[关键词]
[摘要]
目的 制备黄芩苷鼻用凝胶剂,并对其进行体外扩散评价。方法 以卡波姆-936为凝胶基质,以丙三醇为助溶剂,用三乙醇胺调节pH值和黏度,采用正交设计对处方进行优化,并以离体猪鼻黏膜透皮扩散法测定黄芩苷在鼻用凝胶中的释放速率。结果 黄芩苷鼻用凝胶最佳处方为卡波姆-936用量0.5%,丙三醇用量30%,载药量2%;pH值为6.85~7.00,平均黏度1 850~2 350 Pa?s;黄芩苷经猪鼻黏膜扩散符合一级动力学过程,回归方程为Y=0.280 6 X+0.564 3,r=0.997,扩散速率约为0.280 6 μg/(mm2?h)。结论 黄芩苷鼻用凝胶制备工艺简便,黄芩苷主要以简单扩散方式透过鼻黏膜。
[Key word]
[Abstract]
Objective To prepare the nasal gel of baicalin and to evaluate its permeation in vitro. Methods The orthogonal design was carried out using Cabopol-936 as gel matrix, glycerine as solubilizer, and triethanolamine as pH value and viscosity adjuster. The permeating rate of baicalin from nasal gel was determined through pig nasal mucosa in vitro by transdermal diffusion method. Results The optimum nasal gel was made by 0.5% Carbomer-936, 30% glycerine, and 2% baicalin, with pH value 6.85—7.00, and the average viscosity was 1 850—2 350 Pa?s. The permeation of baicalin through nasal mucosa was fitted with first-order kinetics, the regression equation was Y=0.280 6 X+0.564 3, r=0.997, and the permeating rate was 0.280 6 μg/(mm2?h). Conclusion The preparation of baicalin nasal gel is simple. Baicalin is almost permeated through nasal mucosa by simple diffusion.
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[基金项目]
科技部科技人员服务企业行动资助项目(2009GJA10033)