可乐定透皮贴剂体外透皮性能研究

目的:研究可乐定透皮贴剂体外透皮性能.方法:用离体豚鼠皮肤为透皮屏障,采用改进Franz扩散池,比较康倍得公司研制的可乐定透皮贴剂(C-TTS)、美国的可乐定透皮贴剂(Catapres-TTS)和国内的可乐定透皮贴剂(N-TTS)的体外透皮性能.检测方法为高效液相色谱法.结果:C-TTS与Catapres-TTS两种贴剂体外经皮渗透曲线符合零级方程(Q=kt),两者透皮速率无显著性差异(P>0.05);N-TTS体外经皮渗透曲线符合Ritger-peppas方程(Q=ktm),其透皮速率与C-TTS比较有显著性差异(P<0.01).3种样品试验结束揭去贴片后,皮肤中有一定的药物残留量,并且残留量与贴片面积呈线性关系.结论:C-TTS可以维持7d的恒定经皮渗透,与Catapres-TTS体外透皮行为相似.

Study of the percutaneous permeability of clonidine transdermal patch in vitro

Objective:To assess the percutaneous permeability of C-TTS (Compete Pharmaceutical Technology,China) in comparison with Catapres-TTS (USA) and N-TTS (China) through the dissected Guinea-pig skin in vitro. Methods:By a modified Franz diffusion pool and HPLC,the three sources of clonidine were investigated. Results:The cumulative permeation curves of C-TTS and Catapres-TTS were demonstrated to be a zero order equation (Q = kt). Both permeation rates had no significant difference (P>0. 05). The cumulative permeation curve of N-TTS was consistent with Rit-ger-peppas equation (Q = ktm). The permeation rates of N-TTS had a significant difference compared with the one of C-TTS (P < 0. 01). Clonidine residues were detected in the skins after the three sources of the patches were removed from the tested skin. The amount of clonidine residues was linear with the area of the patches covered.Conclusion:The potent efficacy for the percutaneous permeability of the C-TTS was good for 7 days after the placement on the skin. The C-TTS has the similar percutaneous characters in vitro as the Catapres-TTS.