手性HPLC测定Naftopdil代谢产物的对映体
Determination of Naftopidil metabolites enantiomers by Chiral HPLC
作者：白浩;刘夏雯;袁牧;
Author：
收稿日期： 年卷（期）页码：2013,28(01):-89-91
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：Naftopidil;手性代谢产物;手性高效液相色谱法;对映异构体;含量测定
Key words：
基金项目：2010年广州市科技专项(项目编号:2010U1-E00531-2)
中文摘要
目的分离和测定Naftopidil手性代谢产物:去甲基代谢产物(DMN)、苯羟化代谢产物(PHN)和萘羟化代谢产物(NHN)的对映体。方法采用HPLC法,流动相为异丙醇-正己烷(15∶85),流速为1.0 mL.min-1,柱温为25℃,检测波长为283 nm。结果 3对对映体能同时得到良好地分离。经方法学验证,R-DMN(4.99～159.68μg.mL-1)、R-PHN(5.30～168.00μg.mL-1)、R-NHN(5.00～160.16μg.mL-1)与峰面积线性良好;RSD
参考文献
[1]Himmel HM.Naftopidil,anovel antihypertensive drug[J].Card-iov Drug Rev,1994,12(1):32.
[2]Kawasaki H,Nakamura S,Takasaki K,et al.Antihypertensiveeffect of naftopidil(KT2611),a novel alpha1-adrenoceptorantagonist in freely moving experimental hypertensive rats anddogs[J].Jpn J Pharmacol,1990,96:129-139.
[3]Ju XB,Wu HF,Su JT.The clinical efficacy of naftopidil tablet inthe treatment of benign prostatic hyperplasia[J].Natl J Androl,2002,8:286-288.
[4]Yuan M,Tang L,Fu XZ,et al.Determination of naftopidil and itsmain metabolite in plasma by highperformance liquid chromatog-raphy[J].Acta Pharm Sin,1998,33:768-771.
[5]付晓钟,汤磊,袁牧.R,S-1-(取代苯基)-4-[3-(萘-1-氧基)-2-羟基丙基]哌嗪类化合物的设计、合成及血管舒张活性[J].药学学报,2007,42(7):735-740.
[6]Li L,Zhou X,Yuan M,et al.Metabolites of R,S-1-(2-methoxyphenyl)-4-[3-(naphtha-1-yl-oxy)-2-hydroxypropyl]-piperazine in rat plasma[J].Acta Pharm Sin,2006,41:80-84.
[7]Niebch G,Loeher M,Peter G,et al.Metabolic fate of the novelantihypertensive drug naftopidil[J].Arzneimittelforsch,1991,41:1027-1032.
[8]Liu XW,Yuan M,Ji H,et al.Comparison of different polysaccha-ride-based chiral stationary phases for enantioselective resolutionof Naftopidil and its derivatives by HPLC[J].J Chin Pharm Sci,2010,19:293-299.
[9]Sun YX,Huang BY,Yuan M,et al.Development of a chiralHPLC method for the analysis of naftopidil enantiomers[J].JChin Pharm Sci,2009,18:61-63.
[10]李成平,施介华,单纬光.高效液相色谱手性流动相添加剂拆分麻黄碱对映体[J].华西药学杂志,2004,19(5):333-335.
【关闭】
