Abstract
The aim of the present study was to enhance the solubility, dissolution rate and thus antihyperglycemic activity of a poorly soluble, BCS class II drug repaglinide, using its solid dispersions (SDs) with polyethylene glycol (PEG) 6000. Solid dispersions were prepared by kneading, solvent evaporation, conventional fusion method and microwave induced fusion methods. The dispersions were evaluated for various in vitro parameters such as solubility study, dissolution study, fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and scanning electron microscopy (SEM). Microwave induced solid dispersions exhibited significant improvement in solubility and dissolution rate compared to that of pure drug. Results of DSC, XRD and SEM study showed translation of crystalline form of RG to amorphous form. Thus, microwave technology offers a simple, efficient, solvent free promising alternative method to prepare solid dispersion of RG with significant enhancement of the in vitro dissolution rate.
Highlights
Therapeutic success of a drug depends upon the bioavailability and upon the solubility of drug molecules
polyethylene glycol (PEG) 6000 was heated to a molten mass and to this a weighed amount of RG was added with continuous stirring till solidification
Conventional fusion method and microwave induced fusion method were determined in the USP dissolution medium 2.5.4 X-Ray Powder Diffraction Studies: containing citric acid and sodium phosphate pH 5 at 37 ± 0.2° Powder X-ray powder diffraction (XRD) patterns of RG, PEG 6000, physical mixture
Summary
Therapeutic success of a drug depends upon the bioavailability and upon the solubility of drug molecules. Mechanisms for the improved solubility and dissolution properties of poorly soluble drugs from solid dispersions include reduction of the particle size of the drug, partial transformation of the crystalline drug to the amorphous state, formation of solid solutions, formation of complexes, reduction of aggregation and agglomeration, improved wetting of the drug and solubilization of the drug by the carrier at the diffusion layer [9 – 11] It is highly acceptable, that often more than one of these mechanisms determine the rate and extent of dissolution [12]. The objective of the present investigation was to explore the potential of kneading, solvent evaporation, conventional fusion and microwave induced fusion methods with PEG 6000 as carrier to generate solid dispersions for solubility and dissolution rate enhancement of RG
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