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1. 发明申请

WO1999036030A2 PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING DI-HYDROXYTESTOSTERONE DEPENDENT CONDITIONS 审中-公开
标题翻译：药物组合物和治疗二羟基睾酮依赖性病症的方法
公开(公告)号：WO1999036030A2
公开(公告)日：1999-07-22
申请号：PCT/US1999001207
申请日：1999-01-19
申请人： DAVITZ, Michael, A. , LEASON, David , FOITL, Daniel
发明人： DAVITZ, Michael, A. , LEASON, David
IPC分类号： A61K00/00
CPC分类号： A61K9/5084 , A61K31/585 , A61K31/58 , A61K2300/00
摘要： A pharmaceutical composition for treating DHT dependent conditions including androgenic alopecia is disclosed. An oral dosage form according to the invention includes a therapeutically effective amount of a 5 alpha -Reductase inhibitor and another active compound which binds with androgenic receptors. In a preferred form, the bio-available concentration of the compound which binds with androgenic receptors is limited or controlled to avoid appreciable anti-androgenic side effects, for example, by providing a controlled (timed or sustained release) coating on that active compound. Spironolactone is a particularly preferred compound which binds with androgenic receptors. A preferred dosage form has the ratio of the 5 alpha -Reductase inhibitor to spironolactone in the range of 1:5 to 1:2500. A method for creating an oral dosage form for treating DHT dependent conditions is also disclosed.
摘要翻译：本发明涉及用于治疗依赖于包括雄激素性脱发在内的DHT的病理状态的药物组合物。口服剂量的组合物包含足够治疗量的α-还原酶抑制剂和另一种与雄激素受体结合的活性化合物。在一个优选的实施方案中，限制或控制雄激素受体结合化合物的生物可利用浓度，以避免显着的二次抗雄激素效应，例如通过提供对照层（延迟释放或延长释放）在所述活性化合物上。螺内酯是特别优选的与雄激素受体结合的化合物。优选的剂型包含α与螺内酯还原酶抑制剂的比例为1：5至1.2500。本发明还涉及产生用于治疗依赖于DHT的病理状况的口服剂量的方法。

2. 发明申请

WO9936030A3 PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING DI-HYDROXYTESTOSTERONE DEPENDENT CONDITIONS 审中-公开
标题翻译：药物组合物和治疗依赖羟化甾体的条件的方法
公开(公告)号：WO9936030A3
公开(公告)日：1999-09-23
申请号：PCT/US9901207
申请日：1999-01-19
申请人： DAVITZ MICHAEL A , LEASON DAVID , FOITL DANIEL
发明人： FOITL DANIEL
IPC分类号： A61K9/50 , A61K31/585 , A61K31/56
CPC分类号： A61K9/5084 , A61K31/585 , A61K31/58 , A61K2300/00
摘要： A pharmaceutical composition for treating DHT dependent conditions including androgenic alopecia is disclosed. An oral dosage form according to the invention includes a therapeutically effective amount of a 5 alpha -Reductase inhibitor and another active compound which binds with androgenic receptors. In a preferred form, the bio-available concentration of the compound which binds with androgenic receptors is limited or controlled to avoid appreciable anti-androgenic side effects, for example, by providing a controlled (timed or sustained release) coating on that active compound. Spironolactone is a particularly preferred compound which binds with androgenic receptors. A preferred dosage form has the ratio of the 5 alpha -Reductase inhibitor to spironolactone in the range of 1:5 to 1:2500. A method for creating an oral dosage form for treating DHT dependent conditions is also disclosed.
摘要翻译：公开了用于治疗DHT依赖性病症（包括雄激素性脱发）的药物组合物。根据本发明的口服剂型包括治疗有效量的5α-转导酶抑制剂和与雄激素受体结合的另一种活性化合物。在优选形式中，与雄激素受体结合的化合物的生物可用浓度受到限制或控制，以避免明显的抗雄激素副作用，例如通过在该活性化合物上提供受控（定时或持续释放）的涂层。螺内酯是与雄激素受体结合的特别优选的化合物。优选的剂型是5α-转导酶抑制剂与螺内酯的比例为1:5至1:255。还公开了一种用于产生用于治疗DHT依赖性病症的口服剂型的方法。

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