【摘要】 目的　建立人血浆中洛索洛芬钠浓度的HPLC测定方法 ,研究健康受试者口服国产洛索洛芬钠片的药代动力学 ,以进口洛索洛芬钠片作为参比制剂 ,计算两制剂的相对生物利用度 ,判断两种制剂是否等效。方法　血浆样品加入内标后经三氯乙酸沉淀蛋白、涡旋、离心 ,吸取上清液进样。色谱柱为ShimadzuVP ODS(15 0mm× 4 . 6mmi d ,5 μmC18) ,流动相为 0 . 0 5mol·L 1磷酸二氢钾 甲醇 (2 7∶73) (v/v) ,紫外检测波长 2 30nm。测定了 2 0名受试者单剂量口服两种洛索洛芬钠片 6 0mg后血药浓度 时间过程。结果　最低检测浓度 0 . 2 μg·ml 1,回收率大于 80 % ,日间和日内的变异系数小于 10 . 5 % ,线性范围为 0 . 2～12 . 0 μg·ml 1(r=0 9998) ,符合生物样品分析的要求。主要药动学参数分别为 :国产洛索洛芬钠片 :t1/2 为 1. 39± 0 . 15h ,AUC0 . 6h10 . 71± 1 .4 5 μg·h·ml 1,Cmax7. 2 3± 1 .0 2 μg·ml 1,tmax0 4± 0 1h ;参比制剂t1/2 为 1. 4 1± 0 .15h ,AUC0. 6h10 .4 6± 1 .32 μg·h·ml 1,Cmax7 4 9± 1 .2 6 μg·ml 1,tmax0 .4± 0 .1h。结论　建立的HPLC法简单快速 ,定量可靠准确 ,适合于洛索洛芬钠临床研究。洛索洛芬钠受试制剂的相对生物利用度为 (10 3 .2± 15 .1) %。经统计学分更多还原

【Abstract】 OBJECTIVE To establish a reversed phase HPL C method for determination of loxoprofen sodium in plasma and to study the pharmac okinetics and relative bioavailability following oral administration of domestic and imported loxoprofen sodium tablet in healthy volunteers.METHODS After adding internal standard,the plasma samples were precipitated wit h 20% trichloroacetic acid and determined by HPLC-UV.Shimadzu VP-ODS C 18 column was used. Mobile phase consisted of 27% 0.05 mol·L -1 potassi um dihydrogen phosphate and 73% methanol.The eluted peaks were detected by UV d etector at 230 nm.A single oral test tablet and reference tablet of both 60 mg were given to 20 healthy volunteer at random. Plasma concentration of loxoprofe n sodium was determined by HPLC.RESULTS The recoveries of loxop rofen sodium from plasma were over 80% and RSD% of intra-day and int er- day were smaller than 10.5%.Calibration curves were linear within 0.2～12.0 μg·ml -1(r=0.9998) and the minimum detection concentration was 0.2 μg·ml -1.The main pharmacokinetic parameters after oral administration of dome stic and imported loxoprofen sodium tablet (60 mg)were:t 1/2 were 1.3 9±0.15 h and 1.41±0.15 h;AUC 0-6 h were 10.71±1.45 μg·h·ml -1 and 10.46±1.32 μg·h·ml -1;C max were 7.23±1.0 2 μg·ml -1and 7.49±1.26 μg·ml -1;t maxwere 0.4±0 .1 h and 0.4±0.1 h respectively.CONCLUSION A simple, reli able and rugg ed HPLC assay for loxoprofen sodium was developed. The assay method was conveni ent for clinical laboratory. The relative bioavailability of test tablet was(1 03.2±15.1)%.The results demonstrated that two formations of loxoprofen sod ium tablet were bioequivalent.更多还原