文献类型：期刊文献

中文题名：盐酸小檗碱胃漂浮海藻酸钙微球的制备与质量评价

英文题名：Preparation and quality evaluation of berberine hydrochloride gastric floating calcium alginate microspheres

作者：熊慧敏[1];陈安琪[1];于华[2];张琳[1]

第一作者：熊慧敏

机构：[1]北京联合大学特殊教育学院,北京100075;[2]泰投华信(北京)科技发展有限公司,北京100018

第一机构：北京联合大学特殊教育学院

年份：2022

卷号：37

期号：2

起止页码：88-93

中文期刊名：西北药学杂志

外文期刊名：Northwest Pharmaceutical Journal

收录：CSTPCD

语种：中文

中文关键词：盐酸小檗碱;胃漂浮海藻酸钙微球;乳化-交联固化法;包封率;漂浮时间

外文关键词：berberine hydrochloride;gastro retentive floating calcium alginate microspheres;emulsification-crosslinking curing method;encapsulation efficiency;floating time

摘要：目的制备盐酸小檗碱胃漂浮海藻酸钙微球并评价其质量。方法采用乳化-交联固化法将盐酸小檗碱制备成胃漂浮海藻酸钙微球,通过单因素实验考察橄榄油用量对盐酸小檗碱胃漂浮海藻酸钙微球的药物包封率和漂浮能力的影响,并以海藻酸钠质量浓度(X_(1))、氯化钙(CaCl_(2))质量浓度(X_(2))和壳聚糖质量浓度(X_(3))作为变量因素,以包封率(Y)作为评价指标,使用Box-Behnken实验设计优化得到海藻酸钙微球的最优处方;测定了海藻酸钙微球的平均粒径及密度;通过扫描电镜观察微球的表面及内部微观结构;评价微球的漂浮率、漂浮时间以及体外药物释放速率。结果经实验优化得到盐酸小檗碱胃漂浮海藻酸钙微球的最佳处方组成为:橄榄油用量占比为15%,海藻酸钠质量浓度为33.0 mg·mL^(-1),CaCl_(2)质量浓度为10.0 mg·mL^(-1),壳聚糖质量浓度为10.0 mg·mL^(-1);海藻酸钙微球的平均粒径为(1.24±0.07)mm,密度为(0.93±0.05)g·cm^(-3);在扫描电镜下可观察到微球表面粗糙,内部呈多孔状;微球在pH1.2盐酸溶液中可连续漂浮12 h,漂浮率为100%,释放机制符合Higuchi方程。结论将盐酸小檗碱制备成胃漂浮海藻酸钙微球,处方设计合理,生产工艺可行,漂浮时间较长,药物释放平稳,有望进一步开发研究。
Objective To prepare berberine hydrochloride gastric floating calcium alginate microspheres and to evaluate the quality.Methods The emulsification-crosslinking and solidification method was used to prepare berberine hydrochloride into gastric floating calcium alginate microspheres.The effect of the concentration of olive oil on the encapsulation efficiency and floating ability of calcium alginate microspheres was investigated through a single factor experiment.The sodium alginate concentration(X_(1)),CaCl_(2) concentration(X_(2))and chitosan concentration(X_(3))were used as variable factors,and the encapsulation efficiency(Y)was used as evaluation indicators,using Box-Behnken experiment design optimization to obtain the optimal formulation of calcium alginate microspheres.The average particle size and density of calcium alginate microspheres were determined.The surface and internal microstructure of the microspheres were observed under scanning electron microscope.And the floating rate,floating time and in vitro release rate of the microspheres were evaluated.Results The optimal formulation composition of berberine hydrochloride gastric floating calcium alginate microspheres was as follows:the ratio olive oil was 15%,the concentration of sodium alginate was 33.0 mg·mL^(-1),the concentration of CaCl_(2) was 10.0 mg·mL^(-1),and the concentration of chitosan was 10.0 mg·mL^(-1).The average particle size of calcium alginate microspheres was(1.24±0.07)mm,and the density was(0.93±0.05)g·cm^(-3).It could be observed under the scanning electron microscope that the surface of the microspheres was rough and the inside was porous.The microspheres could float continuously for 12 hours in the pH1.2 hydrochloric acid solution,the floating rate was 100%,and the release mode conformed to the Higuchi equation.Conclusion In this study,berberine hydrochloride was prepared into gastric floating calcium alginate microspheres with a longer floating time and stable drug release,which was expected to be further developed and studied.