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Characterisation of Gliclazide-PEG 8000 Solid Dispersions
Abstract
Purpose: The aim of the present study was to characterise gliclazide solid dispersions (SDs) prepared
with polyethylene glycol (PEG) 8000 and compare them with SDs in PEG 6000. Methods: Gliclazide SDs containing varying concentrations of PEG 8000 were prepared using the fusion – solvent technique, and their phase solubility behavior and dissolution in 0.1N HCl were assessed at 37 oC. The physical state of, and gliclazide-PEG interactions in, SDs and physical mixtures prepared in ratios of 1:1, 1:2 and 1:5 (gliclazide: PEG 8000), respectively, were characterized by x-ray
diffraction (XRD), Fourier-transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). Results: The solubility of gliclazide increased with increasing amount of PEG 8000 in aqueous medium.
Gibbs free energy (ΔGο tr) values were all negative, indicating the spontaneous nature of gliclazide solubilisation. Dissolution studies indicated a significant increase in the dissolution of gliclazide when
dispersed in PEG 8000. FTIR analysis demonstrated the absence of well-defined gliclazide - PEG 8000 chemical interaction while DSC and XRD studies indicated the amorphous /microcrystalline state of
gliclazide in the SDs. Conclusion: In both solid dispersions and physical mixture, PEG 8000 increases the solubility and dissolution rate of gliclazide. The increased dissolution rate of gliclazide may be due to the formation of microcrystals, increased wettability and dispersibility in systems containing PEG 8000.
with polyethylene glycol (PEG) 8000 and compare them with SDs in PEG 6000. Methods: Gliclazide SDs containing varying concentrations of PEG 8000 were prepared using the fusion – solvent technique, and their phase solubility behavior and dissolution in 0.1N HCl were assessed at 37 oC. The physical state of, and gliclazide-PEG interactions in, SDs and physical mixtures prepared in ratios of 1:1, 1:2 and 1:5 (gliclazide: PEG 8000), respectively, were characterized by x-ray
diffraction (XRD), Fourier-transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). Results: The solubility of gliclazide increased with increasing amount of PEG 8000 in aqueous medium.
Gibbs free energy (ΔGο tr) values were all negative, indicating the spontaneous nature of gliclazide solubilisation. Dissolution studies indicated a significant increase in the dissolution of gliclazide when
dispersed in PEG 8000. FTIR analysis demonstrated the absence of well-defined gliclazide - PEG 8000 chemical interaction while DSC and XRD studies indicated the amorphous /microcrystalline state of
gliclazide in the SDs. Conclusion: In both solid dispersions and physical mixture, PEG 8000 increases the solubility and dissolution rate of gliclazide. The increased dissolution rate of gliclazide may be due to the formation of microcrystals, increased wettability and dispersibility in systems containing PEG 8000.