Absorption of exaprolol from the in-situ gastrointestinal tract of rats and dogs

Author:

Motheová O1,Zemánek M21,Faberova V21,Trnovec T1,Gabauer I31,Styk J31,Ďurišová M1,Nosáľová V1

Affiliation:

1. Institute of Experimental Pharmacology, Centre of Physiological Sciences, Slovak Academy of Sciences, 842 16 Bratislava

2. Drug Research Institute, 900 01 Modra, Czechoslovakia

3. Institute of Experimental Surgery, Centre of Physiological Sciences, Slovak Academy of Sciences, 842 16 Bratislava

Abstract

Abstract The absorption rate of the β-adrenoceptor blocking drug, exaprolol, from the gastrointestinal tract was studied using in-situ methods in the rat and dog. Exaprolol was rapidly absorbed from the small and large intestine of rats and from the ileum of dogs. The cardiac output and regional blood flow decreased in rats to approximately one half of the original values within 30 min of the in-situ experiment. The logarithm of the amount vs time plots from dogs were linear, whereas with rats a curvilinearity appeared apparently because of the blood flow-limited absorption kinetics of this highly lipophilic drug. The data obtained suggest that exaprolol is suitable for administration in sustained release form.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

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