洛索洛芬片的人体药动学研究

目的 :建立反相高效液相色谱新方法 ,测定洛索洛芬片在健康人体内的药动学。方法 :色谱柱为Hypersil ODS(2 0 0mm×4 .0mmID ,5 μm) ,流动相组成为 pH2 .5 ,0 .0 2mol·L- 1磷酸二氢钠 乙腈 四氢呋喃 (6 6∶30∶4 ) ,检测波长 2 2 2nm。 10名健康志愿者单剂量口服 6 0mg洛索洛芬片后 ,体内血药浓度采用 3P87程序统计矩方法处理。结果 :在确定的色谱分离条件下 ,血浆样品中洛索洛芬无杂质干扰 ,且峰面积与相应浓度之间呈良好的线性关系。人体药动学参数Tmax,Cmax,T1/2 ,MRT ,AUC0～∞分别为 (0 .6± 0 .3)h ,(3.9± 1.1)mg·L- 1,(2 .0±0 .4 )h ,(2 .0± 0 .3)h ,(7.1± 1.3)mg·h·L- 1。结论 :本法操作简便快速 ,定量准确可靠 ,适用于洛索洛芬片的人体药动学研究

Study on pharmacokinetics of loxoprofen tablets in healthy volunteers

AIM: To study pharmacokinetics of loxoprofen tablets in healthy volunteers by a new RP HPLC method. METHODS: The separation was performed on Hypersil ODS(200 mm×4.0 mmID,5 μm)column and the mobile phase system consisting of acetonitrile, tetrahydrofuran and 0.02 mol·L -1 phosphate buffer (pH2.5) with the ratio of 30∶4∶66 and that was suitable for the biosample assay of loxoprofen tablets. The detection wavelength was 222 nm. Ten healthy volunteers were given orally with a single dose of 60 mg loxoprofen tablets and the plasma concentrations of loxoprofen were handled with 3P87 program and the theory of statistical moment. RESULTS: Loxoprofen peaks in plasma samples were not interfered under the optimal chromatographic conditions and the good linearity was obtained between the peak areas of loxoprofen and the concentrations of loxoprofen in plasma samples. The main pharmacokinetic parameters were as follows: T max was (0.6±0.3) h, C max was (3.9±1.1) mg·L -1 , T 1/2 was (2.0± 0.4 ) h, MRT was (2.0± 0.3 ) h, AUC 0～∞ was (7.1±1.3) mg·h·L -1 ,respectively. CONCLUSION: This RP HPLC method is simple, quick, accurate, reliable,and suitable for the pharmacokinetic study of loxoprofen tablets.