蛋白酶抑制剂对酪丝亮肽代谢及药代动力学的影响  

Effect of Protease Inhibitors on the Metabolism and Pharmacokinetics of Tyroserleutide

作　　者：孙迎基 于华玲 韦静 丁文锋 

机构地区：[1]深圳市康哲药业有限公司,深圳518057

出　　处：《药物生物技术》2010年第1期76-78,共3页Pharmaceutical Biotechnology

摘　　要：研究蛋白酶抑制剂对酪丝亮肽代谢及药代动力学的影响。在酪丝亮肽体外血浆代谢系统中,分别加入4种常见的蛋白酶抑制剂,考察其对酪丝亮肽降解曲线的影响,并进一步考察联合使用对酪丝亮肽大鼠药代动力学的影响。体外血浆代谢研究表明,乌苯美司对酪丝亮肽体外血浆降解有明显抑制作用,其它3种酶抑制剂无影响;大鼠药代动力学研究表明,乌苯美司可显著改善酪丝亮肽药代动力学行为,提高体内血药浓度。氨肽酶是酪丝亮肽降解的主要酶,建议在临床中探索乌苯美司与酪丝亮肽的联合用药方案。To study the effect of protease inhibitors on the metabolism and pharmaeokinetics of Tyroserleutide, in the serum metabolism system in vitro, four protease inhibitors were separately added Into tile serum metabolism system in vitro to evaluate the effect on the metabolism curve of Tyroserleutide, and then further evaluate the effect of combination use on the pharmacokinetics of Tyroserleutide. The serum metabolism inhibition test suggests that bestatin significantly inhibits the degradation of Tyroserleutide by serum in vitro. Pharmacokinetics study of Tyroserleutide in rats suggests that aminopeptidase is the main enzyme involved in the degradation of Tyroserleutide. The combination use of bestatin and Tyroserleutide is a promising therapeutic regimen, and need to be investigated in the clinical trial

关 键 词：酪丝亮肽 药代动力学 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学]