Comparative pharmacokinetics of unlabeled and deuterium-labeled terbutaline: demonstration of a small isotope effect
Journal Article
·
· J. Pharm. Sci.; (United States)
An equimolar mixture of terbutaline and (/sup 2/H6)terbutaline was given as an oral solution to six healthy volunteers (three men and three women). Frequent blood samples were collected during a 24-h period and the plasma concentrations of unlabeled and deuterium-labeled terbutaline were measured by GC-MS. The overall geometric mean plasma concentration ratio of terbutaline to (/sup 2/H6)terbutaline (isotope ratio) was 1.04 and differed significantly from unity. The difference can be explained by a difference in lipophilicity between the analogues, affecting their absorption. No trend in isotope ratio over the experimental time was observed. For unknown reasons, the isotope ratio was higher for women (1.07) than for men (1.00). Deuterium-labeled terbutaline can be used, intravenously or orally, as an absolute reference in bioavailability studies on terbutaline. If deuterium-labeled terbutaline is given orally in a single-day relative bioavailability study, a correlation should be made for the observed isotope effect.
- Research Organization:
- Pharmacokinetics Laboratory, AB Draco, Lund (Sweden)
- OSTI ID:
- 6279739
- Journal Information:
- J. Pharm. Sci.; (United States), Journal Name: J. Pharm. Sci.; (United States) Vol. 77:11; ISSN JPMSA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL AVAILABILITY
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY FLUIDS
CARDIOVASCULAR AGENTS
CHROMATOGRAPHY
COMPARATIVE EVALUATIONS
DEUTERIUM
DRUGS
GAS CHROMATOGRAPHY
HYDROGEN ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPE EFFECTS
ISOTOPE RATIO
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
MASS SPECTROSCOPY
MATERIALS
NUCLEI
ODD-ODD NUCLEI
REACTION KINETICS
SEPARATION PROCESSES
SEX DEPENDENCE
SPECTROSCOPY
STABLE ISOTOPES
TRACER TECHNIQUES
VASODILATORS
59 BASIC BIOLOGICAL SCIENCES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL AVAILABILITY
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY FLUIDS
CARDIOVASCULAR AGENTS
CHROMATOGRAPHY
COMPARATIVE EVALUATIONS
DEUTERIUM
DRUGS
GAS CHROMATOGRAPHY
HYDROGEN ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPE EFFECTS
ISOTOPE RATIO
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGHT NUCLEI
MASS SPECTROSCOPY
MATERIALS
NUCLEI
ODD-ODD NUCLEI
REACTION KINETICS
SEPARATION PROCESSES
SEX DEPENDENCE
SPECTROSCOPY
STABLE ISOTOPES
TRACER TECHNIQUES
VASODILATORS