高效液相色谱法测定扑炎痛在人血浆中活性代谢物及生物利用度研究

Evaluation of Benorylate and Its Active Metabolite by HPLC and Comparative Bioavailability Investigation in Human Plasma

采用高效液相色谱法测定人血浆中扑炎痛活性代谢物水杨酸及扑热息痛含量，以比较两种不同制剂的生物利用度。血浆中药物分别用乙醚和乙酸乙酯两步提取；ＹＷＧＣ（１８）为固定相，甲醇－ｐＨ２．１磷酸盐缓冲液（６０：５０）为流动相，测定波长为２３８ｎｍ；水杨酸和扑热息痛的检测范围分别为１．０～２００．μｇ／ｍｌ，１．０～２５．μｇ／ｍｌ，平均回收率分别为９７．５７±６．１５％，９７．４３±４．３９％。用本法测定了８名健康志愿者分别服用市售扑炎痛片剂Ａ（５００ｍｇ／片）及自制片剂以４００ｍｇ／片）后的血药浓度，结果表明Ａ、Ｂ的水杨酸血药峰浓度分别为１１３．０５，１３１．７８μｇ／ｍｌ；达峰时间分别为２．５，２．Ｏｈ；Ｂ对Ａ的相对生物利用度为１２５．５９％。

An analitical method of HPLC was developed which detected benorylate and its active metabolites in order to compare the bioavailability in human plasma was carried out in two steps with ether and acetate.The seperation was performed on the YWG C(18)column with mobile phase of methanol-pH2.1 phosphate buffer(60:50)at 238 nm of detection wavelength.The lowest limit was 50 ng for paracetamol and salicylic acid.The mean recover ies in plasma were 97.57±6.15%,97.43±4.39%for SA and PA respectively.The plasma concentration of 8 healthy volunteers after taking benorylate tablet A(500 mg×9)and B(400 mg×9)was detected.The results showed that the maxium plasma concentration of SA was 113.05μg/ml from tablet A and 131.78μg/ml from B;the top time was 2.5 and 2.0 h for A and B respectively. The relative bioavailability of B to A was 125.59%.