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    • 15. 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。
    • 18. 发明申请
    • ONDANSETRON ORALLY DISINTEGRATING TABLET COMPOSITIONS FOR PREVENTION OF NAUSEA AND VOMITING
    • ONDANSETRON ORALLYRON OR DISETEGATING TABLET COMPOSITIONS FOR EVEREN NAUSEA AND VOMITING
    • WO2011066289A1
    • 2011-06-03
    • PCT/US2010/057813
    • 2010-11-23
    • EURAND, INC.VENKATESH, Gopi M.
    • VENKATESH, Gopi M.
    • A01N43/50
    • A61K31/4178A61K9/0056A61K9/2077A61K9/2081A61K9/5026A61K9/5031A61K9/5047A61K9/5078
    • This invention is related to a pharmaceutical composition in the patient-friendly orally disintegrating tablet form comprising a weakly basic, selective serotonin 5-HT3 blocking agent for the prevention of nausea and/or vomiting for up to 24 hrs postdosing in cancer patients prior to undergoing moderately emetogenic chemotherapy or partial or whole body radiotherapy or in subjects at moderate to high risk of postoperative or postdischarge nausea and/or vomiting prior to inpatient or outpatient ambulatory surgery. The unit dosage form comprising a multitude of immediate-release drug particles providing dissolution profiles similar to that of reference drug product, and one or more timed, pulsatile-release bead populations, comprising 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.
    • 本发明涉及一种患者友好的口腔崩解片形式的药物组合物,其包含弱碱性选择性5-羟色胺5-HT 3阻断剂,用于预防恶心和/或呕吐在癌症患者之前多达24小时后进行 中度排卵化疗或部分或全身放射治疗或中度至高风险的患者术后或出院后恶心和/或呕吐在住院或门诊门诊手术之前。 所述单位剂量形式包含大量立即释放的药物颗粒,其提供类似于参考药物产品的溶出曲线,以及一个或多个定时的脉冲释放珠粒群,其包含至少一种有机酸,其溶解所述弱碱性选择性5-羟色胺 5-HT3阻断剂在将其释放到敌对肠道环境中之前。