驻极体利多卡因贴剂的透皮促渗作用

目的:研究驻极体对利多卡因透皮吸收的促渗作用。方法:利用Franz扩散池和高效液相色谱法测定利多卡因贴剂、含不同浓度氮酮利多卡因贴剂、正/负极性驻极体利多卡因贴剂和含不同浓度氮酮的正/负极性驻极体利多卡因贴剂在10 h内的体外大鼠皮肤累积渗透量,研究驻极体对利多卡因的透皮促渗作用。结果:(1)含1%、3%和5%氮酮的利多卡因贴剂的10 h药物累积渗透量分别是利多卡因贴剂的1.06、1.10、1.66倍(5%氮酮组有统计学差异，P＜0.05)。(2)含1%、3%和5%氮酮的负极性驻极体利多卡因贴剂与相应的含化学促渗剂利多卡因贴剂具有类似的促渗效果。(3)含1%、3%和5%氮酮的正极性驻极体利多卡因贴剂与相应的化学促渗剂利多卡因贴剂相比,具有更大的增渗倍数(P＜0.05 或P<0.01),且5%氮酮与正极性驻极体对利多卡因的透皮吸收有联合促渗作用。结论:正极性驻极体对利多卡因贴剂有更好的促渗效果,氮酮与正极性驻极体对利多卡因透皮吸收有联合促渗作用,并与氮酮的浓度有关。

Enhancing effects of electret on transdermal delivery of lidocaine patches in vitro

Objective:To study the enhancing effects of electret on transdermal delivery of lidocaine patches in vitro.Methods:In vitro rat skin permeation experiment was carried out with lidocaine patches,lidocaine paches with azone,positive/negative electret lidocaine patches,and positive/negative electret lidocaine patches with azone by using Franz diffusion cells.The accumulated lidocaine concentrations in rat skin treated with each kind of patches were examined by HPLC to investigate the influence of electret on transdermal delivery of lidocaine.Results:(1) The enhancement rates of 1%,3% and 5% azone lidocaine patches 10 h after application were 1.06,1.10 and 1.66 folds (P<0.05,5% azone vs lidocaine patch group) that of the lidocaine patch,respectively.(2) Lidocaine patches with negative electret containing 1%,3% and 5% azone showed similar transdermal behavior to the corresponding chemical enhancer patches.(3) Lidocaine patches with positive electret containing 1%,3% and 5% azone showed much better enhancing effect than the corresponding chemical enhancer lidocaine patches (P<0.05). Besides,5% azone together with positive electret showed a cooperative enhancing effect.Conclusion:Positive electret patch has better effect in enhancing transdermal delivery of lidocaine.Besides,the cooperative enhancing effect of azone with positive electret on transdermal delivery of lidocaine is in a concentration-dependent manner with azone.