Title : Solubility enhancement of carvedilol using solid dispersion methods
Abstract:
Introduction: Carvedilol is poorly water-soluble and show low oral bioavailability. Solubility enhanced of low water soluble drug enhanced by solid dispersion method.
Method: Design expert-13 software used to enhance the solubility of poorly water soluble drug by solid dispersion methods. Using central composite designs(CCD) to study the effect of independent variables on solid dispersion of carvedilol and 9 formulations prepared by solvent evaporation and fusion method using different natural and synthetic polymers Hydroxy-propyl methylcellulose (HPMC), Locust bean Gum(LBG) , PEG 6000 (polyethylene glycolate) 6000 and sodium starch glycolate . Prepared formulation evaluation check by solubility, stability, Percentage yields, dissolution rate studies and characterized by Scanning electron microscopy (SEM), Powdered X-ray Diffractometry (PXRD), Differential Scanning Calorimetry (DSC) and Fourier Transform Infra-red (FTIR).
Result: Based on physicochemical evaluation and in-vitro characterization, the solid dispersion drug content, percentage yield and drug release was found to be 94.06%, 66.532%, 93.20% respectively and follows Peppas model. In FTIR studies Shifting of peaks confirmed the interaction of polymers with the pure drugs .SEM results show that the prepared agglomerates were spherical in shape, which enabled them to flow very easily. The PXRD, SEM and DSC indicated a change in the crystalline state of Carvedilol.
Conclusion: Based on evaluation, in-vitro characterization drug content, Drug percentage yield, drug release was maximized because of the increase in the amount of hydrophobic polymer maximize drug release and increased polymers concentration to produce reproducible results. This study indicated that the solubility of carvedilol was increased by solvent evaporation and fusion method.
Keywords: Carvedilol, drug release, Solubility, locust bean gum,polymers.
