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    • 6. 发明授权
    • Chronotherapeutic diltiazem formulations and the administration thereof
    • 计时治疗性地尔硫卓制剂及其施用
    • US07348028B2
    • 2008-03-25
    • US10657752
    • 2003-09-09
    • Kenneth Stephen AlbertTheophilus Jones GanaPaul Maes
    • Kenneth Stephen AlbertTheophilus Jones GanaPaul Maes
    • A61K9/14A61K9/16A61K9/20A61K9/22
    • A61K31/55A61K9/2081A61K9/4866A61K9/5031A61K9/5047
    • A method of treating or preventing myocardial ischemia in a patient in need thereof comprising administration of a controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 180 mg to about 420 mg of the form of Diltiazem associated with excipients to provide controlled (sustained) release of the form of Diltiazem for providing a Cmax of Diltiazem in the blood at between about 10 hours and about 17 hours after administration, the preparation comprising the form of Diltiazem in oral sustained-release dosage form in which the Diltiazem is adapted to be released after administration over a prolonged period of time and exhibits when given to humans(i) a higher bioavailability when given at night compared to when given in the morning without food according to FDA guidelines or criteria and(ii) bioequivalence when given in the morning with and without food according to the same FDA guidelines or criteria.
    • 一种在有需要的患者中治疗或预防心肌缺血的方法,包括施用药学上可接受的地尔硫卓的可释放的Galenical制剂,包括其药学上可接受的盐,适合于每24小时进行晚间给药,其含有约180mg至约420mg 与给药相关的地尔硫卓形式,以提供受控(持续)释放的地尔硫卓形式,用于在给药后约10小时至约17小时之间在血液中提供地尔硫卓的最大值, 包含地尔硫卓口服持续释放剂型形式的制剂,其中地尔硫卓适于在长时间给药后释放,并在给予人时显示(i)与给予时相比较,在晚上给予时具有较高的生物利用度 在早晨没有食物根据FDA指导方针或标准,和(ii)生物等效性在早晨w给予 根据相同的FDA指南或标准,不含食物。
    • 8. 发明申请
    • Modified release formulations of at least one form of tramadol
    • 至少一种曲马多的缓释制剂
    • US20050182056A9
    • 2005-08-18
    • US10434266
    • 2003-05-09
    • Seth PawanPaul Maes
    • Seth PawanPaul Maes
    • A61K9/22A61K9/28A61K31/137A61K31/535A61K9/20
    • A61K9/2866A61K9/284A61K31/137
    • The present invention provides for a modified release pharmaceutical composition comprising at least one form of tramadol selected from the group consisting of tramadol, enantiomers thereof, pharmaceutically acceptable salts thereof and combinations thereof, the composition exhibiting an in vitro dissolution profile (measured using the USP Basket Method at 75 rpm in 900 ml 0.1 N HCl at 37° C.) such that after 2 hours, from about 0% up to about 30% (by weight) of the at least one form of tramadol is released, after 4 hours, from about 5% to about 22% (by weight) of the at least one form of tramadol is released, after 6 hours, from about 15% to about 38% (by weight) of the at least one form of tramadol is released, after 8 hours, more than about 40% (by weight) of the at least one form of tramadol is released.
    • 本发明提供一种包含至少一种形式的曲马多的改性释放药物组合物,其选自曲马多,其对映异构体,其药学上可接受的盐及其组合,所述组合物显示体外溶出曲线(使用USP Basket 方法在75rpm,在900ml 0.1N HCl中于37℃下进行),使得在2小时后,释放至少一种形式的曲马多的约0%至约30%(重量),4小时后, 释放约5%至约22%(重量)的该曲马多的至少一种形式的曲马朵,6小时后,至少一种曲马多的约15%至约38%(重量)被释放, 8小时后,释放至少一种形式的曲马多的大于约40%(重量)。