透皮促渗剂对黄芩总黄酮凝胶膏剂成分体外经皮渗透的影响

目的研究不同透皮促渗剂对黄芩总黄酮凝胶膏剂中总黄酮及其中6种黄酮类成分(黄芩苷、黄芩素、汉黄芩苷、汉黄芩素、千层纸素A苷及木蝴蝶素)体外经皮渗透的影响,为筛选最佳的促渗剂提供实验依据。方法选择3种常用的透皮促渗剂氮酮(azone,AZ)、薄荷醇(menthol,MT)、丙二醇(propylene glycol,PG),采用体外扩散池法考察单一促渗剂与二元复合促渗剂对体外经皮渗透参数的影响。结果采用单一促渗剂时,AZ对苷类成分的促渗效果较好,MT对苷元类成分的促渗效果较好,而PG的促渗效果相对较差,总体以3%AZ对于总黄酮及其单体的促渗能力最强;采用二元复合促渗剂时,促渗效果整体优于单一促渗剂,总体以3%AZ+5%PG渗透效果最佳。结论促渗剂可以显著影响黄芩总黄酮凝胶膏剂中总黄酮及其中6种活性黄酮类成分的经皮渗透动力学参数,3%AZ+5%PG构成的二元复合促渗剂用于黄芩总黄酮凝胶膏剂促渗效果最佳。

Effects of penetration enhancers on in vitro transdermal permeation of components from total flavones in Scutellariae Radix Gel-unguentum

Objective To investigate the effects of common peneration enhancers on the transdermal permeation of total flavones and six flavonoid components from Scutellariae Radix Gel-unguentum (SRGU), thus to provide the experimental evidence for the selection of optimal penetration enhancers. Methods In vitro diffusion cell method was used to evaluate the changes of the transdermal pemeation parameters by azone (AZ), menthol (MT), and propylene glycol (PG), separately or in combination. Results When applied individually, AZ and MT showed the best enhancing effect on the transdermal permeability and cumulative permeation of flavonoids and their aglycons, respectively. PG, in contrast, produced poor enhancement. When applied in combination, the permeation enhancing effects were generally more remarkable than those of single enhancer. In particular, 3% AZ + 5% PG could achieve the most effective enhancement effect on the transdermal permeation of flavonoids. Conclusion Penetration enhancers could significantly affect the transdermal permeation of total flavones and flavonoid components from SRGU in vitro, and 3% AZ + 5% PG may serve as the most effective enhancer.