小分子激酶抑制剂药物制剂处方工艺研究  

Research progress on preparation of small molecule kinase inhibitors

作　　者：刘婷 马新荣 罗慧敏 

机构地区：[1]辰欣药业股份有限公司,山东济宁272073

出　　处：《药学研究》2017年第8期477-480,共4页Journal of Pharmaceutical Research

摘　　要：激酶功能异常在癌症治疗中具有重要意义,正常细胞通常可以耐受对激酶的抑制,因此为选择性杀死肿瘤细胞提供了一种方法。目前所有的小分子激酶抑制剂(sm KIs)类药物均为口服固体制剂,药物的构效关系决定此类药物的溶解度低,进而造成生物利用度低且差异性大。本文对此类药物的理化性质、目前上市产品的制备工艺进行综述,目的在于为小分子激酶抑制剂类药物提供更合理的处方工艺设计思路。Kinase dysfunction is important in the treatment of cancer,and normal cells can tolerate the inhibition of kinases,thus providing a method for selective killing of tumor cells. All of these small molecular kinase inhibitor（ sm KIs）drugs are administered orally.The structure-activity relationship of the drug determines the low solubility of the drug,resulting in low and variable bioavailability.In this paper,the physical and chemical properties of this kind of drugs,the current progress on preparation of the commercial pharmaceutical products were reviewed,the purpose was to provide a more reasonable formulation design for sm KIs drugs.

关 键 词：小分子激酶抑制剂 生物利用度 制备工艺 

分 类 号：TQ460.6[化学工程—制药化工]