Formulation of Berberine Hydrochloride andHydroxypropyl-β-Cyclodextrin Inclusion Complex with EnhancedDissolution and Reduced Bitterness
2013
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°C. 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.
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