双氯芬酸二乙胺凝胶贴剂的药动学

Pharmacokinetics of diclofenac diethylamine gel-matrix patch

目的:研究自制的双氯芬酸二乙胺凝胶贴剂的兔体内的药动学特征。方法:外贴经皮给药,以德国上市贴剂Flector EP-flaster为参比制剂,用HPLC测定不同时间血药浓度,用3P97药动学程序进行处理,计算药动学参数,并对2种制剂在体内的主要药动学参数分别进行t检验。结果:兔透皮给予双氯芬酸二乙胺后的药动学过程符合一室模型,2种贴剂的药动学参数AUC、Cmax、tmax、t1/2(ka)、ka和Lagtime差异无显著性(P>0.05),而t1/2(ke)和ke差异有显著性(P<0.05),CL/F和V/F差异有极显著性(P<0.01)。结论:自制的双氯芬酸二乙胺凝胶贴剂与相应的德国贴剂相比,具有更缓释、长效的作用。

OBJECTIVE To study the pharmacokinetics of diclofenac diethylamine gel-matrix patch on rabbit. METHODS The HPLC was used to assay the plasma concentration of diclofenac diethylamine after the transdermal delivery, and the comparative patch was diclofenac epolamin patch developed and sold in Germany. The data were processed by 3P97 programme, and the pharmacokinetics parameters were calculated and compared by t test. RESULTS The process of the pharmacokineties of diclofenac diethylamine gel-matrix patch on rabbit fitted to the open one compartment model. There was no significant difference （P〉0. 05） between the respective pharmaeokinetics parameters AUC, Cmax t1/2（ka）,ka, and Lag time of the two kinds of patches. The significant difference （P〈0.05） shown between the respective t1/2〈ke） and ke, and the extremely significant differ ence （P〈0.01） was revealed between the respective CL/F and V/F. CONCLUSION The dielofenac diethylamine gel matrix patch has prolonged action.