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    • 10. 发明授权
    • Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same
    • 稳定的药学有效组合物和包含其的药物制剂
    • US06806290B2
    • 2004-10-19
    • US10298187
    • 2002-11-15
    • Zlatko PflaumJanez Kerc
    • Zlatko PflaumJanez Kerc
    • A61K31225
    • A61K31/366A61K31/401
    • Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, and some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The aforementioned active substances may be destabilized by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers, binders, lubricants, glidants and disintegrating agents, therefore the pharmaceutical ingredients and the process for preparation of the pharmaceutical formulation should be meticulously chosen to avoid the aforementioned undesired interactions and reactions. The present invention relates to a HMG-CoA reductase inhibitor which is stabilized by forming a homogeneous composition with a buffering substance or a basifying substance. This homogeneous composition is suitably used as the active substance in a pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia.
    • 洛伐他汀,普伐他汀,辛伐他汀,美伐他汀,阿托伐他汀及其衍生物和类似物被称为HMG-CoA还原酶抑制剂,并用作抗高胆固醇血症药。 它们中的大多数是通过使用被鉴定为曲霉属,红曲霉,诺卡氏菌属,无性系,毛霉属或青霉属的物种的不同物种的微生物进行发酵的,一些是通过使用化学合成方法处理发酵产物而得到的,或者它们是 化学合成产物。 上述活性物质可能被环境因素不稳定,它们的降解也可以通过与其它药物成分例如填料,粘合剂,润滑剂,助流剂和崩解剂的相互作用而加速,因此药物成分和药物制备方法 应精心选择配方以避免上述不良的相互作用和反应。 本发明涉及通过用缓冲物质或碱化物质形成均匀组合物来稳定的HMG-CoA还原酶抑制剂。 该均匀组合物适合用作用于治疗高胆固醇血症和高脂血症的药物制剂中的活性物质。