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、普拉伐他汀、
辛伐他汀、麦伐他汀、
阿托伐他汀以及它们的衍
生物和类似物被称为
HMG-CoA还原酶
抑制剂,用作抗高
胆固醇药物。它们大多数是通过利用不同物种的微
生物进行发酵生产的,这些物种被鉴定为属于曲霉、
红曲霉、诺卡氏菌、阿米科拉托普西斯、毛霉或青霉属,有些是通过对发酵产物进行
化学合成方法处理得到的,或者它们是全
化学合成的产物。上述活性物质可能会受到环境因素的破坏,它们的降解也可能会因与其他药物成分(如填料、粘结剂、润滑剂、
滑石和分散剂)的相互作用而加速,因此应该精心选择药物成分和药物配方制备过程,以避免上述不良的相互作用和反应。本发明涉及一种通过与缓冲物质或碱化物质形成均匀组合而稳定的
HMG-CoA还原酶
抑制剂。这种均匀组合适用作为药物配方中的活性物质,用于治疗高
胆固醇血症和高脂血症。