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中国临床药理学与治疗学 ›› 2003, Vol. 8 ›› Issue (4): 425-427.

• 研究原著 • 上一篇    下一篇

HPLC法检测盐酸戊乙奎醚R型异构体经小鼠尿排泄的方法学研究

薛明1, 阮金秀, 张振清, 袁淑兰, 吴波, 李宇航1   

  1. 军事医学科学院毒物药物研究所,北京 100850;
    1首都医科大学药物研究所,药理教研室,北京 100054
  • 收稿日期:2002-11-23 修回日期:2003-04-03 出版日期:2003-08-26 发布日期:2020-11-19
  • 通讯作者: 薛明,男,博士,副研究员,硕士生导师.研究方向:药物代谢与药代动力学。Tel:010-63051453  E-mail:xuemd@163.net

Method studies on HPLC determination of R-isomers ofPenehyclidine hydrochloride in urine excretion in mice

XUE Ming1, RUAN Jin-Xiu, ZHANG Zhen-Qin, YUAN Shu-Lan, WU Bo, Li Yu-Hang1   

  1. Institute ofPharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850,China;
    1Institute of Materia Medica,Capital University of Medicai Sciences,Beijing 100054,China
  • Received:2002-11-23 Revised:2003-04-03 Online:2003-08-26 Published:2020-11-19

摘要: 目的 建立HPLC 测定方法研究R 型盐酸戊乙奎醚光学异构体在小鼠体内的排泄。方法 采用新建立的正相HPLC 法,尿样经提取处理后,选用Spherisorb SiO2色谱柱,以甲醇-二氯甲烷-氨水(8∶2∶0.1)为流动相,流速0.8 ml·min-1,检测波长254 nm,进样量20μl 。结果 在0.5 ~ 100 mg·L-1浓度范围内,R 异构体峰面积与浓度呈良好的线性关系(r 分别为0.9994 与0.9997)。两R 型异构体的平均回收率均大于85 %,日内和日间RSD 均小于13 %。小鼠肌注给药后不同时间内,R 型异构体在尿中的比值(R-1/R-2)存在显著差异(P<0.05)。48 h 内R 型异构体在尿中的排泄量明显不同。结论 本法简单方便,可用于R 型异构体在小鼠体内立体选择性排泄研究。

关键词: 高压液相色谱法, 盐酸戊乙奎醚, 光学异构体, 排泄

Abstract: AIM: To study a method of HPLC determination of R-isomers ofPenehyclidine hydrochloride(RPHC)in mouse urine excretion.METHODS: Urine samples were collected andPrepared after i.m.a single dose 30μg of R-PHC in mice.The HPLC system consisted of Spherisorb SiO2column,methanol-dichloromethaneammonialiquor(8∶2∶0.1)as mobilePhase with 254 nm,flow rate:0.8 ml·min-1,and injection volume of 20μl.RESULTS: Thelinear range was 0.5 -100mg·L-1(r =0.9994 and 0.9997,respectively),and the average recovery was more than 85 %.The RSD of intra-day and inter-day assays of two isomers were allless than 13 %.Thelimit of detectionProved to be 0.1μg·ml-1.The ratio of R-1/R-2 in urine changed within the time after dosing.The cumulative excretion of the two optical isomers had distinguished differences(P<0.05)in urine.CONCLUSION: This HPLC method is simple and convenient,and able to investigate the stereo-selective excretion of R-PHC isomers in urine.

Key words: pharmacology, HPLC, penethyclidine hydrochloride, R-isomers, excretion

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