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    • 6. 发明申请
    • DRUG DELIVERY SYSTEMS COMPRISING WEAKLY BASIC SELECTIVE SEROTONIN 5-HT3 BLOCKING AGENT AND ORGANIC ACIDS
    • 包含弱碱性选择性丝氨酸5-HT3阻断剂和有机酸的药物递送系统
    • WO2007090082A3
    • 2007-12-21
    • PCT/US2007061217
    • 2007-01-29
    • EURAND INCVENKATESH GOPI MLAI JIN-WANGVYAS NEHAL H
    • VENKATESH GOPI MLAI JIN-WANGVYAS NEHAL H
    • A61K9/22
    • A61K9/2077A61K9/0056A61K9/5073A61K9/5084A61K31/4178
    • A pharmaceutical dosage form such as a capsule, a conventional or orally disintegrating tablet capable of delivering a weakly basic, nitrogen (N)-containing selective serotonin 5- HT 3 blocking agent having a pKa in the range of from about 5 to 14 and a solubility of not more than about 200 µg/mL at pH 6.8 into the body in a sustained-released fashion, suitable for a once-daily dosing regimen, comprises at least one organic acid, which solubilizes said weakly basic selective serotonin 5-HT 3 blocking agent prior to releasing it into the hostile intestinal environment wherein the blocking agent is practically insoluble. The unit dosage form may be 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) and is designed in such a way that the weakly basic blocking agent and the organic acid do not come into close contact during processing and/or storage thereby avoiding in-situ formation of acid addition compounds while ensuring that the acid is not depleted prior to completion of the drug release.
    • 一种药物剂型,例如胶囊,常规或口腔崩解片,其能够递送具有pKa范围的弱碱性,含氮(N)的选择性5-羟色胺5-羟色胺阻断剂 约5至14,并且以pH 6.8的不超过约200μg/ mL的溶解度以持续释放的方式适应于每日一次的给药方案,包含至少一种有机酸,其溶解所述弱化 碱性选择性5-羟色胺5-HT 3封闭剂,然后将其释放到敌对的肠道环境中,其中封闭剂几乎不溶。 单位剂量形式可以由多种多重微粒(即即释丸,缓释珠和/或一个或多个定时,脉冲释放珠群)组成,并且以这样的方式设计:弱碱性 封闭剂和有机酸在加工和/或储存期间不会紧密接触,从而避免了原位形成酸加成化合物,同时确保在药物释放完成之前酸不被耗尽。