止痛微乳凝胶膏的制备及体外评价

目的探讨微乳技术对凝胶膏中药物释放及透皮性能的影响。方法以初黏力、180°剥离强度和综合感官评分为指标,结合单因素实验与星点设计-效应面法优选止痛微乳凝胶膏处方。采用改良Franz扩散池法,以有效成分阿魏酸和欧前胡素为指标,对比微乳凝胶膏和普通凝胶膏体外释放和经皮渗透性能。结果最终优选出基质配方为NP700,卡波姆-941,卡波姆-934,铝化合物,酒石酸,丙三醇(1∶0.1∶0.25∶0.04∶0.04∶6)。2种凝胶膏中有效成分的体外释放均符合零级动力学方程,具有扩散和溶蚀的双重机制。微乳凝胶膏和普通凝胶膏中阿魏酸的透皮速率分别为1.92、0.97μg/(h·cm2),欧前胡素的透皮速率分别为0.28、0.09μg/(h·cm2)。与普通凝胶膏相比,微乳凝胶膏中有效成分的累积透过率成倍数增加。结论微乳技术能促进凝胶膏中药物的经皮渗透。

Preparation and in vitro evaluation of analgesic microemulsion cataplasm

Objective To investigate the influence of microemulsion technology on release capability and transdermal permeability of components in cataplasm. Methods With the initial bonding strength, 180 degree force strength and sensory evaluation scores as indicators, the formula of the analgesic microemul-sion cataplasm matrix was optimized by using single factor experiment combined with central composite de-sign-response surface design methodology. Modified Franz diffusion cell was used to compare the release capability and transdermal permeability between analgesic microemulsion cataplasm ( MEC) and analgesic common cataplasm ( CC) with indicators of ferulic acid and imperatorin. Results Optimized matrix formu-la was NP700, carbomer 941, carbomer 934, aluminum compounds, tartaric acid and glycerin with the rati-o of 1∶0. 1∶0. 25∶0. 04∶0. 04∶6 . The release capability in vitro of ferulic acid and imperatorin in MEC and CC conformed to zero-order kinetic equation with a dual mechanism of diffusion and dissolution. The stead-y-state permeation rate of ferulic acid in MEC was 1. 92 μg/( h·cm2 ) and that in CC was 0. 97 μg/( h· cm2);that of imperatorin in MEC was 0. 28 μg/(h·cm2), while in CC was 0. 09 μg/(h·cm2). Com-pared with CC, the cumulative release rate of effective components multiplied. Conclusion Microemul-sion technology can significantly promote the transdermal permeability of components in cataplasm.