盐酸西替利嗪在人体内的立体选择性研究

Enantioselective Analysis of Cetirizine in Human Plasma by HPLC

目的研究盐酸西替利嗪在人体内的立体选择性。方法建立了非手性-手性联用色谱法(achiral-chiralchromatogra-phy),先用HypersilBDSCl8色谱柱和乙腈-0.05mol.L-1NH4H2PO4溶液(37∶70)为流动相的HPLC色谱系统将西替利嗪与血浆内源性物质分离,然后收集色谱柱后西替利嗪消旋体色谱峰馏分,以手性糖蛋白(α1-acidglycoprotdn,AGP)固定相柱和乙腈-60mmol.L-1醋酸钠溶液(5∶95)组成的手性色谱系统将两种对映体完全拆分。测定了12名中国健康男性志愿受试者口服20mg西替利嗪胶囊(被试制剂)后最大血药浓度时血浆中西替利嗪两个对映体的浓度。结果最大血药浓度时两个对映体在人体血浆中的浓度有不同程度的差异。结论西替利嗪在血浆中具有中等程度立体选择性。

OBJECTIVE To study enantioselective analysis of cetirizine in human plasma by HPLC, METHODS An enantioselective and sensitive aehiral-ehira] chromatographic assay employing Hypersil BDS-C18 column for preseparation and ehiral-AGP column for enantioselective analysis was developed for the determination of the enantiomers of cetirizine in human plasma following an oral administration of capsules （20 mg cetirizine dihydrochloride） to 12 healthy male subjects. The mobile phase was 5% acetonitrile in 60 mmol · L^-1 sodium acetate buffer, Two enantiomers were separated well enough for the quantification of concentrations of enantiomers in human plasma. RESULTS The plasma concentrations of two enantiomer were differenL CONCLUSION Cetirizine has middle enantioselection in human plasma.