| 摘要: |
| 目的:将巴布剂结合电致孔透皮给药，与被动扩散透皮给药进行比较，初步考察在电致孔条件下巴布剂中青藤碱透皮吸收的药动学特点。方法:以青风藤为模型药物，以活体兔分别进行被动扩散给药(PD)和电致孔透皮给药(EP)，高效液相色谱仪测定不同时间的血药浓度，采用统计矩分析法处理分析血药浓度数据。结果:电致孔技术透皮给药的AUC0→∞为43.396，是被动扩散的1.32倍，体内平均滞留时间为20.025，是被动扩散的86%，cmax为1.825，是被动扩散的1.31倍， tmax减小，比被动扩散提前4 h；消除速率常数λ二者一致；电致孔技术透皮给药的药-时曲线比被动扩散的药-时曲线平滑且下降较慢。结论: 将电致孔技术与巴布剂结合能够提高药物透皮吸收的速度和程度，从而提高生物利用度。 |
| 关键词: 电致孔 巴布剂 透皮吸收 青藤碱 药代动力学 |
| DOI：10.3724/SP.J.1008.2008.01096 |
| 投稿时间：2008-03-22修订日期：2008-07-13 |
| 基金项目: |
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| Pharmacokinetics of transdermal absorption of Sinomenine in patch under electroporation condition |
| LI Fan1,HAO Bao-hua1*,LI Wei-ze2,LIU Sen1,TANG Bin-bin1,DU Shu-jun1 |
| (1.Department of Traditional Chinese Medicine,College of Life Science,Northwest University, Xi’an 710069,China*2.Department of Pharmaceutics,College of Pharmaceutical Sciences,China Pharmaceutical University, Nanjing 210009) |
| 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. |
| Key words: electroporation patch transdermal absorption sinomenine pharmacokinetics |
