Formulation of Berberine Hydrochloride and Hydroxypropyl-&#946-Cyclodextrin Inclusion Complex with Enhanced Dissolution and Reduced Bitterness

作者：Shengjie Ma, Yuhua Wang, Xu Shang, Fei Yan · 发表于：Tropical Journal of Pharmaceutical Research · 年份：2013 · DOI：10.4314/tjpr.v11i6.1 · 被引用次数：7 · 研究领域：Drug Solubulity and Delivery Systems、Berberine and alkaloids research、Drug Transport and Resistance Mechanisms

Purpose: To prepare and characterize inclusion complex of berberine hydrochloride with hydroxypropyl-â-cyclodextrin in order to achieve enhanced solubility and reduced bitterness of the former.Methods: The inclusion complex of berberine hydrochloride with hydroxypropyl-â-cyclodextrin (1:1) was prepared by freeze-drying method and compared with the the physical mixtures of the compounds. Inclusion complexation was studied by phase solubility diagram, differential thermal analysis, spectrophotometric characterization and dissolution rate. The solubility of the formulations was evaluated by saturation solubility studies while their bitterness was tested in human volunteers.Results: Differential thermal analysis and spectrophotometric characterization indicate that berberine hydrochloride formed inclusion complex with hydroxypropyl-â-cyclodextrin. The phase solubility diagramof berberine hydrochloride with hydroxypropyl-â-cyclodextrin was of AL-type, with a stability constant was 694.5 L/mol at 25 oC. The solubility of berberine hydrochloride was increased by 5.27 times for thecomplex at a concentration of 0.01 mol/L. The dissolution of berberine hydrochloride after 20 min from the inclusion complex, physical mixture and pure berberine hydrochloride was 89.6, 69.8 and 58.8 %, respectively. The bitterness of the inclusion complex was considerably lower than that of the drug alone or the physical mixture with hydroxypropyl-â-cyclodextrin.Conclusion: The inclusion complex demonstrat...