Solubility enhancement technique for an anti-malarial drug

Atovaquone is a competitive inhibitor of ubiquinol channel, specifically inhibiting the mitochondrial electron transport chain at the bcl complex. Inhibition of bcl activity results in a loss of mitochondrial function with poorly water soluble antiprotozoal drug, Atovaquone, by fabricating its solid dispersions were prepared by employing Kollidon VA-64 and Soluplus by solvent evaporation and spray drying method. Both solid dispersions significantly improved the dissolution profile of Atovaquone. Solid dispersions prepared by spray drying method showed more solubility enhancement with enhanced dissolution as compared to solid dispersions prepared by solvent evaporation method. IR and UV spectral analysis of solid dispersions indicated that there was no probable interaction between drug and carriers. Optimised solid dispersions were further evaluated by XRD and DSC. Dissolution rate of solid dispersions increased with increased concentration of polymer like Soluplus and Kollidon VA-64.

Author(s): Ram S. Pentewar, Nasheer S. Shaikh, Aparna V. Bhalerao, Rohit Bharti and Gajanan V. Pulgamwar

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