雷公藤内酯醇在不同种属肝微粒中体外稳定性性别差异研究  

Metabolic Stability of PG490 in Liver Microsoms of Different Species and Genders

作　　者：刘萍霞 庄笑梅[2] 李铮 张玉杰[3] 张振清[2] LIU Pingxia;ZHUANG Xiaomei;LI Zheng;ZHANG Yujie;ZHANG Zhenqing(Department of Pharmacy,Lushan Sanitarium of PLA,Jiujiang,Jiangxi 332000;Key Laboratory of Drug Metabolism and Pharmacokinetics,Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing,100850;Beijing Medicass Biotechnology Co Ltd,Beijing 100012,China)

机构地区：[1]联勤保障部队庐山康复中心,江西九江332000 [2]军事医学科学院毒物药物研究所药物代谢与药代动力学重点实验室,北京100850 [3]北京美迪克斯生物技术有限公司,北京100012

出　　处：《九江学院学报（自然科学版）》2020年第1期77-79,共3页Journal of Jiujiang University：Natural Science Edition

基　　金：国家重大新药创制(编号2009ZX090304-004);北京市科委重大创新药物研制资助项目(编号D07080201330721)的成果之一。

摘　　要：目的研究雷公藤内酯醇(PG490)在不同种属不同性别肝微粒代谢稳定性差异。方法药物加入大鼠、比格犬以及人不同性别肝微粒体中孵育,于不同时间点加入终止剂,LC-MS/MS测定PG490浓度,计算固有清除率CLint和肝清除率CLh。结果PG490孵育2h后雄性大鼠肝微粒体中转化了80%,而雌性大鼠转化了20%,在比格犬和人肝微粒体较稳定,孵育2h均转化不到15%。结论PG490在大鼠不同性别肝微粒中代谢统计学上有差异,而在比格犬和人肝微粒中没有表现出性别差异。Objective To study the metabolic stability of PG490 in human,beagle dog and rat liver microsomes.Methods The concentrations of PG490 in incubates were measured by LC-MS/MS method.Results The biotransformation in male rat liver microsomes was 80%,but 20%in female and less than 15%in the dog and human liver microsomes with different genders.Conclusion The results indicated that there were a statistical differences of PG490 in rat liver microsomes of different genders and no differences of the biotransformation in dog and human liver microsomes.

关 键 词：雷公藤内酯醇 PG490 代谢 性别差异 

分 类 号：R966[医药卫生—药理学]