Formulation and Optimization of Dolutegravir Fast Dissolving Tablets Using Various Solubility Enhancement Methods

Abstract

Dolutegravir is a HIV-1 antiviral agent to control HIV/AIDS. In the present study Dolutegravir solid dispersion has been subjected to improve the solubility and dissolution rate performance by formulating as fast dissolving tablets, in which PEG 6000 and Poloxamer 407 were used as polymers. Solid dispersions of Dolutegravir were prepared with different carriers in different ratios of drug and carriers such as PEG 6000 and Poloxamer 407 (1:1, 1:2 and 1:3) by solvent evaporation and fusion method. The pre-compression and post-evaluation parameters were studied and the results were shown. All the results were within acceptable IP limits Finally, by comparing all the dissolution profile of solid dispersions , formulation F3 containing Dolutegravir + PEG 6000 (1:3) showed better results by solvent evaporation method at the end of 60 min with maximum drug release, hence it is selected as the best formulation. From the obtained optimized solid dispersion formulation, the fast dissolving tablets were prepared by using different concentrations of various super disintegrants. The in-vitro drug releases of the formulated Dolutegravir tablets were performed using a 6.8 pH Phosphate buffer as dissolution medium. The optimized DF3 formulation containing Sodium starch glycolate (SSG) (6% w/w) as super disintegrant, and it showed 98.04±1.9 % percentage drug release at 25 min. Characterization in solid-state were done by analytical methods such as UV-Visible, FT-IR studies. The optimized formulation followed first order release kinetics.