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    • 9. 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
    • US20070190145A1
    • 2007-08-16
    • US11668167
    • 2007-01-29
    • Gopi VenkateshJin-Wang LaiNehal Vyas
    • Gopi VenkateshJin-Wang LaiNehal Vyas
    • A61K9/26
    • 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-HT3 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-HT3 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,常规或口腔崩解片剂,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-HT 3阻断剂 约5至14,并且以持续释放的方式在pH 6.8下不超过约200mug / mL的溶解度适合于每日一次的给药方案,其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(即立即释放珠,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。
    • 10. 发明申请
    • Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
    • 口感掩蔽的药物组合物与胃溶性成孔剂
    • US20060105039A1
    • 2006-05-18
    • US11256653
    • 2005-10-21
    • Jin-Wang LaiGopi VenkateshKen Qian
    • Jin-Wang LaiGopi VenkateshKen Qian
    • A61K9/26
    • There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active), coated with a taste-masking membrane comprising a water-insoluble polymer and one or more gastrosoluble inorganic or organic pore-formers (practically insoluble in water and saliva, but soluble in an acidic buffer), exhibit acceptable taste-masking when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.
    • 提供了一种制备包含一种或多种掩味活性药物成分,快速分散微粒和其它任选的药学上可接受的赋形剂的微粒的口腔崩解片(ODT)组合物的方法,其中ODT与 颊腔中的唾液形成平滑,易于吞咽的悬浮液。 此外,涂覆有包含水不溶性聚合物和一种或多种胃溶性无机或有机成孔剂(实际上不溶于水和唾液,但几乎不溶于水和唾液,但是不溶于水)的掩味膜的微粒(晶体,颗粒,含有活性物质的颗粒或颗粒) 可溶于酸性缓冲液),当放置在口腔中时显示出可接受的味道掩蔽,并且在进入胃中提供快速,基本上完全释放的剂量。