不同促渗剂对氢溴酸高乌甲素贴片体外经皮渗透的影响

目的：研究不同促渗剂单用、合用对氢溴酸高乌甲素贴片的体外透皮促渗作用。方法：采用不同种类和浓度的促渗剂，制备氢溴酸高乌甲素贴片。采用改良Franz扩散池，以人体皮肤为模型，以高效液相色谱法测定接受液中药物含量，进而计算其累积透皮量和稳态透皮速率。结果：3%油酸、氮酮、丙二醇，1%十二醇、肉豆蔻酸异丙酯的促透效果较好，并尤以油酸和氮酮作用更为显著。而氮酮与丙二醇以及与油酸合用时均小于其单用时的效果。此外，促渗剂浓度亦影响氢溴酸高乌甲素的经皮渗透。结论：以氮酮或3%油酸为促渗剂，可以制备得到具有较高透皮速率的氢溴酸高乌甲素贴片。氮酮与其他促渗剂的合用不利于氢溴酸高乌甲素的经皮渗透。

Influence of different penetration enhancers on Lappaconitine transcutaneous permeation

Objective: to investigate the effects of different kinds and concentration of transdermal enhancers on Lappaconitine transcutaneous permeation when used individually or together. Method: Using modified Franz-type diffusion cell and excised human body skin as an in vitro transdermal model, the concentration of lappaconitine was determined by HPLC, then cumulative permeation quantity (Q) and stability rate (J) of progesterone were calculated. Result: Penetration enhancers such as propylene glycol, dodecanol, IPM, and particularly 3% OA and Azone, can significantly enhance the penetration rate of lappaconitine. Concentration effect of penetration enhancers concentration on lappaconitine transcutaneous permeation were found in experiments, the permeation effect of Azone was better than Azone+OA and Azone+propylene glycol. Conclusion: The transdermal rate of lappaconitine from batch which contains 3% OA or Azone is higher than others. Combination of Azone with other penetration enhancers is not recommended for Lappaconitine transcutaneous permeation.