ISSN:
1432-1041
Keywords:
indoramin
;
6-hydroxyindoramin
;
bioavailability
;
pharmacokinetics
;
healthy volunteers
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Summary We have studied the pharmacokinetics and absolute systemic availability of indoramin (50 mg) given orally in solution or as a tablet with reference to intravenously administered drug (0.15 mg/kg) in 9 healthy volunteers. After intravenous administration the median apparent volume of distribution was 6.3l·kg−1, plasma clearance was 20.0 ml·min−1·kg−1, and terminal half-time was 4.1 h. When given by tablet indoramin was absorbed with moderate rapidity, with a median tmax of 1.5 h. The median systemic availability was 24%. After oral administration in solution the drug was more rapidly absorbed, with a median tmax of 1.0 h (p〈0.01). The median systemic availability was 43% (15–85%). Plasma concentrations of an active metabolite, 6-hydroxyindoramin, after single oral doses in either dosage form, were of a similar order to those of unchanged drug and fell with similar rapidity. After intravenous administration, however, concentrations of the metabolite were negligible.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02455999
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