Application of a radiotelemetric system to evaluate the performance of enteric coated and plain aspirin tablets

Abstract

The bioavailability of enteric coated and plain aspirin tablets was studied in four beagle dogs. Blood sampling for enteric coated tablets was planned with the aid of a radiotelemetric system. The release of aspirin from its dosage form was detected by monitoring the change in intestinal pH. Aspirin and salicylic acid levels in plasma obtained from the enteric coated dosage form exhibited familiar concentration versus time absorption profiles. Variation in the plasma concentrations of these two compounds within each dog studied (four runs each) was relatively small when time zero was adjusted to the commencement of tablet dissolution. The plasma levels obtained from plain aspirin (three runs each), however, show atypical absorption. The estimated absolute bioavailability was 0.432 ± 0.0213 and 0.527 ± 0.0260 for enteric coated and plain aspirin, respectively. Other pharmacokinetic parameters for these two dosage forms such as the highest observed plasma concentration (Cmax) (10.9 ± 0.535 μg/mL versus 13.6 ± 1.88 μg/mL) and the time to reach Cmax (tmax) (26.6 ± 1.94 min versus 31.0 ± 7.04 min) agree well. The mean values for gastric emptying time, in vivo coating dissolution time, and in vivo disintegration/dissolution time of the tablet core for enteric coated aspirin are 48.7 ± 7.23 min, 44.3 ± 3.80 min, and 34.7 ± 2.04 min, respectively. Copyright © 1986 Wiley‐Liss, Inc., A Wiley Company