不同促渗剂对盐酸氨酮戊酸原位凝胶体外透皮吸收的影响

目的：研究不同透皮促渗剂对盐酸氨酮戊酸原位凝胶体外透皮吸收的影响，为筛选最佳透皮促渗剂提供实验依据。方法：采用Franz扩散池法，以离体大鼠皮肤为模型，选择3种常用透皮促渗剂月桂氮芯卓酮（azone，AZ）、丙二醇（propylene glycol，PG）、二甲亚砜（dimethyl sulfoxide，DMSO），分别考察单一促渗剂及二元促渗剂对盐酸氨酮戊酸原位凝胶体外透皮吸收的影响。结果：含促渗剂盐酸氨酮戊酸原位凝胶体外透皮吸收显著高于未添加促渗剂盐酸氨酮戊酸原位凝胶及市售制剂；采用单一促渗剂时，1% PG促渗效果最好；采用二元促渗剂时，3% AZ+1% PG促渗效果最好；3% AZ+1% PG促渗效果优于1% PG，含促渗剂3% AZ+1% PG的盐酸氨酮戊酸原位凝胶透皮性优于市售制剂艾拉。结论：添加促渗剂的方法能够显著改善盐酸氨酮戊酸的体外透皮吸收性，3% AZ+1% PG构成的二元促渗剂用于盐酸氨酮戊酸原位凝胶促渗效果最佳；本研究为设计优良的盐酸氨酮戊酸经皮给药系统药物奠定了重要基础。

Effects of different permeation enhancers on in vitro transdermal absorption of 5-aminolevulinic acid hydrochloride in situ gel

OBJECTIVE To investigate the effects of various permeation enhancers on in vitro transdermal absorption of 5-aminolevulinic acid hydrochloride in situ gel,and provide experimental evidences for the selection of best penetration enhancers.METHODS The franz diffusion cell method and model of excised mouse back skin were used to evaluate the effects on in vitro transdermal absorption of 5-aminolevulinic acid hydrochloride in situ gel from azone (AZ),propylene glycol (PG),dimethyl sulfoxide (DMSO),separately or in combination.RESULTS The 5-aminolevulinic acid hydrochloride in situ gel contained permeation enhancer showed better transdermal absorption than that without permeation enhancer.When applied individually,1% PG showed the best enhancing effects on transdermal permeability.When applied in combination,3% AZ + 1% PG showed the best enhancing effects on transdermal permeability.And 3% AZ + 1% PG performed the better transdermal permeability than 1% PG.5-aminolevulinic acid hydrochloride with permeation enhancers 3% AZ + 1% PG showed better transdermal permeability than the listed preparation Aila.CONCLUSION The permeation enhancers added successfully enhance the transdermal absorption of 5-aminolevulinic acid hydrochloride in situ gel.And 3% AZ + 1% PG would be the best effective permeation enhancers.This study lays a foundation for the development of a good transdermal absorption drug of 5-aminolevulinic acid hydrochloride.