Evaluation of the effect of different kinds of foods on the bioavailability of a sustained-release theophylline tablet.
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 standardized normal, high fat or high fat/high protein meal. The results showed no differences in AUC, K, tmax, ka and MRT. Statistical differences were found in Cmax 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.
Gai
M N
MN
Department of Science and Pharmaceutical Technology, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Santiago.
Thielemann
A M
AM
Arancibia
A
A
D000042:Absorption; D000328:Adult; D001682:Biological Availability; D001825:Body Fluid Compartments; D003692:Delayed-Action Preparations; D004041:Dietary Fats / Q000008:administration & dosage / Q000494:pharmacology*; D004044:Dietary Proteins / Q000008:administration & dosage / Q000494:pharmacology*; D005069:Evaluation Studies as Topic; D006801:Humans; D008297:Male; D013806:Theophylline / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D004041:Dietary Fats; D004044:Dietary Proteins; D013806:Theophylline