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Research Article


Formulation of Berberine Hydrochloride and Hydroxypropyl-β-Cyclodextrin Inclusion Complex with Enhanced Dissolution and Reduced Bitterness

Suying Ma1*, Yong Wang2, Xiaojun Shang1 and Fulin Yan1

1School of Pharmacy, 2Department of Laboratory Animal Center, Xinxiang Medical University, Xinxiang Henan, 453003, PR China

*For correspondence: Email: : suyingma@163.com  Tel: +86-373-3029879

Received: 18 November 2011                                     Revised accepted: 27 October 2012    

Tropical Journal of Pharmaceutical Research, December 2012; 11(6): 871-877

http://dx.doi.org/10.4314/tjpr.v11i6.1  

Abstract

 

Purpose:  To prepare and characterize inclusion complex of berberine hydrochloride with hydroxypropyl-β-cyclodextrin in order to achieve enhanced solubility and reduced bitterness of the former.

Methods: The inclusion complex of berberine hydrochloride with hydroxypropyl-β-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-β-cyclodextrin. The phase solubility diagram of berberine hydrochloride with hydroxypropyl-β-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 the complex 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-β-cyclodextrin.

Conclusion: The inclusion complex demonstrated improved dissolution properties and lowered the bitterness of berberine hydrochloride.

 

Keywords: Berberine hydrochloride, Hydroxypropyl-β-cyclodextrin, Inclusion complex, Solubility, Bitterness

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