双氯芬酸钾胶囊人体药代动力学与相对生物利用度研究

目的 :研究双氯芬酸钾胶囊在正常人体内的药代动力学与相对生物利用度。方法 :采用HPLC法测定10名健康男性志愿者随机自身交叉单剂量口服50mg 双氯芬酸钾胶囊和进口双氯芬酸钾片后的血药浓度 ,计算两者的药代动力学参数及相对生物利用度 ,并以AUC(0～6) 、Tmax 、Cmax 为指标 ,用配对t检验法分析国产胶囊与进口片的生物等效性。结果 :国产与进口双氯芬酸钾制剂的药 -时曲线符合口服吸收一房室模型。AUC(0～6 ) 分别为 (1834 52±711 06) μg/(h·L)、(1891 19±859 08) μg/(h·L) ;Tmax 分别为 (1 15±0 77)h、(1 30±0 97)h ;Cmax 分别为 (1522 29±1063 87)ng/ml、(1508 54±892 44)ng/ml。配对t检验结果表明 ,AUC(0～6) Tmax、Cmax 均无显著性差异 (P>0 05)。结论 :国产双氯芬酸钾胶囊对进口片的相对生物利用度为 (100 80±16 59) % ,国产与进口两种双氯芬酸钾制剂具有生物等效性

Pharmacokinetics and Relative Bioavailability of Diclofenac Potassium Capsules

OBJECTIVE:To study the pharmacokinetics and relative bioavailability of diclofenac potassium capsules in normal volunteers.METHODS:A single oral 50mg dose of domestic diclofenac potassium capsules or imported diclofenac potassium tablets were given to 10 healthy male volunteers in an open randomized crossover study.Diclofenac potassium concentration in plasma were determined by HPLC.The pharmacokinetic parameters as well as relative bioavailability were measured.RESULTS:The concentration－ time curves of domestic diclofenac potassium capsules and imported diclofenac potassium tablets were conformed to one compartment open model.The AUC(0～ 6)was (1 834.52± 711 06） μ g/（ h· L） and (1 891.19± 859.08)μ g/（ h· L） ， Tmax(1.15± 0.77)h and (1.30± 0.97)h,Cmax(1 522.29± 1 063.87)ng/ml and (1 508.54± 892.44)ng/ml respectively.There were no significant differences between the two formulations in the AUC(0～ 6),Tmax,Cmax.CONCLUSION:The relative bioavailability of domestic diclofenac potassium capsule was(100.80± 16 59)％ compared with the imported tablet.The result of the statistical analysis showed that the two formations were bioequivalent.