薄荷醇衍生物对荜茇提取物贴剂中胡椒碱体外经皮通透性的影响

Effect of O-acylmenthol derivatives on in vitro skin permeation of piperine from Piperis longi extractum patch

目的研究薄荷醇衍生物对荜茇提取物贴剂中胡椒碱体外经皮通透性的影响,探讨将荜茇提取物制成贴剂的可行性。方法采用卧式双室扩散池,以离体大鼠皮肤作为通透屏障进行体外透皮实验,用HPLC法测定接收池中胡椒碱的浓度。结果戊酸薄荷醇酯、己酸薄荷醇酯、丁酸薄荷醇酯和乳酸薄荷醇酯对胡椒碱经皮吸收有明显的促透效果,其中以戊酸薄荷醇酯的促透效果最好;庚酸薄荷醇酯、十四酸薄荷醇酯和油酸薄荷醇酯的促透作用不明显;薄荷醇对胡椒碱的经皮吸收有抑制作用。结论在含有化学促进剂的贴剂中,胡椒碱的累积透过量及稳态通透速率均显著增加,说明将荜茇提取物制成贴剂是可行的。

Objective To investigate the effects of O-acylmenthol derivatives on in vitro skin permeation of piperine from Piperis longi extractum patch and predict the potential capability of Piperis longi extractum to be formulated in a patch. Methods 2-Chamber diffusion cells were adopted as the apparatus for in vitro skin permeation, excised rat abdominal skin as barrier. HPLC was used to determine the content of piperine in receiver diffusion cell. Results 2-Isopropyl-5-methylcyclohexyl pentanoate, 2-isopropyl-5-methylcyclohexyl hexanoate, 2-isopropyl-5-methylcyclohexyl butyrate and 2-isopropyl-5-methylcyclohexyl-2-hydroxy panoate produced significant enhancing effects on piperine permeation. Of these ,2-isopropyl-5-methylcyclohexyl pen- tanoate had the greatest enhancing effect. 2-Isopropyl-5-methylcyclohexyl heptanoate, 2-isopropyl-5-methylcyclohexyl tetradecanoate and（E）-2-isopropyl-5-methylcyclohexyl octadec-9-enoate had no effect on piperine permeation. Menthol produced an inhibitive effect on piperine permeation. Conclusions The cumulative transport and the flux of piperine increase markedly when chemical enhancers are added in the patches, allowing a rational approach for designing an effective Piperis longi extractum patch.