ISSN:
1432-1041
Keywords:
Nocloprost
;
PGE2-analoga
;
clearance
;
half life
;
absolute bioavailability
;
pharmacokinetics
;
i. v. dose
;
oral dose
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Summary The pharmacokinetics and absolute bioavailability of nocloprost, a synthetic PGE2-analogue with cytoprotective properties, was investigated in human volunteers as a function of the dose. Ten young male volunteers received nocloprost 5 μg i. v. and 100, 200 and 400 μg p.o. in random order at weekly intervals. Serum nocloprost levels were monitored for up to 12 h after each dose, using a specific, validated assay. After nocloprost 5 μg i. v. the highest serum level of 373 pg·ml−1 was found in the first sample 5 min after injection, and the subsequent decline showed one or two phases, with half-lives of 4 and 49 min. The AUC was 89 pg·h·ml−1, the total plasma clearance was 13.2 ml·min−1·kg−1, and the volume of distribution at steady state was 0.16 l·kg−1. After oral administration the maximum serum level and AUC increased in proportion to the dose. tmax showed a wide scatter, with an average value of about 30 min independent of the dose. Although not detectable in every subject, post maximum serum levels declined biphasically, with half-lives of ca 10 and 35–40 min. The absolute bioavailability after oral administration averaged about 2% and was independent of the dose.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00315552
Permalink
