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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 |
