Pharmacophore an International Research Journal
The formulation of poorly soluble drug for oral delivery is one of the biggest challenges for formulation scientists. Efavirenz, a non-nucleoside reverse transcriptase inhibitor is used as a part of highly active antiretroviral therapy treatment of a human immunodeficiency virus type I. It exhibits poor dissolution characteristics when administered in conventional oral dosage form with a bioavailability of just 40-45%. The objective of this study is to evaluate the effects of novel excipients such as Soluplus®, dioctyl sulphosuccinate and various superdisintegrants in increasing the dissolution efficiency of Efavirenz. Physical mixtures of Efavirenz with one or more of these excipients was used in different ratios for formula optimization to increase the dissolution rate of Efavirenz. Analytical techniques such as Fourier Transform Infra red spectroscopy (FTIR) and differential scanning calorimetry (DSC) were used to confirm compatibility of efavirenz with the excipients. Preliminary trials along with factorial studies were performed for finalization of formula. Dissolution studies performed revealed improvement in release profile as compared to conventional tablet. Short-term stability studies were performed on the optimized formula. Optimized formulation was subjected to analytical studies to confirm stability of formulation. Evaluation by X-ray diffraction (XRD), DSC and FTIR techniques revealed that the formulation was stable. Techniques such as solid dispersion of drug in solubilizing agent can be tried to bring about further enhancement in extent of drug release.
