桂皮酸透皮吸收影响因素的研究.doc

桂皮酸透皮吸收影响因素的研究 王海艳*，季宇彬，李文兰，扈正婷，于莹莹 (1.哈尔滨商业大学 生命科学与环境科学研究中心 哈尔滨 150076) 摘 要 目的：通过对桂皮酸在不同药物浓度、接收液、pH值、温度、转速和促渗剂时透皮吸收效果的考察，筛选出桂皮酸透皮吸收效果最佳的条件。方法：采用改良的Franz扩散池，以离体大鼠皮肤为透皮屏障，用高效液相色谱法测定各透皮吸收影响因素对桂皮酸的累积渗透量、透皮吸收速率、透皮时滞等体外透皮吸收动力学参数的影响。对氮酮(Azone)、丙二醇(PG)、油酸(OA)、月桂酸甘油酯(GL)、乙醇(Ethanol)5种透皮吸收促进剂单独应用和合用的促渗效果进行考察。结果：在接收液为10%乙醇-生理盐水，药物浓度为200μg/mL，37℃水浴恒温，pH=7，转速为300r/min时桂皮酸的透皮吸收效果最佳，以1%Azone+0.5%OA+10%GL+10%PG、0.5%OA+10%GL+10%PG、10%GL+10%PG为复合促进剂时吸收速率显著提高，其中以1%Azone+0.5%OA+10%GL+10%PG促渗作用最强。结论：通过考察各影响因素对桂皮酸透皮吸收的影响，为研究其透皮给药提供了参考依据。 关键词：桂皮酸；透皮吸收；促渗剂；HPLC Study on influencing factors of percutaneous absorption of cinnamic acid WANG Hai-yan JI Yu-bin LI Wen-lan HU Zheng-ting YU Ying-Ying (Center of Research on Life Sciences and Environmental Sciences, Harbin University of Commerce, Harbin China 150076,；Engineering research center of natural anticancer drugs, ministry of educatuion, Harbin China 150076) Abstract Objective: Studied the percutaneous absorption effects of cinnamic acid at different concentration, receiving solution, pH value,temperature, rotational speed, and penetration enhancer. Screened the optimum condition of percutaneous absorption. Methods: Improved Franz diffusion cell was adopted as the apparatus for in vitro rats’ skin permeation. Kinetic parameters of percutaneous absorption, such as permeability amount, penetration rate and percutaneous time-delay, were determinated by HPLC. Futher more, azone, propylene glycol, oleic acid, glyceryl monolaurate and ethanol were investigated in percutaneous absorption effects for single or combined use. Results: The optimum condition is 10% 基金项目：黑龙江省科技厅攻关项目(GC05C31601)；黑龙江省教育厅振兴老工业基地项目（1151gzd25）；黑龙江教育厅科学技术研究项目 作者简介：研究方向为Tel E-mail: xuere ethanol in saline as receiving solution, administration concentration is 200μg/mL,37℃,pH value is 7, rotational speed is 300r/min. When (1%Azone,0.5%OA,10%GL and 10%PG), (0.5%OA,10%GL and 10%PG) and (10%GL and 10%PG) are cho