仁术微乳凝胶膏剂的制备

Preparation of Renzhu Microemulsion Cataplasm

目的将仁术脐贴基质改制成微乳凝胶膏剂,并通过其透皮吸收与止泻作用进行验证。方法制备仁术处方(砂仁、苍术、肉桂、丁香)挥发油微乳,正交试验考察聚丙烯酸钠(NP-700)、聚乙烯吡咯烷酮(PVP-K90)、甘羟铝、甘油用量对制备工艺的影响。以桂皮醛和丁香酚为指标,改良的Franz扩散池法研究凝胶膏剂的体外透皮吸收。通过番泻叶致小鼠腹泻模型,评价凝胶膏剂的止泻作用。结果最佳条件为0.4 g PVP-K90,1.0 g NP-700,0.08 g甘羟铝,6 g甘油。与仁术脐贴比较,凝胶膏剂中桂皮醛、丁香酚的透皮吸收速率分别提高了3.54、4.06倍,24 h累积透过率分别提高了2.86、2.84倍。其止泻作用显著优于同浓度低剂量仁术脐贴(含0.97%挥发油),并与后者高剂量(含10%挥发油)相当。结论所制备的仁术微乳凝胶膏剂透皮吸收快、止泻效果好、皮肤相容性佳,兼备微乳与凝胶膏剂的优点。

AIM To change the umbilical paste substrate of Renzhu Formula into microemulsion cataplasm and to verify its percutaneous absorption and antidiarrheal effect. METHODS Orthogonal test was used for investigating the effects of varied dosages of sodium polyacrylate（ NP-700）,polyvinyl pyrrolidone（ PVP-K90）,aluminium glycinate and glycerin on the microemulsion process of volatile oils extracted from Renzhu Formula. With cinnamaldehyde and eugenol as indicative constituents,modified Franz diffusion cell was applied to studying the in vitro percutaneous absorption of cataplasm. The cataplasm＇s antidiarrheal effect was evaluated through diarrhea mice model induced by senna. RESULTS The optimal conditions were determined to be 0. 4 g PVP-K90,1. 0 g NP-700,0. 08 g aluminium glycinate and 6g glycerin. The percutaneous absorption rates of cinnamaldehyde and eugenol in cataplasm were increased to 3. 54 times and 4. 06 times more than those in Renzhu Umbilical Paste,and the 24 h accumulated penetrating rates of them were increased to 2. 86 times and 2. 84 times more,respectively. The microemulsion cataplasm displayed its antidiarrheal superiority than low-dosed Renzhu Umbilical Paste at the same concentration（ containing 0. 97% volatile oil）,which was almost similar to the high dose paste（ containing 10% volatile oil）. CONCLUSION With rapid percutaneous absorption,good antidiarrheal effect and ideal skin compatibility,the prepared Renzhu Microemulsion Cataplasm has the quality of both microemulsion and cataplasm.