四逆软膏剂基质处方优化与体外渗透性研究  

Optimization of Matrix Formulation and in Vitro Permeability of Sini Plaster

作　　者：李明杰 孙芮芮 李慧峰 李国艳 曾桐春 裴妙荣 LI Mingjie;SUN Ruirui;LI Huifeng;LI Guoyan;ZENG Tongchun;PEI Miaorong(Shanxi University of Chinese Medicine,Jinzhong 030619,Shanxi,China)

机构地区：[1]山西中医药大学,山西晋中030619

出　　处：《辽宁中医药大学学报》2020年第11期43-49,共7页Journal of Liaoning University of Traditional Chinese Medicine

基　　金：国家自然科学基金(81373546)。

摘　　要：目的采用L16(54)正交试验法对四逆软膏剂基质处方进行优化;并考察不同种类促渗剂对其体外透皮特性的影响,优选适宜最佳促渗剂。方法在前期预实验基础上,依据膏体的均匀性、软硬程度、37℃融化性、黏稠度为综合指标对四逆软膏剂基质处方进行优化;采用改良Franz扩散池法,以苯甲酰新乌头原碱、甘草苷、甘草酸铵、6-姜酚的单位累积渗透量为检测指标,考察1%、2%、3%、5%(氮酮、干姜挥发油)透皮促渗剂对四逆软膏有效成分体外经皮渗透性的影响。结果四逆软膏剂基质最佳组合为甘油∶凡士林∶羊毛脂∶液体石蜡(1.0∶0.4∶0.15∶0.2);3%氮酮对指标成分的促渗效果最好,苯甲酰新乌头原碱、甘草苷、甘草酸铵、6-姜酚的体外透皮速率依次是0.2486、0.0649、0.0266、1.5830μg/(cm^2·h)。结论制备的四逆软膏膏体细腻有光泽,软硬、黏性适中,手触之无膏体残留,融化性良好。具有较好的释药性能与透皮性,透皮性能符合零级动力学方程。Objective To optimize the formulation of Sini Plaster matrix by L16(54)orthogonal test.The effects of different kinds of permeability promoters on transdermal properties in vitro were investigated.Methods On the basis of preliminary experiments,the matrix prescription of Sini Plaster was optimized according to the comprehensive indexes of uniformity,hardness,melting at 37℃and viscosity.Using the modified Franz diffusion cell method,the unit cumulative osmotic amount of benzoyl new aconitine base,glycyrrhizin,ammonium glycyrrhizinate,and 6-gingerol as the detection indexes,the effects of 1%,2%,3%,5%(azone,dry ginger volatile oil)transdermal permeability promoting agents on the transdermal permeability of the effective components of tetrafil plaster in vitro were investigated.Results The best combination of tetramine paste matrix was glycerine∶vaseline∶lanolin∶liquid paraffin(1.0∶0.4∶0.15∶0.2).The transdermic rate of benzoyl new aconitine base,glycyrrhizin,ammonium glycyrrhizinate,6-gingerol in vitro was 0.2486,0.0649,0.0266,1.5830μg/(cm2·h),respectively.Conclusion The prepared Sini Plaster paste is smooth and shiny,with moderate hardness and viscosity.It has good drug release and transdermal properties,and the transdermal properties conform to the zero order kinetic equation.

关 键 词：正交试验 四逆软膏剂 透皮促渗剂 透皮扩散试验 

分 类 号：R284[医药卫生—中药学]