Abstract

IMPROVEMENT OF THE DISSOLUTION RATE OF ATOVAQUON BY IMPROVING SOLUBILITY IN DISSOLUTION MEDIUM BY SOLID DISPERSION TECHNIQUE

Toshiba Khanum, Brijesh K. Arjariya, R. S. Ghosh and Ravi Prakash Yadav*

ABSTRACT

Drug dissolution is the rate limiting step for bioavailability of poor aqueous soluble drug that consequently affects the in vivo drug absorption. In the present study solid dispersion based drug delivery system of Atovaquone were successfully developed in the form of tablets with improved dissolution characteristic by forming solid dispersion with PEG 4000. For the Atovaquone formulation, F1 was chosen as it has % drug release about 46 % in 180 min. FTIR spectra of drug with other excipients have not shown any interaction and also selected formulation was stable after stability studies. The in-vitro dissolution studies revealed a considerable boost in dissolution rate of Solid dispersions of Atovaquone in contrast to pure drug. From FTIR spectroscopy, it was concluded that there was no well-defined chemical interaction between Atovaquone and PEG 4000 in Solid dispersions, as no important new peaks could be observed. The Atovaquone solid dispersion based tablet (F1) showed 30.33% drug release within first 20 min. and 46.45% drug release within 180 min. Thus from studies, it could be concluded that solid dispersion of poor aqueous soluble Atovaquone by solvent evaporation technique were effectively formulated using PEG-4000 and PVP-K 30 hydrophilic polymers. Thus, the statement can be given that the rate of dissolution and solubility of poor aqueous soluble Atovaquon can be appreciably improved by solid dispersion by use of water soluble carriers by solvent evaporation technique.

Keywords: Bioavailability; Dissolution Enhancement; In-Vitro Evaluation; Solid Dispersion; Atovaquone.