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Ternary systems of HP β-cyclodextrin felodipine inclusion complexes: Preparation, characterization and solubility studies

Minal Narkhede Raghunath, , Jitendra Nehete Yadav
Published in
2011
Volume: 4
   
Issue: 12
Pages: 1809 - 1815
Abstract
The aim of this study was to investigate the effect of presence of water soluble polymer, PVP K -25, PEG 6000 and HPMC, on complexation of felodipine with HP $\beta$ CD. Solid complexes at mole ratio 1:1 were obtained by freeze drying method. The phase solubility studies indicated the formation of HP- $\beta$ cyclodextrin complexes at a 1:1M ratio in solution, in presence and absence of water soluble polymers. All complexes were studied by X- ray diffractometry, Differential Scanning Calorimetry, FT-IR spectroscopy and dissolution study. X-ray diffraction data revealed decrement in crystallinity of binary and ternary systems. All DSC curves of binary and ternary systems showed shifting of characteristics melting peaks of pure drug. The process of felodipine complexation with HP $\beta$ CD, in presence of water soluble polymer was shown to involved aromatic ring, the carbonyl groups in ester bonds and carbon atom of DHP (dihydropyridine) linked via ester bonds. One of aim of complexation was to improve drug solubility and hence the dissolution rate of binary and ternary system tested. As result of inclusion complex formation, obtained by freeze drying method, brought dramatic 20 fold increase Felodipine solubility in presence of water soluble polymer HPMC. In photo-stability studies it is observed that upon inclusion complexation of felodipine with HP $\beta$ CD showed dramatic decreases in degradation rate constants and increases in the values of t0.1%. The possible reasons for protection of complexed felodipine against photo degradation could be due to inclusion of dihydropyridine ring into CD cavity where, dihydropyridine ring is involved in the first step of drug photo degradation. In docking of felodipine with cyclodextrin derivative(HP$\beta$ CD), a hypothetical structures of complex also supported inclusion of dihydropyridine ring into CD cavity. {\textcopyright} RJPT All right reserved.
About the journal
JournalResearch Journal of Pharmacy and Technology
ISSN0974360X
Open AccessNo