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目的:为了促进益肤凝胶主要有效成分丹皮酚透皮吸收,本文考察了多种透皮促进剂对凝胶中丹皮酚体外透皮吸收的影响。方法:以小鼠离体皮肤微渗透屏障,采用Franz扩散池装置进行体外透皮实验,运用HPLC法测定接受池中药物累积透过量,考察不同接受液与不同透皮促进剂对凝胶中有效成分丹皮酚透皮吸收的影响,筛选最佳透皮促进剂的种类和浓度。结果:以甲醇/生理盐水(1:1)为接受液,渗透速率Js(4.5501±0.4583μg/(cm2.h))明显高于其他接受液(P<0.05);氮酮(Azone)与棕榈酸乙酯(EPM)促进不大(P>0.05),油酸(OA)与丙二醇(PG)明显对促进凝胶中丹皮酚透皮吸收(P<0.05,P<0.01),且丙二醇(PG)为促渗透效果最佳,浓度为5%时,对丹皮酚的促透作用最强,皮肤滞留量最高。结论:5%浓度的丙二醇可促进凝胶中丹皮酚的透皮吸收,可作为本制剂的透皮促进剂。
OBJECTIVE: In order to promote the transdermal absorption of paeonol, the main active ingredient of the benefit skin gel, the effects of various skin penetration enhancers on the transdermal absorption of paeonol in the gel were investigated. Methods: The in vitro dermal micro-osmotic barrier of mice was used. The Franz diffusion cell was used for in vitro transdermal experiments. The cumulative permeation of drug in the receiving pool was measured by HPLC. The effects of different receiving fluids and different transdermal accelerators on the gel were investigated Ingredients Paeonol transdermal absorption, screening the best type and concentration of transdermal enhancers. Results: The permeation rate Js (4.5501 ± 0.4583μg / (cm2.h)) was significantly higher than that of other solutions (P <0.05) with methanol / saline (1: 1) (P <0.05, P <0.01), while propylene glycol (OA) and propylene glycol (PG) significantly promoted the transdermal absorption of paeonol in the gel, PG) to promote the penetration of the best effect, the concentration of 5%, the most effective penetration of paeonol, the highest retention of the skin. Conclusion: 5% propylene glycol can promote the transdermal absorption of paeonol in the gel and can be used as transdermal enhancer of this preparation.