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。 The effects of protease inhibitors on the metabolism and pharmacokinetics of tyroserulene were studied. In the in vitro plasma metabolites of tyroserpene, four kinds of common protease inhibitors were added respectively to investigate their effects on the degradation of tyroserpene, and the effects of combined use on the pharmacokinetics of tyroserpeptide in rats influences. In vitro plasma metabolism studies showed that ubenimex had a significant inhibitory effect on the in vitro degradation of tyroserme in vitro, and no effect was observed by the other three enzyme inhibitors. Pharmacokinetic studies in rats showed that ubenimex significantly improved Bright peptide pharmacokinetic behavior, increase in vivo blood concentration. Aminopeptidase is tyroserpin degradation of the main enzyme, it is proposed to explore in the clinical ubenimex and casein bright peptide combination regimen.