Effect of curing on the in vitro release of theophylline as model drug from lipidic or lipidic/polymeric matrix.

GUERRERO P; CIFUENTES P; PALMA SD; ROMERO, VL

Rosario

Congreso; RICIFA. 4 Reunión Internacional de Ciencias Farmacéuticas; 2016

Universidad Nacional de Rosario

Effect of curing process on drug release from lipidic or lipidic/polymeric matrices Guerrero P, Cifuentes P, Palma SD, Romero VLE-mail: veronica.romero@unab.clEscuela de Farmacia, Facultad de Medicina, Universidad Andrés Bello, Santiago, CHILE. Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, ARGENTINAKeywords: theophylline, termal treatment, lipidic matrixWax has been used as matrix in pharmaceutical controlled release dosage form since decades. It provides several advantages that include good stability at varying pH and moisture levels and effective retardation of highly water-soluble drug from the matrix. Curing is defined as the bonding of adjacent particle surfaces in a mass of powder or in a compact by application of heat. This concept in pharmaceutical science is relatively recent, but research interests relating to this process have been growing.The study was conducted to evaluate several mixtures of Compritol® with either Precirol®, cetilic alcohol or HPMC K100M in different percentages, also we evaluated if the diluents in the matrix has any impact on the in vitro release profile of theophyline (drug model). In addition we also compared if the thermal treatment affects the release profile of theophylline from simulated chewable matrix or the intact matrix. All the matrices were obtained with direct compression and the heat treatment was performed for 30 minutes at 60 °C.Our results show that the thermal treatment decreases the release rate of theophylline from 60-70% without the curing to 20-30% with the thermal treatment for Compritol and Compritol/cetilic alcohol matrix in intact matrix after 8 hours. This difference was a little smaller with the chewed matrix in comparation with the same matrix but without curing. We have observed no notorious change with the application of the heat treatment in the release rate when HPMC was in the formula or by the incorporation of different diluents (lactose, Encompress ®, microcrystalline cellulose). This works shows that curing could be an excellent alternative to obtain a controlled release rate of a drug from a lipídic matrix even for the formulation of chewable tablets