微乳基质对苦参碱经皮渗透的影响

Effects of Microemulsion Components on Cutaneous Permeation of Matrine

以小鼠离体皮肤为模型,采用双室渗透扩散装置考察了微乳中不同的油相、表面活性剂和助表面活性剂对苦参碱经皮渗透的影响。采用HPLC法,以Kromasil NH2为色谱柱、乙腈-无水乙醇-3%磷酸(80:10:10)为流动相测定苦参碱的经皮渗透量。结果表明,油酸对苦参碱有显著的阻碍渗透作用,故油酸不宜作为苦参碱微乳的油相。本试验优化所得的微乳处方为油酸乙酯-丁酸乙酯(4:1,w/w)4.5%,Cremophor EL35-乳化剂OP-10(1:1,w/w)23%,PEG40015%,苦参碱7.2%。

The influences of different kinds of oils,surfactants and cosurfactants in microemulsions on the permeation of matrine were investigated with excised mice skin as the model by a two-compartment diffusion cell.The drug concentration was determined by HPLC with a Kromasil NH2 column and the acetonitrile-anhydrous ethanol-3% phosphoric acid（80：10：10） as mobile phase.The results showed that oleic acid had a significant inhibitive effect on the permeation of matrine.It indicated that oleic acid could not be used as the oil phase.The optimized formulation of the microemulsion was as follows：4.5% ethyl oleate-ethyl butyrate（4：1,w/w） as oil phase,23% Cremophor EL35-OP-10（1：1,w/w） as surfactant,15% PEG 400 as cosurfactant and 7.2% matrine.