Nisha Thakre1, Kapil Khatri1, Satish Shilpi1*
Pharmaceutical Research Lab, Department of Pharmaceutics,
Ravishankar College of Pharmacy, Bhopal (MP) India
*Corresponding Author
Dr. Satish Shilpi
Pharmaceutical Research Lab, Department of Pharmaceutics,
Ravishankar College of Pharmacy, Bhopal (MP)
Email: shilpisatish@gmail.com
Phone: 09406520691
Abstract
Objective: The objective of the present investigation was to improve solubility of ezetimibe (EZE), results increasing its bioavailability. Materials and method: The solid dispersion of ezetimibe was prepared by solvent evaporation method by using different ratios of PVP K-30: PEG6000 (1:1:1, 1:1:2 and 1:1:3) respectively. Complex formation was authenticate by Powder X-Ray Diffraction (XRD) and differential scanning calorimetry (DSC) analysis. The prepared solid dispersion was further characterized for drug content, drug-polymer interactions, in vitro drug release and stability studies. Results: There was no any interaction found between drug and polymer and got a single thermogram of polymer that indicates the formation of complex. Powder X-Ray Diffraction (PXRD) revealed that no sharp crystalline peak was abstained because of conversion of solid mixture from crystalline to amorphous form. The prepared dispersion showed marked increase in the solubility as well as dissolution rate of ezetimibe in comparison of pure drug and the in vitro release studies revealed that there was an improvement in the dissolution characteristics of EZE in the form of solid dispersions. Conclusion: Solid dispersion with PEG 6000 and PVPK30 gave better rate and extent of dissolution. The best fit model indicating the probable mechanism of drug release from solid dispersions was found to be Koresmeyer peppas model. It can be concluded that PEG6000 and PVP K30 is suitable to prepare solid dispersions of ezetimibe to increase the solubility and bioavailability.
Keywords: Solubility, Bioavialability, Ezetimibe, PVP-K30, PEG6000, Solid dispersion
