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    • 7. 发明申请
    • HIGH DOSE SOLID UNIT ORAL PHARMACEUTICAL DOSAGE FORM OF MYCOPHENOLATE SODIUM AND PROCESS FOR MAKING SAME
    • 高剂量固体单位口服药用麦芽酚钠的剂型及其制备方法
    • WO2009047799A1
    • 2009-04-16
    • PCT/IN2008/000651
    • 2008-10-08
    • PANACEA BIOTEC LIMITEDJAIN, RajeshSINGH, SukhjeetDEVARAJAN, Sampath Kumar
    • JAIN, RajeshSINGH, SukhjeetDEVARAJAN, Sampath Kumar
    • A61K31/343A61K31/365
    • A61K31/343A61K9/2054A61K31/365
    • Provided are high dose solid unit oral pharmaceutical dosage form compositions comprising mycophenolate sodium as active agent in an amount of from greater than about 720 mg to about 1500 mg, preferably from about 800 mg to about 1440 mg calculated as mycophenolic acid, and one or more pharmaceutically acceptable excipient(s). Particularly the dosage form compositions are meant for once-a-day or twice-a-day administration and provide the active agent in an extended release form which is released in a sustained manner in-vivo for a prolonged duration. The invention is also directed to process of manufacturing the high dose formulations, and prophylactic and/or therapeutic methods of using such dosage forms. The composition of the present invention are easy to formulate, safe, effective and well-tolerated, and 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).
    • 提供了包含以霉酚酸计算的大于约720mg至约1500mg,优选约800mg至约1440mg的量的霉酚酸钠作为活性剂的高剂量固体单元口服药物剂型组合物,以及一种或多种 药学上可接受的赋形剂。 特别地,剂型组合物是指每天一次或每天两次施用,并且以延长的释放形式提供活性剂,其以持续的方式在体内长时间释放。 本发明还涉及制备高剂量制剂的方法,以及使用这种剂型的预防和/或治疗方法。 本发明的组合物易于配制,安全,有效和耐受性良好,并且可用于治疗,例如预防,改善和/或治疗指定的疾病/病症,特别是用于治疗的免疫抑制剂 或预防器官,组织或细胞同种异体移植物或异种移植排斥,例如 移植后,或免疫介导的疾病(自身免疫性疾病)的管理。
    • 9. 发明申请
    • EXTENDED RELEASE COMPOSITIONS COMPRISING MYCOPHENOLATE SODIUM AND PROCESSES THEREOF
    • 包含MYCOPHENOLATE SODIUM的延伸释放组合物及其过程
    • WO2009022355A1
    • 2009-02-19
    • PCT/IN2008/000505
    • 2008-08-11
    • PANACEA BIOTEC LIMITEDJAIN, RajeshSINGH, SukhjeetDEVARAJAN, Sampath Kumar
    • JAIN, RajeshSINGH, SukhjeetDEVARAJAN, Sampath Kumar
    • A61K9/22A61K31/341A61K31/365
    • 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 such dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The composition of the present indention are safe, effective and well-tolerated, and 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。 本发明的组合物是安全,有效和耐受性良好的,并且可用于诸如预防,改善和/或治疗免疫抑制剂,特别是用于治疗或预防器官的疾病/病症 ,组织或细胞同种异体移植物或异种移植物排斥,例如 移植后,或免疫介导的疾病(自身免疫性疾病)的管理。