Abstract:Objective:To study the pharmacokinetics of the transdermal absorption of Sinomenine in patch under electroporation condition by comparing with the transdermal absorption of passive diffusion. Methods: Sinomenine was taken as a model drug and was given to rabbits by passive diffusion (PD group) or by electroporation (EP group). The plasma drug concentration was determined by HPLC. The statistical moment theory was used for analyzing the values of plasma drug concentration.Results: The AUC0→∞ was 43.396 in the EP group, which was 1.32 folds that of the PD group. The mean residence time (MRT) was 20.025 in the EP group, which was 86% of the PD group. The cmax was 1.825 in the EP group, which was 1.31 folds that of the PD group. The decrease of tmax in the EP group was 4 hours earlier than that in the PD group. Their elimination rate constants λ were the same. The drug-time curve of EP group was more smooth and slow when declining compared with that of the PD group.Conclusion: The combination of electroporation and the patch can improve the speed and extent of transdermal absorption of sinomenine, and thus enhance the bioavailability.