丁香花蕾油作为微乳的油相促进黄芩苷透皮吸收的研究

目的:黄芩苷作为黄芩的主要成分之一,其制剂虽应用广泛,但存在较多缺点,如水溶液不稳定、口服吸收差、生物利用度不高及药物体内半衰期短等从而导致用药剂量大且频繁给药。本文目的是研究丁香花蕾精油及其微乳对黄芩苷体外经皮渗透性的影响。方法:采用Valia-Chien扩散池,以生理盐水为接受液,不同浓度的丁香花蕾精油以及以丁香花蕾精油作为微乳的油相及促进剂进行大鼠离体皮肤的体外渗透实验。结果:黄芩苷微乳的平均粒径为41.3±5.1 nm,多分散指数为0.18,表明该制剂粒径小且均一。微乳(不含丁香花蕾精油)、丁香花蕾精油及含丁香花蕾精油的微乳对黄芩苷均有不同程度的增渗作用。其中,含丁香花蕾精油的微乳对黄芩苷的促渗作用最强。结论:丁香花蕾精油以及以丁香花蕾精油作为微乳的油相对黄芩苷均有一定的促进渗透作用。

Effect of Eugenol in the Microemulsion as an Oil Excipient and Enhancer on Percutaneous Absorption of Baicalin

Objective:As one of the main constituents of Scutellaria baicalensis, the formulation of baicalin has been applied widely, but it has many disadvantages, such as water solution is unstable, poor oral absorption, low bioavailability and short half-life, resulting to high dose and frequent administration. The purpose of this paper is to explore the effects of eugenia oil and its microemulsionformon the transdermal delivery of baicalin.Methods:With saline solution as receptor fluid and eugenia oil of differentconcentrations as enhancers, the modified Valia-Chien diffusion cells were used to evaluate the percutaneous absorption of baicalin in vitro.Results:The average diameter of baicalin microemulsion was 41.3± 5.1 nm, and the polydispersity index is 0.18. Microemulsion (not containing clove bud oil), eugenia oil and microemulsion containing eugenia oil can enhance the transdermal permeability of baicalin to different degrees, but the effects varied. Among them, microemulsion containing eugenia oil is the optimumoption to improve the percutaneous absorption of baicalin at a highest level.Conclusion:Eugenol is an efficient component in the transdermal formulation for improving the skin absorption of baicalin.