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    • 10. 发明申请
    • DRUG DELIVERY SYSTEMS COMPRISING WEAKLY BASIC DRUGS AND ORGANIC ACIDS
    • 包含弱碱性药物和有机酸的药物递送系统
    • WO2007090091A2
    • 2007-08-09
    • PCT/US2007061237
    • 2007-01-29
    • EURAND INCVENKATESH GOPI M
    • VENKATESH GOPI M
    • A61K9/2077A61K9/0056A61K9/5047A61K9/5078A61K9/5084
    • A pharmaceutical dosage form such as a capsule, a conventional or orally disintegrating tablet capable of delivering a nitrogen (N)-containing therapeutic agent having a pKa in the range of from about 5 to 14 into the body in a sustained- released fashion, in order to be suitable for a twice- or once-daily dosing regimen, comprises at least one organic acid, which solubilizes the therapeutic agent the drug prior to releasing it into the hostile intestinal environment wherein said weakly basic drug is practically insoluble. The unit dosage form is composed of a multitude of multicoated particulates (i.e., immediate-release beads, sustained- release beads and/or one or more timed, pulsatile-release bead populations) is designed in such a way that said weakly basic drug and said organic acid do not come into close contact during processing and/or storage for in-situ formation of acid addition compounds while ensuring that the acid is not depleted prior to completion of the drug release.
    • 药物剂型例如胶囊,常规或口腔崩解片剂,其能够以缓释方式将pKa为约5至14的含有氮(N)的治疗剂以持续释放的方式递送至体内, 为了适用于每日两次或每天一次的给药方案,包含至少一种有机酸,其在药物释放到其中所述弱碱性药物实际上不可溶的恶劣肠环境中之前溶解药物的治疗剂。 单位剂型由多种多层颗粒(即,立即释放珠,缓释珠和/或一种或多种定时,脉冲释放珠粒群)组成,使得所述弱碱性药物和 所述有机酸在处理和/或储存过程中不会紧密接触以原位形成酸加成化合物,同时确保酸在药物释放完成之前不被耗尽。