利多卡因-月桂醇二元共熔系统的体外经皮渗透

In vitro transdermal permeation of lidocaine-dodecanol binary eutectic system

目的研究利多卡因-月桂醇二元共熔系统对利多卡因经皮渗透的影响。方法制备不同比例的利多卡因月桂醇二元共熔混合物和含二元共熔混合物的透皮贴剂。测定了利多卡因和利多卡因月桂醇二元共熔混合物在pH7.9的磷酸盐缓冲液的溶解度。以Franz类型的单室扩散池测定利多卡因及利多卡因月-桂醇二元共熔混合物贴剂的体外透皮性能。结果利多卡因-月桂醇二元共熔混合物的熔点明显比利多卡因低。含利多卡因月桂醇二元共熔混合物贴剂中利多卡因的稳态透皮速率是纯利多卡因贴剂的6倍。结论利多卡因-月桂醇二元低共熔混合物中的利多卡因具有较高的热力学活性,从而显著提高了利多卡因的体外透皮速率。

Aim To study the effect of lidocaine-dodecanol binary eutectic system on the transdermal permeation of lidocaine. Methods Binary eutectic mixture of different proportions of lidocaine and dodecanol were prepared and the patch containing the binary eutectic mixture was developed. The solubilities of pure lidocaine and lidocaine from the binary eutectic system were determined in pH 7.9 phosphate buffer. The transdermal flux of lidocaine from the patches containing the binary eutectic system and pure lidocaine were measured using Franz-type single diffusion cell. Results The melting point of the lidocaine-dodecanol binary eutectic system was markedly lower than that of pure lidocaine. The steady state transdermal flux of lidocaine from the patch of the binary eutectic system was six times as much as that of pure lidocaine patch. Conclusion The lidocaine-dodecanol binary eutectic system could produce thermodynamic activity of the drug and the high driving force for transdermal permeation of lidocaine.