普罗帕酮在中国健康受试者体内的羟基化代谢产物研究

被引:6
作者
陈笑艳
黄海华
钟大放
李文
沙沂
不详
机构
[1] 沈阳药科大学!沈阳
关键词
普罗帕酮; 羟基化代谢物; 液相色谱离子阱质谱(LC/MSn)法; 微生物转化;
D O I
10.16438/j.0513-4870.1999.10.013
中图分类号
R969.1 [药物代谢动力学];
学科分类号
100602 ; 100706 ;
摘要
目的:阐明普罗帕酮羟基化代谢过程的种属及种族差异。方法:选择10 名中国健康受试者单剂量po300 mg 盐酸普罗帕酮片,收集0 ~12 h 的尿样,经液 液萃取后,采用LC/ MSn 技术,对羟基化代谢产物进行选择性离子监测(m/z 358) 和多级全扫描质谱分析。结果:在服药后的尿样中检测到两种羟基化代谢产物,根据质谱数据,推测这两种代谢产物分别为4′ 羟基普罗帕酮和5 羟基普罗帕酮。采用微生物转化法结合半制备HPLC制备并分离了4′ 羟基普罗帕酮的对照品,通过NMR 证实了其结构。结论:在10 名受试者服药后的尿样中均能检测到代谢物4′ 羟基普罗帕酮和5 羟基普罗帕酮,与文献报道的白人受试者代谢结果相比,中国受试者有较宽的羟基化代谢谱
引用
收藏
页码:776 / 781
页数:6
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