血浆中比索洛尔对映体的拆分及含量测定方法  

Resolution and determination of enantiomers of bisoprolol in human plas ma

作　　者：陈鹰[1] 马旻[1] 郑汉平[1] 

机构地区：[1]广州军区武汉总医院药剂科,湖北武汉430070

出　　处：《中国药学杂志》2002年第12期940-943,共4页Chinese Pharmaceutical Journal

摘　　要：目的　探索血浆中比索洛尔 (BSP)两个对映体的拆分及含量测定方法。方法　采用乙酰葡萄糖异硫氰酸酯 (GITC)为柱前衍生化试剂 ,以RP HPLC测定血浆中各对映体的含量。结果　流动相为乙腈 水 (3∶2 ) ,紫外检测波长为 2 70nm ,两个对映体分离度好 ,各对映体血药浓度在 2 5～ 50 0ng·mL- 1 范围内呈良好线性关系 ,BSP最低检测浓度为 1 0ng·mL- 1 (S/N >3) ,低、中、高 3种浓度的 (S) BSP或 (R) BSP的日内、日间RSD均小于 1 0 % ,方法回收率 >95 % ,萃取回收率 >80 %。结论　本方法可用于分离测定血浆中比索洛尔对映体以及对映体药动学立体选择性差异的研究。OBJECTIVE: To study a method to resolve and determine the enantiomers of bisoprolol (BSP) in human plasma. METHODS: 2,3,4,6-tera-O-acetyl-β-D-glucopyranosyl isothiocynate(GITC) was selected as a chiral derivative reagent, and a RPHPLC method was established to determine the enantiomers of bisoprolol in plasma. The mobile phase was composed of acetonitrile-water (3:2), the detection wavelength was 270 nm. RESULTS: The two enantiomers of Bisoprolol were well separated. The linear range was 25-500 ng&middotmL-1. The detection limit of BSP was 10 ng&middotmL-1. Both RSD of intra-day and inter-day of the low, medial and high level of (S)-BSP or (R)-BSP were less than 10%. The recoveries were >95%, and the extracted recoveries were >80%. CONCLUSION: The method can be used to resolve and determine the enantiomers of Bisoprolol in plasma. And it can be further used to study its stero-selectivity of pharmacokinetics.

关 键 词：比索洛尔 对映体 柱前衍生化法 反相高效液相色谱法 RP-HPLC法 血药浓度 

分 类 号：R969.1[医药卫生—药理学] R972[医药卫生—药学]