EVALUATION OF THE EFFECT OF DIFFERENT KINDS OF FOODS ON THE BIOAVAILABILITY OF A SUSTAINED-RELEASE THEOPHYLLINE TABLET

Abstract

Food-induced changes on the bioavailability of a sustained-release theophylline tablet, which uses acrylic resins Eudragit as sustaining agent, were studied in 12 healthy male volunteers. The tablet was developed in our laboratory using conventional technology. It presented a good bioavailability pattern and maintained plasmatic concentrations within the therapeutic range for 12 hours under conditions of steady-state. The study design was a 4 x 4 latin square involving 12 subjects who received a single dose of the tablet while fasting or with a standarized normal, high fat or high fat/high protein meal. The results showed no differences in AUC, K, t(max), ka and MRT. Statistical differences were found in C-max comparing the fasting condition with high fat/high protein diet. A delay was also observed in the detection of the drug in plasma when the tablet was administered with high fat and high fat/high protein food, but clinically the changes seem to be irrelevant.