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1. 发明申请

WO0130337A3 OPHTHALMIC FORMULATION OF DOPAMINE ANTAGONISTS 审中-公开
标题翻译：多巴胺拮抗剂的眼用配方
公开(公告)号：WO0130337A3
公开(公告)日：2002-01-24
申请号：PCT/US0041491
申请日：2000-10-23
申请人： ORBON CORP
发明人： CHIOU GEORGE C Y
IPC分类号： A61K9/00 , A61K31/00 , A61K47/12
CPC分类号： A61K31/00 , A61K9/0048
摘要： This invention provides ocular formulations comprising an ocular drug and a carboxylic acid in an amount sufficient to maintain the pH of the formulation from about 4.5 to about 7.5. The ocular drug may be a dopamine antagonist and the acid may be lactic acid, citric acid or tartaric acid. In some aspects, the pH of the formulation is about 5.5. The ocular formulations of this invention provide enhanced bioavailability which results in increased drug concentrations across the cornea and in the eye ball, i.e., aqueous humor and intraocular organs and chambers. Moreover, the present formulations are non-irritating when applied topically and have a shelf-life of at least fourteen days at 25 DEG C. Methods are also provided to increase ocular blood flow by using present ocular formulations comprising dopamine antagonists or other drugs for the prevention and treatment of ocular hypertension, glaucoma, ischemic retinopathy and age-related macular degeneration (AMD).
摘要翻译：本发明提供包含足以将制剂的pH保持在约4.5至约7.5的量的眼药物和羧酸的眼用制剂。眼药可以是多巴胺拮抗剂，酸可以是乳酸，柠檬酸或酒石酸。在一些方面，制剂的pH为约5.5。本发明的眼用制剂提供增强的生物利用度，其导致跨越角膜和眼球，即房水和眼内器官和室的药物浓度增加。此外，本发明的制剂在局部施用时是无刺激性的，并且在25℃下具有至少14天的保质期。还提供了方法以通过使用包含多巴胺拮抗剂或其它药物的目前的眼用制剂来增加眼部血流量预防和治疗高眼压症，青光眼，缺血性视网膜病变和年龄相关性黄斑变性（AMD）。

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