PHASE SOLUBILITY STUDIES OF THE
INCLUSION COMPLEXES OF REPAGLINIDE
WITH β-CYCLODEXTRIN AND
β-CYCLODEXTRIN DERIVATIVES.
CAMELIA NICOLESCU*, CORINA ARAMĂ, ANGELA NEDELCU,
CRINA-MARIA MONCIU
Analytical Chemistry Department, Faculty of Pharmacy, UMF Carol
Davila, Traian Vuia Street no. 6, Bucharest, Romania
*corresponding author: nicolescu_camelia@yahoo.com
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Abstract:
The present study is intended to evaluate the possibilities to improve repaglinide - an oral antidiabetic drug - solubility in water, based on inclusion complexes formation with β-cyclodextrin (β-CD), hydroxypropyl β-cyclodextrin (HP-β-CD) and randomly methylated β-cyclodextrin (RAMEB), respectively, and also to estimate their composition and apparent stability constants, Kst, from the phase-solubility diagrams.
We have noticed that the phase solubility diagram for the repaglinide – HP-β-CD inclusion complex is A type, while those of repaglinide - β-CD and RAMEB are B type.
Taking into account the lipophilicity of the zwitterionic structure of repaglinide, all determinations were performed in buffered phosphate solutions (pH 6). The phase-solubility diagrams indicate an enhancement of the repaglinide solubility in the presence of β-CD, as well as its derivatives, HP-β-CD and RAMEB in different extents, related to the type of cyclodextrin.
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