盐酸小檗碱自微乳剂的处方设计及体外评价

Formulation Design and in vitro Evaluation of Berberine Hydrochloride self-microemulsion

目的:制备盐酸小檗碱自微乳剂,并对其质量及体外溶出度进行考察。方法:通过正交设计和伪三元相图优化处方,分别以乳化程度、乳化速度、有无油层及混合分层情况为指标,对自微乳化系统中的油相、乳化剂及助乳化剂的组成和用量进行研究,筛选盐酸小檗碱自微乳剂的最佳组成及比例。采用紫外分光光度法进行质量评价,并考察其溶出度。结果:盐酸小檗碱自微乳剂组成为盐酸小檗碱-油酸乙酯-聚氧乙烯(40)氢化蓖麻油-聚乙二醇-400 0.015∶0.120∶0.160∶0.120;乳滴粒径80.59 nm;在质量考察中,盐酸小檗碱在4.49～22.44 mg·L-1和吸光度呈良好线性关系,r=0.999 9,平均回收率100.9%,RSD 1.65%,样品平均质量分数97.4%,RSD 0.84%。在人工胃液中20 min的溶出度>80%,远高于市售片剂。结论:自微乳剂能够改善盐酸小檗碱难溶性,且制备工艺简单,具有良好应用前景。

Objective： To prepare berberine hydrochloride self-microemulsion, and investigate its quality and in vitro dissolution. Method： Prescription was optimized by orthogonal design and pseud0=ternary phase diagram with degree of emulsification, emulsion speed, oil layer and mixed-layered as indexes, prescription composition and dosage of oil phase, emulsifier and co-emulsifier from self-microemulsion system were studied, to select optimum composition and proportion of BR-SMEDDS. UV spectrophotometry was used to assess quality of BR-SMEDDS and investigate its dissolution. Result： Optimum formulations of BR-SMEDDS were composed of BR- ethyl oleate-cremophor RH40-PEG 400 0. 015： 0. 120： 0. 160： 0. 120. Particle size of droplet was 80.59 nm. In inspection of quality, The concentration of berberine hydrochloride showed a good linear relationship in 4. 488- 22.44 mg. L-1 with absorbance （r = 0. 999 9） , average recovery was 100.9% , RSD 1.65%. The average content of samples was 97.4% , RSD 0. 84%. Dissolution of BR-SMEDDS in artificial gastric juice was 80% in 20 min, it was higher than commercial tablets. Conclusion： BR-SMEDDS could improve dissolution of BR, and the preparation technology was simple, it would have a good applicable prospect.