PHYSICOCHEMICAL CHARACTERIZATION OF AMORPHOUS SOLID DISPERSION OF KETOPROFEN–POLYVINYLPYRROLIDONE K-30
Keywords:
Solvent co-evaporation, Amorphous solid dispersion, Ketoprofen, Polyvinyl pyrrolidone K-30Abstract
Objective: The aim of the current study was to prepare an amorphous solid dispersion of ketoprofen in polymer PVP K-30 by solvent co-evaporation technique and to characterize the physicochemical properties.
Methods: An amorphous solid dispersion of ketoprofen, a water insoluble non-steroidal anti- inflammatory drug with polyvinyl pyrrolidone K-30, were prepared by solvent co-evaporation method at drug to polymer ratios 1:1, 1:3, 1:5 and 1:9 (w/w). Physicochemical properties of the solid drug were evaluated by X-ray powder diffractometry (XRPD), differential thermal analysis (DTA) and scanning electron microscopy (SEM). Dissolution studies were conducted according to the USP paddle method.
Results: The X-ray powder diffraction and differential thermal analysis showed that ketoprofen was transformed from a crystalline phase to an amorphous state, as showed by disappearance of its characteristic of diffraction peaks and an endothermic peak. SEM Microphoto of amorphous solid dispersion showed homogeneous size and morphology. In addition, ketoprofen in amorphous solid dispersion showed better dissolution rate compared to crystalline drugs. The dissolution efficiency (DE) of ketoprofen from its amorphous solid dispersion increased with an increasing ratio of polymer.
Conclusion: The study has shown that dispersions of ketoprofen into water-soluble polymer PVP K-30 formed an amorphous ketoprofen in solid dispersion system. All amorphous solid dispersion of ketoprofen in PVP K-30 prepared by solvent co-evaporation demonstrated a significant improvement in dissolution rate of ketoprofen compared to pure ketoprofen.
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