PREPARATION, CHARACTERIZATION AND IN-VITRO EVALUATION OF PROBENECID: A PROTOTYPICAL URICOSURIC AGENT IN TO EXTENDED RELEASE MICROSPHERES

In the present research work, drug PRBENECID an anti-gout drug called as a prototypical URICOSURIC agent was selected for preparation of controlled release microspheres. Polymers sodium alginate and Methocel K100 was used as release retarding agents and to prolong the release of drug in a predetermined time rate of release. To attain the objectives of present work an attempt of formulation was made from trial T1-T5 using sodium alginate and from trial T6-T10 using Methocel K100. Micrometric properties bulk density, tapped density, angle of repose and Hausner's ratio was found to be satisfactory in trial T5 with sodium alginate and more in T10 with Methocel K100 as T5-1.35, 0.76, 29.46 and 1.03: T10- 1.83, 0.59, 35.65 and 1.21. Comparative drug release was performed from T1-T5 and T6-T10 of which trial T10 was optimized based on drug release and rate of release of the drug from the microspheres were determined by placing the values in various kinetic models and the rate of release was conformed based on the regression coefficient R2 value of various kinetic models as to be followed in the order of 0.969 KORESMEYER PEPPAS PLOT>0.887 HIGUCHIS MODEL>0.886 FIRST ORDER>0.796 ZERO ORDER. Base on the R2 value the release of PROBENECID was following KORESMEYER PEPPAS PLOT MODEL with R2 0.969. Key Words: Probenecid, Uricosuric, Methocel K100