Bambuterol: uptake and metabolism in guinea pig isolated lungs
The lung uptake and biotransformation of /sup 3/H-bambuterol, a prodrug to terbutaline, were studied using isolated perfused and ventilated guinea pig lungs. /sup 14/C-Sucrose was used as an extracellular marker. The lung uptake of bambuterol was significantly (0.05 greater than or equal to P greater than or equal to 0.001) higher than that found for sucrose in single-pass perfusion experiments. High-performance liquid chromatographic (HPLC) analysis showed that 95.6 +/- 3.6% of the effluent /sup 3/H radioactivity was attributable to bambuterol. In recirculating experiments (120 min) the lung biotransformation of /sup 3/H-bambuterol (8.5 pmol/ml) was studied. Both oxidative and hydrolytic metabolism took place. The dominating metabolites were hydroxylated bambuterol and the monocarbamate derivative which is a product of hydrolysis of bambuterol. Traces of terbutaline were also formed. The results show that bambuterol has a certain affinity to lung tissue and that the drug is, to some extent, biotransformed in the guinea pig lung.
- Research Organization:
- Safety Assessment, Soedertaelje (Sweden)
- OSTI ID:
- 5904686
- Journal Information:
- Pharm. Res.; (United States), Journal Name: Pharm. Res.; (United States) Vol. 5:3; ISSN PHREE
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BODY
CARBOHYDRATES
CARBON 14 COMPOUNDS
CARDIOVASCULAR AGENTS
CHROMATOGRAPHY
COUNTING TECHNIQUES
DISACCHARIDES
DRUGS
GUINEA PIGS
IN VITRO
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIQUID COLUMN CHROMATOGRAPHY
LUNGS
MAMMALS
METABOLISM
METABOLITES
OLIGOSACCHARIDES
ORGANIC COMPOUNDS
ORGANS
PERFUSED ORGANS
RESPIRATORY SYSTEM
RODENTS
SACCHARIDES
SACCHAROSE
SCINTILLATION COUNTING
SEPARATION PROCESSES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UPTAKE
VASODILATORS
VERTEBRATES