Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
Gastric Acidity-Dependent Bioavailability of Commercial Sustained Release Preparations of Indomethacin, Evaluated by Gastric Acidity-Controlled Beagle Dogs
Ichimaro YAMADATomoko GODAMiwako KAWATATakako SHIOTUKIKenji OGAWA
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Volume 38 (1990) Issue 11 Pages 3112-3115

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Abstract

The relationship between gastric acidity and the bioavailability of two kinds of sustained-release indomethacin (IM) formulations was investigated in gastric acidity-controlled beagle dogs, and compared with that of rapid-release IM formulations.All test dosage forms were more rapidly dissolved in simulated intestinal fluid than in simulated gastric fluid.Gastric acidity did not affect the bioavailability of IM from the rapid-release formulation. However, the bioavailability of IM from the two kinds of sustained-release formulations were markedly influenced by gastric acidity. The rates of IM bioavailability from both of the sustained-release formulations were faster under low acidity conditions than under high acidity conditions (p<0.01). In addition, Tmax and mean residence time (MRT) were approximately the same for the rapid-release and sustained-release formulations under low acidity conditions.These results suggest that the IM sustained-release formulations showed a rapid-release profile under low acidity conditions.

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