Solubility enhancement technique for an anti-malarial drug using amino acid

Atovaquone is an Anti-malarial agent and is used in the treatment of malarial complications as chemoprophylaxis. The present research work is focused with an aim to increase solubility and hence dissolution rate of Atovaquone by using the various techniques of preparation of solid dispersion. The polymers like Kollidon VA-64 were used for solid dispersion using amino acids like Arginine was used. For preparation of solid dispersions, various solid dispersion methods (Solvent evaporation, Spray drying) were used. The effect of several variables to both solid dispersion preparations was investigated. IR and UV spectral analysis, Diffrential Scanning Calorimetry were used to characterize solid dispersions. Solid dispersions prepared by various methods were evaluated by methods like Saturation solubility, percent drug content, and by in -vitro dissolution method for percent cumulative drug release. Optimised solid dispersions were further evaluated by XRD, DSC, and SEM. The release rate for pure Atovaquone was found to be 46.7% in 2 hours. This release rate was increased by using amino acid that is arginine in ratio 1:1:1 to 1:1:4. By keeping Arginine constant and only increasing polymer the dissolution rate was improved from 76.6% to 84.4% when solvent evaporation method was used to prepare solid dispersions. The same compositions on spray drying showed increased dissolution rate from 97.5% to 100% in 100 minutes with Kollidon VA-64.

Author(s): Nasheer S. Shaikh,Ram S. Pentewar, Aparna V. Bhalerao, Saroja P. Adepwar, Sunil Taldeand NishatKazi

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