Kinetics of the epimeric glucocorticoid budesonide
Budesonide is a potent nonhalogenated glucocorticoid consisting of a 1/1 mixture of the two epimers 22R and 22S. The kinetics of these epimers were studied in six healthy male subjects after intravenous administration of 500 micrograms /sup 3/H-budesonide. Estimation of the epimer concentrations in plasma was made possible by development of an HPLC method for simultaneous separation and quantification. The plasma t 1/2, distribution volume (V beta), and plasma clearance for epimer 22R were (mean +/- SD) 2.66 +/- 0.57 hr, 425 +/- 100 l, and 117 +/- 40 l/hr. The corresponding values for epimer 22S were 2.71 +/- 0.69 hr, 245 +/- 38 l, and 67 +/- 19 l/hr. Differences in V beta and plasma clearance between the two were significant. The larger V beta noted for epimer 22R may be a result of higher tissue affinity. The high plasma clearance for both epimers should largely reflect their high rate of liver biotransformation.
- Research Organization:
- AB Draco, Research and Development Laboratories, Lund, Sweden
- OSTI ID:
- 6975638
- Journal Information:
- Clin. Pharmacol. Ther.; (United States), Journal Name: Clin. Pharmacol. Ther.; (United States) Vol. 35:4; ISSN CLPTA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ADRENAL HORMONES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BLOOD-PLASMA CLEARANCE
BODY FLUIDS
CHROMATOGRAPHY
CLEARANCE
CORTICOSTEROIDS
GLUCOCORTICOIDS
HORMONES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
KETONES
KINETICS
LABELLED COMPOUNDS
LIQUID COLUMN CHROMATOGRAPHY
MAMMALS
MAN
MATERIALS
ORGANIC COMPOUNDS
PREGNANES
PRIMATES
REACTION KINETICS
SEPARATION PROCESSES
STEROID HORMONES
STEROIDS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES