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PREPARATION AND IN VITRO CHARACTERIZATION OF PELLETS CONTAINING FELODIPINE SOLID DISPERSIONS

RAREȘ IULIU IOVANOV^1*, IOAN TOMUȚĂ¹, ALEXANDRA BARBU¹, LUCIA RUS², SORIN E. LEUCUȚA¹

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The aim of the study was the preparation and characterization of prolonged release pellets loaded with felodipine (FD) solid dispersions (SD) and coated with different polymeric coatings in order to release the active pharmaceutical ingredient (API) over a 12 hours period. A central composite experimental design with three factors and three levels was developed in order to determine the influence of the polyvinylpyrrolidone (PVP)/FD ratio in the SD, the percentage of polymeric coating and the percent of pore forming polymer in the coating on the kinetics release of FD. The good data fit with the chosen model indicates that the results dependent on the studied formulation factors. All the studied formulations released the API over a 12 hours period. The DSC analysis showed that in the PVP:FD = 2 SD, the FD is found in an amorphous state. The SEM studies showed that the pellets were evenly loaded and coated throughout the entire preparation process. The statistical analysis of the experimental data highlighted that the increase of PVP ratio in the SD and the increase in the percent of pore forming polymer in the coating increases the release rate of FD and that the increase in the percent of the polymeric coating determines a reduction in the release rate of the chosen model drug. In this research there were developed and characterized some prolonged release coated pellets with FD solid dispersions, pellets that released the model drug over a 12 hours period and the release kinetics of the API fitted best with the Peppas, Higuchi, Baker-Lonsdale and First order mathematical equations.