HPLC法测定健康人血清中吗咯替酯及其代谢产物浓度

HPLC Determination of Malotilate and Its Metabolite in Human Serum

本文介绍用ＨＰＬＣ法测定人血清中吗咯替酯（Ⅰ）及其代谢产物（Ⅱ）的浓度，以二仲丁基－１，３－二硫杂环戊烯－２－亚丙二酸酯（Ⅲ）为内标，血样用乙酸乙酯萃取Ⅰ和Ⅱ，浓缩进样，使用Ｗａｔｅｒｓ－μ－ＢｏｎｄａｐａｋＣ＿（１８μ）３．９ｍｍ×３００ｍｍ色谱柱，流动相为甲醇－水－３６％醋酸（８０：１９．２：０．８），检测波长为３６２ｎｍ。Ⅱ、Ⅰ和Ⅲ的峰分离度好，保留时间分别为５．８、８．２、１２．１ｍｉｎ。测定线性范围Ⅰ为０．０１～１．０μｇ／ｍｌ，ｒ＝０．９９９７，最低检测限为０．００５μｇ／ｍｌ；Ⅱ为０．１～１．００μｇ／ｍｌ，ｒ＝０．９９７５。本文还介绍了６例健康人口服吗咯替酯后，用本法测定Ⅰ和Ⅱ的血清浓度及药代动力学参数。

A RP-HPLC modified method has been developed for th determination of malotilate and its main metabolite in human serum Waters μ-Bondapark C_(18) Column was used. The mobile phase was methanol-water-36% HAc (80:19. 2 :0.8). The eluent was monitored at 362nm. Serum samples were extracted with ethyl acetate. The extract was evaporated to dryness and dissolved in 95% alcohol. The colibration curve is linear in the range of 10～20ng/ml (r=0. 999) for metabolite. The minimal detectable concentration of 5ng/ml of Malotilate was achieved. The recoveries of Malotilate and its main metabolite were found to be 99. 4% and 98. 4% respectively.The RSD within day and day to day were less than 5%.The results of pharmacokinetic study were reported. This method is sensitive. simple. accurate and rapid.