胡巧红,金祝萍,易军,李晓芳
HU Qiao-hong~1,JIN Zhu-ping~2,YI Jun~1,LI Xiao-fang~1(1.Guangdong Pharmaceutical University Guangzhou 510006

• 1:广东药学院
• 2:浙江省临海市第二人民医院
• 3:广东药学院
• 4:广东药学院 广州510006

摘要(Abstract)：

目的研究外加电脉冲的施与方式对小分子解离型药物盐酸丁卡因经皮渗透速率的影响。方法以盐酸丁卡因为小分子离子型模型药物,应用水平双室扩散池,大鼠腹部皮肤,研究使用多个脉冲时,外加脉冲的施与方式对药物体外电穿孔经皮渗透速率的影响,并与被动扩散和离子导入进行比较。结果电穿孔(方波脉冲,脉冲电压为130 V,脉冲率为40 pu lses.m in-1,脉冲时间为0.4 s)可显著提高盐酸丁卡因的经皮渗透速率,且电穿孔的促渗作用显著大于离子导入(0.2 mA.cm-2,4 h)。400个脉冲时,施加脉冲方式对经皮渗透速率无显著影响。200个脉冲时,施加脉冲后0.25 h和0.75 h时一次施加和分两次施加的经皮渗透速率没有显著性差异,随后一次施加脉冲的经皮渗透速率显著大于分两次加脉冲的经皮渗透速率。结论电穿孔可显著促进盐酸丁卡因的经皮渗透,且促渗效果优于离子导入;脉冲施与方式对盐酸丁卡因电穿孔经皮渗透速率的影响与所加的脉冲数有关。
Objective To study the influence of pulse mode on the electroporative fluxes of tetracaine hydrochloride,a small molecule ionic drug,through rat skin.Method Using side-by-side compartment cells,rat abdominal skin,tetracaine hydrochloride as a model of small molecule ionic drugs, the effect of pulse mode on the in vitro electroporative fluxes of drug was investigated,and compared with passive diffusion and iontophoresis.Result The fluxes of tetracaine hydrochloride were obviously increased by electroporation(square wave pulses,pulse frequency: 40 pulses·min~(-1),pulse time: 0.4 s).The enhancing effect of electroporation was greater than iontophoresis(0.2 mA·cm~(-2),4 h).There were no obvious difference between the electroporative fluxes by total 400 pulses given at a time and those by total 400 pulses given twice.There were no obvious difference between the electroporative fluxes at 0.25 h or 0.75 h,by total 200 pulses given at a time and those by total 200 pulses given twice.From then on,there were obvious differences between them.The electroporative fluxes of tetracaine hydrochloride by total 200 pulses given at a time were greater than those by total 200 pulses given twice.Conclusion: The percutaneous permeation of tetracaine hydrochloride was obviously increased by electroporation.The enhancing effect of electroporation was greater than iontophoresis.The influence of pulse mode on the fluxes of tetracaine hydrochloride was related to pulse number.

关键词(KeyWords)： 电穿孔;盐酸丁卡因;经皮渗透
electroporation;tetracaine hydrochloride;percutaneous permeation

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 胡巧红,金祝萍,易军,李晓芳
HU Qiao-hong~1,JIN Zhu-ping~2,YI Jun~1,LI Xiao-fang~1(1.Guangdong Pharmaceutical University Guangzhou 510006

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