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    • 22. 发明申请
    • MODIFIED DOSAGE FORMS OF TACROLIMUS
    • 改良剂量剂型
    • US20100086592A1
    • 2010-04-08
    • US12530011
    • 2008-03-25
    • Amarjit SinghSarabjit SinghShivanand PuthliRajesh Jain
    • Amarjit SinghSarabjit SinghShivanand PuthliRajesh Jain
    • A61K9/24A61K31/436A61K9/16
    • A61K9/146A61K9/1676A61K9/5078A61K9/5084A61K31/436
    • The present invention provides a modified release dosage form of tacrolimus that releases two or more amount of tacrolimus upon oral administration, the first amount of tacrolimus releases from the immediate release dosage unit substantially immediately within 0-2 hours followed by a time interval ranging from about 1-10 hours during which substantially no amount of tacrolimus is released from the dosage form, after which a second amount of tacrolimus is released wherein said second amount is released from the delayed release dosage unit either immediately e.g. within 0-2 hours or over a period of time ranging from about 2-12 hours from its initial release from the delayed release dosage unit. The dosage form may further comprise additional amount of tacrolimus to provide additional pulse of tacrolimus. The dosage forms of tacrolimus exhibit improved bioavailability and reduced flux or fluctuation over existing composition of tacrolimus. A method of preparing the dosage forms is also described.
    • 本发明提供了他克莫司的释放剂量形式,其口服给药释放两种或更多量的他克莫司,第一批量的他克莫司基本上立即在0-2小时内立即从即时释放剂量单位释放,之后是从约 1-10小时,其中基本上没有量的他克莫司从剂型中释放出来,之后第二量的他克莫司被释放,其中所述第二量从延迟释放剂量单位释放, 在0-2小时内或超过延迟释放剂量单位从其初始释放约2-12小时的时间段内。 剂型还可包含额外量的他克莫司以提供他克莫司的额外脉冲。 他克莫司的剂型表现出改善的生物利用度和减少通量或波动超过现有组合的他克莫司。 还描述了制备剂型的方法。
    • 28. 发明申请
    • Pharmaceutical compositions comprising of proton pump inhibitor and prokinetic agent
    • 包含质子泵抑制剂和促动力剂的药物组合物
    • US20070160664A1
    • 2007-07-12
    • US11482186
    • 2006-07-06
    • Rajesh JainKour JindalSukhjeet Singh
    • Rajesh JainKour JindalSukhjeet Singh
    • A61K31/4439A61K9/64A61K9/24
    • A61K31/4439A61K9/2081A61K9/209A61K9/4808A61K9/5078A61K31/136A61K31/138
    • Oral pharmaceutical compositions and process for preparation thereof are provided comprising at least one gastric acid suppressing agent, preferably a proton pump inhibitor or its pharmaceutically acceptable salts, esters, hydrates, derivatives or prodrugs, and one or more prokinetic agent or its pharmaceutically acceptable salts, esters, hydrates, derivatives or prodrugs, optionally with other pharmaceutically acceptable excipients, characterized in that the gastric acid suppressing agent is present in a delayed release form and the prokinetic agent is present in a bimodal release form such as an immediate release form to provide an initial loading dose, and a delayed release form to provide a dose with a lag time; with the proviso that the prokinetic agent is not formulated using a hydrophilic rate controlling polymer and is not present in a sustained release form. Method of treatment of gastro esophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer, and other gastric acid related disorders by administering to a patient such a pharmaceutical composition in need thereof is also provided.
    • 提供了口服药物组合物及其制备方法,其包含至少一种胃酸抑制剂,优选质子泵抑制剂或其药学上可接受的盐,酯,水合物,衍生物或前药,以及一种或多种促动力剂或其药学上可接受的盐, 酯,水合物,衍生物或前药,任选地与其它药学上可接受的赋形剂,其特征在于所述胃酸抑制剂以延迟释放形式存在,并且促动力剂以双峰释放形式存在,例如立即释放形式,以提供 初始加载剂量和延迟释放形式以提供具有滞后时间的剂量; 条件是促动剂不是使用亲水性速率控制聚合物配制的,并且不以缓释形式存在。 还提供了通过向患者施用这种有此需要的药物组合物来治疗胃食管反流病,反流性食管炎,消化性溃疡,胃溃疡和其它胃酸相关疾病的方法。