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    • 8. 发明申请
    • EXTENDED RELEASE COMPOSITIONS COMPRISING MYCOPHENOLATE SODIUM AND PROCESSES THEREOF
    • 包含MYCOPHENOLATE SODIUM的扩展性释放组合物及其过程
    • US20110223249A1
    • 2011-09-15
    • US12672180
    • 2008-08-11
    • Rajesh JainSukhjeet SinghSampath Kumar Devarajan
    • Rajesh JainSukhjeet SinghSampath Kumar Devarajan
    • A61K31/343A61K9/00A61K9/24A61K9/28A61P35/00A61P11/00A61P25/00A61P9/00A61P29/00A61P31/00
    • A61K9/2077A61K9/2013A61K9/2846A61K31/365
    • Extended release pharmaceutical compositions comprising mycophenolate sodium as the active agent, wherein the said composition exhibits a characteristic release profile when subjected to in-vitro dissolution study, and wherein said mycophenolate sodium is released in a sustained manner in-vivo for a prolonged duration in such quantities that substantially alleviates or at least reduces the chances of causing any associated gastrointestinal side effect(s) without compromising the bioavailability of the said active agent are provided. The present invention also provides process of preparing dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The compositions of the present invention are useful for the management such as prophylaxis, amelioration and/or treatment of immunosuppressant indicated disease(s)/disorder(s) especially for the treatment or prevention of organ, tissue or cellular allograft or xenograft rejection, e.g. after transplant, or the management of immune-mediated diseases (autoimmune diseases).
    • 包含霉酚酸钠作为活性剂的延长释放药物组合物,其中当进行体外溶出研究时,所述组合物表现出特征性释放曲线,并且其中所述霉酚酸钠以持续的方式在体内以这种方式长时间释放 提供了大大减轻或至少降低引起任何相关胃肠道副作用而不损害所述活性剂的生物利用度的机会的量。 本发明还提供了使用这种剂型的剂型组合物和预防和/或治疗方法的制备方法。 本发明的组合物可用于治疗,例如预防,改善和/或治疗指示的疾病/病症,特别是用于治疗或预防器官,组织或细胞同种异体移植物或异种移植物排斥反应的免疫抑制剂,例如, 移植后,或免疫介导的疾病(自身免疫性疾病)的管理。
    • 10. 发明申请
    • Novel Pharmaceutical Modified Release Dosage Form Cyclooxygenase Enzyme Inhibitor
    • 新型药物改性释放剂型环氧合酶抑制剂
    • US20100204333A1
    • 2010-08-12
    • US11988860
    • 2006-07-19
    • Rajesh JainKour Chand JindalSukhjeet SinghMunish Talwar
    • Rajesh JainKour Chand JindalSukhjeet SinghMunish Talwar
    • A61K31/18A61P25/00A61P25/06
    • A61K9/2018A61K9/2027A61K9/2054A61K9/2059A61K9/209A61K9/4808A61K9/4858A61K9/4866A61K9/5084A61K31/18A61K31/192A61K31/415
    • Pharmaceutical modified release dosage form comprising at least one cyclooxygenase enzyme inhibitor or its pharmaceutically acceptable salts, esters, prodrugs, solvates, hydrates, or derivatives thereof as active agent, with a pharmaceutically acceptable carrier for controlling the release of the cyclooxygenase enzyme inhibitor is provided. The dosage form preferably provides a release of not more than about 60% of the cyclooxygenase enzyme inhibitor in 1 hour and not less than about 75% of the cyclooxygenase enzyme inhibitor after 12 hours when tested in accordance with the dissolution method (I) described herein employing Distilled water with 2.0% Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution method (II) described herein employing pH 7.0 Phosphate buffer with 2.0% Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution method (III) described herein employing 0.001 N Hydrochloric acid with 1.0% Sodium lauryl sulphate as dissolution medium. Further, the pharmaceutical composition of the present invention when tested in a group of healthy humans preferably achieves a mean peak plasma concentration (Cmax) after at least about 1 hour of administration of the dosage form. The present invention also provides process of preparing such dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form.
    • 提供了包含至少一种环加氧酶酶抑制剂或其药学上可接受的盐,酯,前药,溶剂化物或其衍生物作为活性剂的药物改性释放剂型,以及用于控制环加氧酶抑制剂释放的药学上可接受的载体。 根据本文所述的溶解方法(I)测试时,剂型优选在12小时后提供不超过约60%的环氧合酶抑制剂的释放量,并且不少于约75%的环氧合酶抑制剂。 使用2.0%十二烷基硫酸钠作为溶解介质的蒸馏水或根据本文所述的溶解方法(II),使用pH 7.0的磷酸盐缓冲液,含有2.0%十二烷基硫酸钠作为溶解介质,或根据溶解方法(III) 本文使用0.001N盐酸与1.0%十二烷基硫酸钠作为溶解介质。 此外,当在一组健康人中测试时,本发明的药物组合物优选在施用剂型至少约1小时后达到平均峰值血浆浓度(C max)。 本发明还提供了制备这种剂型组合物的方法和使用这种剂型的预防和/或治疗方法。