盐酸小檗碱鼻用凝胶的研究

Studies on nasal gel of Berberine Hydrochloride

关键词:  盐酸小檗碱  卡波姆  鼻用凝胶  药物释放

Key words:  berberine hgdrochloride  carbopol  nasal gel  drug release

摘要:

[目的] 小檗碱具有神经保护作用，特别对神经退行性疾病具有良好的治疗效果，鼻腔给药为一种向脑输送药物的新途径，药物滴人鼻腔后能传人脑脊液达到治疗神经的目的，设计一种盐酸小檗碱鼻用凝胶剂，并对其进行体外扩散评价. [方法] 以卡伯姆-980为凝胶基质，以丙三醇为潜溶剂，用三乙醇胺调节pH和黏度，采用正交设计对处方进行优化，用紫外分光光度法测定体外溶出，并溶出数据进行Weibull概率拟合. [结果] 盐酸小檗碱鼻用凝胶最佳处方为卡波姆-980浓度0.2%，载药量1%，pH在6.0～7.0范围内，平均黏度约为1 000～1 200 mPa·s，体外溶出结果经Weibull概率模型拟合，其T_d值为104.8 min.[结论] 以生物黏附性材料卡波姆-980为基质制备盐酸小檗碱鼻用凝胶，处方简单，质量稳定，药物释放平稳.

Abstract:

[Objective] To design a kind of nasal gel of berberine and inspect the quality of it in vitro. Nasal administration is a new way to deliver drugs to the brain. The drug can transport into cerebrospinal fluid after nasal drops to treat Neurodegenerative diseases. [Methods] In order to optimize the prescription the orthogonal design was carried out. The experiment used Cabarbopol-980 as gel base, triethanolamine as pH and viscosity adjuster, and glycerin as cosolvent. The release of berberine from nasal gel was determined by UV and the curve was fitted by Weibull model. [Results] The optimum nasal gel was made by Carbopol-980 0.1%, berberine 1%, appearance pH was adjusted to 6.0～7.0, the average viscosity was about 1 200 mPa·s. The release curve of berberine fitted by Weibull showed that T_d was 104.8 min. [Conclusion] Using bioadhesive material carbopol-980 to make nasal gel of berberine is easy to operate and control. The release of berberine is stable.