Metabolic studies of salbutamol-3H: A new bronchodilator, in rat, rabbit, dog and man

doi:10.1016/0014-2999(71)90211-1

European Journal of Pharmacology

Volume 14, Issue 2, April 1971, Pages 183-199

https://doi.org/10.1016/0014-2999(71)90211-1 Get rights and content

Abstract

Salbutamol-³H, labelled on the β-carbon atom, was rapidly absorbed from the gastro-intestinal tract of rat, rabbit, dog and man. 60–90%, depending upon the species studied, of the administered radioactivity was recovered in the 24 hr urine. 70–90% of the radioactivity present in the dog urine was due to unchanged salbutamol-³H, whereas 90% in the rabbit and 40% in the rat urine was due to salbutamol-³H o-phenylglucuronide. The latter has been isolated and shown to be neither a β-stimulant nor a β-blocker. The rat conjugated salbutamol-³H in the liver, and excreted the glucuronide via the bile. 0–48 hr rat faeces contained 25–40% of the label. Analysis of the tissues from the rat and dog indicated that the drug was completely cleared from the body. Salbutamol-³H inhaled by dogs and humans as an aerosol was slowly adsorbed from the lung, and excreted via the urine.

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Metabolic studies of salbutamol-3H: A new bronchodilator, in rat, rabbit, dog and man

Abstract

J. Pharm. Sci.

Microchem. J.

Biochem. Pharmacol.

Anal. Biochem.

Lancet

Metabolic studies of salbutamol-³H: A new bronchodilator, in rat, rabbit, dog and man