Böhm R, Ellrich R, Koytchev R
Analytisches Laboratorium, Bero-Lab GmbH, Rodleben.
Pharmazie. 1995 Aug;50(8):542-5.
Several methods for the determination of racemic propafenone or its enantiomers as well of the main metabolite R,S-5-hydroxypropafenone are known from the literature. The method described here enables the simple simultaneous quantification of R- and S-propafenone and of R,S-5-hydroxypropafenone in human plasma. The method is based on an HPLC separation using a Chiralpak AD column. High recovery rates (80-95%) were achieved by means of a liquid-liquid-extraction at pH 11 with dichloromethane as solvent. The separation on the chiral carrier were carried out with n-hexane/2-propanol; the addition of diethylamine is useful. The obtained capacity factors are k' = 2.36 for R-propafenone and k' = 3.82 for S-propafenone. R,S-propanolol and R,S-metoprolol were used as internal standards. The method described can be used for pharmacokinetic trials in man with the following limits of quantitation: 10 ng/ml for R- and S-propafenone and 20 ng/ml for R,S-5-hydroxypropafenone.
文献中已知几种测定消旋普罗帕酮或其对映体以及主要代谢物R,S-5-羟基普罗帕酮的方法。本文所述方法能够简单地同时定量人血浆中的R-和S-普罗帕酮以及R,S-5-羟基普罗帕酮。该方法基于使用Chiralpak AD柱的高效液相色谱分离。通过以二氯甲烷为溶剂在pH 11下进行液-液萃取，实现了高回收率（80 - 95%）。在手性载体上的分离用正己烷/2-丙醇进行；添加二乙胺是有用的。得到的容量因子为：R-普罗帕酮的k' = 2.36，S-普罗帕酮的k' = 3.82。R,S-普萘洛尔和R,S-美托洛尔用作内标。所述方法可用于人体药代动力学试验，定量限如下：R-和S-普罗帕酮为10 ng/ml，R,S-5-羟基普罗帕酮为20 ng/ml。
