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Pharmacokinetics of coumarin and its 7-hydroxy-metabolites upon intravenous and peroral administration of coumarin in man
- Source :
- European journal of clinical pharmacology. 12(6)
- Publication Year :
- 1977
-
Abstract
- The pharmacokinetics of coumarin (C) upon i.v. and p.o. administration and its metabolites 7-hydroxy-coumarin (7-HC) and 7-hydroxy-coumarin glucuronide (7-HCG) have been studied. Six healthy volunteers were involved in this investigation. Four of the volunteers participated in a crossover study. Coumarin was administered i.v. and p.o. in dose sizes of 0.25 mg/kg and 0.857 mg/kg, respectively. Coumarin is rapidly absorbed p.o., however the availability to systemic circulation is less than 4%. The rest of the dose appears quantitatively as 7-HC and 7-HCG in systemic circulation suggesting an extensive firstpass effect. Coumarin and 7-HCG are best fitted to an open two-compartment model, whereas 7-HC is best fitted to an open one-compartment model. The biological half-life of both C (0.80 vs. 1.02 h) and 7-HCG (1.47 vs. 1.15 h) was not significantly different for the two routes of administration. The large total clearance of C again suggests a first-pass effect; while that of 7-HCG, which is nearly exclusively eliminated into urine, indicates active tubular secretion of the glucuronide.
- Subjects :
- Adult
Male
Administration, Oral
Glucuronates
Urine
Pharmacology
Systemic circulation
Models, Biological
First pass effect
chemistry.chemical_compound
Pharmacokinetics
Coumarins
Humans
heterocyclic compounds
Pharmacology (medical)
Chemistry
General Medicine
Middle Aged
Coumarin
Crossover study
Bioavailability
Kinetics
Injections, Intravenous
Female
Glucuronide
Subjects
Details
- ISSN :
- 00316970
- Volume :
- 12
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- European journal of clinical pharmacology
- Accession number :
- edsair.doi.dedup.....5d80fdcf2341d4b01d04d8593c19da3a