Biopharmaceutical characterization of sustained release matrix tablets based on novel carbomer polymers: formulation and in vivo investigation.

With the increased interest in modified release dosage forms and drug delivery systems, there is an increasing concern for biopharmaceutical characterization of the formulation in the early stages of drug product development. The main objectives of biopharmaceutical characterization are the in vitro and in vivo evaluation of the selected formulations in order to identify the factors influencing drug release; define the in vitro test methodology that would be predictive of drug products in vivo behavior and develop quantitative in vitro - in vivo correlation. The purpose of this study was to assess the potential of novel carbomer polymers, Carbopol 971P and Carbopol 71G, as a sustained release agents in matrix tablets containing high dosage drug substance. Although chemically identical, the two polymers exhibited substantially different drug release properties in vitro. Hypothetical in vivo drug release profiles were calculated by numerical deconvolution from cumulative urinary excretion data observed in vivo. The obtained results indicated that sound and reliable in vivo drug release profiles could be obtained from urinary excretion data and also, emphasized the need for in vitro testing under a range of experimental conditions in order to develop the biorelevant drug release methodology.