丹皮酚凝胶处方优选及结晶行为研究

目的：优选丹皮酚凝胶处方并考察其结晶行为。方法：摇瓶法测定丹皮酚在不同乳化剂及助乳化剂中的饱和溶解度；结合凝胶外观及药物结晶情况，分别优选凝胶处方中的乳化剂、助乳化剂及凝胶材料；采用Franz扩散池法考察丹皮酚凝胶及软膏在离体小鼠皮肤的渗透及滞留；比较丹皮酚凝胶及软膏在放置过程中的结晶行为。结果：丹皮酚在不同乳化剂及助乳化剂中的溶解度均显著优于纯水；以10%丙二醇单辛酸酯为乳化剂、5%甘油为助乳化剂、1%卡波姆934为凝胶材料制得的丹皮酚凝胶较稳定，其小鼠离体皮肤透过率及滞留量均优于市售软膏，且放置1个月未观察到与软膏类似的结晶行为。结论：所得丹皮酚凝胶的透皮性能及结晶稳定性均优于软膏。

Research on the formulation optimization and crystallization behaviors of paeonol gel

OBJECTIVE To optimize the formulation and investigate the crystallization behaviors of paeonol gel.METHODS The solubility of paeonol in different emulsions and co-emulsions was determined by shaking flask method.The emulsion,co-emulsion,composite emulsion/co-emulsion and gel materials were optimized to prepare paeonol gel by observing the crystallization under a microscope.The behaviors of in vitro skin penetration and retention of paeonol gel and ointment were investigated on mouse skin by Franz diffusion method.The crystallization behaviors of paeonol gel and ointment were compared at 40℃ and 20℃,respectively.RESULTS The solubilities of paeonol in emulsion and co-emulsion were significantly superior to that in water.The optimal formulation of paeonol gel was prepared with 10% capryol 90 as emulsion,5% glycerin as co-emulsion and 1% carbopol 934 as gel material.The higher skin penetration and drug retention per unit area were obtained in paeonol gel compared with ointment and the crystallization behaviors of paeonol gel were superior to those of ointment.CONCLUSION The formulation of paeonol gel is optimized and stability and transdermal permeation are all better than those of ointment.