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1. 发明授权

US4499066A Pharmaceutical sustained-release compositions 失效
标题翻译：药物缓释组合物
公开(公告)号：US4499066A
公开(公告)日：1985-02-12
申请号：US403475
申请日：1982-07-30
申请人： Luigi Moro , Grazia Maffione , Guido Neri , Alessandro Rigamonti
发明人： Luigi Moro , Grazia Maffione , Guido Neri , Alessandro Rigamonti
IPC分类号： A61K47/32 , A61K9/20 , A61K9/22 , A61K9/26 , A61K9/54 , A61K9/58 , A61K47/30 , A61K9/32
CPC分类号： A61K9/2027
摘要： New pharmaceutical sustained-release compositions, formulated as tablets, are prepared by mixing the active ingredient with excipient already granulated and coated with polymers and/or copolymers or a polymers- and/or copolymers-mixture substantially insoluble in water. Such pharmaceutical preparations enable one to enhance or to decrease very easily and precisely the sustained-release effect by regulating the granulometry of the excipient, the excipient/active ingredient ratio, the hardness, and the percentage of the polymers and/or copolymers or of the polymers- and/or copolymers-mixture.
摘要翻译：配制成片剂的新型药物缓释组合物通过将活性成分与已经造粒并用聚合物和/或共聚物或基本上不溶于水的聚合物 - 和/或共聚物混合物的赋形剂混合来制备。这样的药物制剂使得能够通过调节赋形剂的粒度，赋形剂/活性成分比，硬度和聚合物和/或共聚物的百分比或者聚合物和/或共聚物混合物。

2. 发明授权

US4746516A Pharmaceutical compositions consisting or consisting essentially of freeze-dried drug-carrying liposomes 失效
标题翻译：由冷冻干燥的携带药物的脂质体组成或基本组成的药物组合物
公开(公告)号：US4746516A
公开(公告)日：1988-05-24
申请号：US921856
申请日：1986-10-22
申请人： Luigi Moro , Guido Neri , Alessandro Rigamonti
发明人： Luigi Moro , Guido Neri , Alessandro Rigamonti
IPC分类号： A61K9/127 , A61K9/10 , A61K31/70 , A61K31/74
CPC分类号： A61K9/1277
摘要： A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins. Treatment may also be carried out with polymers, copolymers, or mixtures thereof, not having any specific chemical function and which normally, but not exclusively, react according to Van der Waals' forces, commonly known as adsorbents. The invention also includes freeze-dried pharmaceutical compositions consisting or consisting essentially of lyophilic liposomes of drugs, such as doxorubicin hydrochloride, aminosidine sulphate or 5-fluoro-uracil. The pharmaceutical compositions are characterized by a high degree of stability.
摘要翻译：公开了一种用于从非包埋药物中纯化非均匀系统（称为脂质体悬浮液）的方法，其中所述悬浮液用作为离子交换剂的化学官能团的具有合成和有机性质的液体或固体聚合物处理。液体或固体聚合物基于苯乙烯，二乙烯基苯，丙烯酸，甲基丙烯酸等，通常称为离子交换树脂，并且可以包括不同基质的羧酸，膦酸或磺酸的功能。离子交换树脂还可以包括成盐季铵，一级，二级和叔级氨基或次膦酸功能或具有不同基质的其它功能，包括苯酚 - 二甲苯基苯，丙烯酸酯，甲基丙烯酸酯，烃和缩合树脂。处理也可以用不具有任何特定化学功能的聚合物，共聚物或其混合物进行，通常但不排他地根据范德华力（通常称为吸附剂）进行反应。本发明还包括冷冻干燥的药物组合物，其基本上由药物的亲脂性脂质体组成或组成，例如盐酸多柔比星，硫酸氨基西丹或5-氟尿嘧啶。药物组合物的特征在于高度的稳定性。

3. 发明授权

US4460577A Pharmaceutical compositions consisting or consisting essentially of liposomes, and processes for making same 失效
标题翻译：由脂质体组成或组成的药物组合物及其制备方法
公开(公告)号：US4460577A
公开(公告)日：1984-07-17
申请号：US111837
申请日：1980-01-14
申请人： Luigi Moro , Guido Neri , Alessandro Rigamonti
发明人： Luigi Moro , Guido Neri , Alessandro Rigamonti
IPC分类号： A61K9/127 , A61K31/70 , A61K31/505 , A61K31/74
CPC分类号： A61K9/1277
摘要： A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic, or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins. Treatment may also be carried out with polymers, copolymers, or mixtures thereof, not having any specific chemical function and which normally, but not exclusively, react according to Van der Waals' forces, commonly known as adsorbents. The invention also includes pharmaceutical compositions consisting or consisting essentially of lyophilic liposomes of doxorubicin hydrochloride, aminosidine sulphate or 5-fluoro-uracil.
摘要翻译：公开了一种用于从非包埋药物中纯化非均匀系统（称为脂质体悬浮液）的方法，其中所述悬浮液用作为离子交换剂的化学官能团的具有合成和有机性质的液体或固体聚合物处理。液体或固体聚合物基于通常称为离子交换树脂的苯乙烯，二乙烯基苯，丙烯酸，甲基丙烯酸等，并且可以包括不同基质的羧酸，膦酸或磺酸的功能。离子交换树脂还可以包括成盐季铵，一级，二级和叔级氨基或次膦酸功能或具有不同基质的其它功能，包括苯酚 - 二甲苯基苯，丙烯酸酯，甲基丙烯酸酯，烃和缩合树脂。处理也可以用不具有任何特定化学功能的聚合物，共聚物或其混合物进行，通常但不排他地根据范德华力（通常称为吸附剂）进行反应。本发明还包括由盐酸多柔比星，硫酸氨基西丹或5-氟尿嘧啶的亲液脂质体组成或组成的药物组合物。

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