四氢异喹啉类衍生物药物制剂及其制备方法 |
US11655240B1 (en) | 2022-05-10 | 2023-05-23 | Beijing Grand Johamu Pharmaceutical Company, Ltd. | Crystal form of compound and fumaric acid, pharmaceutical composition and method for treating coronavirus-induced diseases |
CN117159555A (zh) * | 2022-05-27 | 2023-12-05 | 北京远大九和药业有限公司 | 药物组合物及其制备方法和用途 |
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CA1334092C (en) | 1986-07-11 | 1995-01-24 | David John Carini | Angiotensin ii receptor blocking imidazoles |
US5196444A (en) | 1990-04-27 | 1993-03-23 | Takeda Chemical Industries, Ltd. | 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and compositions and methods of pharmaceutical use thereof |
US5616599A (en) | 1991-02-21 | 1997-04-01 | Sankyo Company, Limited | Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their therapeutic use |
AT398202B (de) * | 1991-10-04 | 1994-10-25 | Chem Pharm Forsch Gmbh | Neue imidazolderivate, verfahren zu ihrer herstellung und ihre verwendung |
JPH083162A (ja) * | 1994-04-19 | 1996-01-09 | Tanabe Seiyaku Co Ltd | イミダゾピリジン誘導体及びその製法 |
US5990134A (en) * | 1998-08-12 | 1999-11-23 | Taylor Pharmaceuticals | Oral droperidol compositions and method for treating migraine |
US20060276523A1 (en) * | 2003-07-31 | 2006-12-07 | Nicoletta Almirante | Nitoroxy derivatives of losartan, valsatan, candesartan, telmisartan, eprosartan and olmesartan as angiotensin-II receptor blockers for the treatment of cardiovascular diseases |
CN101024643A (zh) | 2006-02-20 | 2007-08-29 | 上海艾力斯医药科技有限公司 | 咪唑-5-羧酸类衍生物、制备方法及其应用 |
JP5290190B2 (ja) * | 2006-12-06 | 2013-09-18 | サルブリス・アセット・マネイジメント・カンパニー・リミテッド | イミダゾール−5−カルボン酸誘導体の塩、製造方法及びその医薬組成物 |
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- 2007-01-05 CN CNA2007100362375A patent/CN101214242A/zh active Pending
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- 2008-01-07 JP JP2009544355A patent/JP5295123B2/ja active Active
- 2008-01-07 CN CN2008800016680A patent/CN101616668B/zh active Active
- 2008-01-07 EP EP08700608.6A patent/EP2116242B1/en active Active
- 2008-01-07 WO PCT/CN2008/000048 patent/WO2008086733A1/zh active Application Filing
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Also Published As
Publication number | Publication date |
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JP5295123B2 (ja) | 2013-09-18 |
EP2116242B1 (en) | 2016-10-12 |
CN101616668B (zh) | 2013-01-09 |
US8138214B2 (en) | 2012-03-20 |
EP2116242A4 (en) | 2013-02-13 |
CN101214242A (zh) | 2008-07-09 |
JP2010514813A (ja) | 2010-05-06 |
US20090326025A1 (en) | 2009-12-31 |
WO2008086733A1 (fr) | 2008-07-24 |
EP2116242A1 (en) | 2009-11-11 |
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