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Pharmacokinetics and bioavailability of oral ergometrine in male volunteers

✍ Scribed by A. N. J. A. De Groot; T. B. Vree; Y. A. Hekster; M. Van Den Biggelaar-Martea; P. W. J. Van Dongen; J. Van Roosmalen


Publisher
John Wiley and Sons
Year
1994
Tongue
English
Weight
380 KB
Volume
15
Category
Article
ISSN
0142-2782

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✦ Synopsis


The aim of this investigation was to assess the pharmacokinetics and bioavailability of ergometrine in six human male subjects after an oral dose of 0.200 mg and after an intravenous dose of 0.075 mg of ergometrine maleate. A large variation in bioavailability of between 34% and 117% in the six volunteers was observed. The lag time was also subject dependent and ranged between 0.0073 h (0.4 min) and 0.47 h (28 min). After intravenous administration, the pharmacokinetic profile can be described by a twocompartment model. The distribution half-life t is 0.18 2 0.20 h, the elimination halflife t E O is 2.06k0.90 h, the total body clearance (CL) amounts to 35.9k 13.41 h-' and the steady-state volume ( V s s ) of distribution is 73.4+ 22-0 1. After oral administration, the pharmacokinetic profile can be described by a one-compartment model. The absorption half-life tRlabs is 0.1920.22 h, and the elimination half-life t 1 -90f 0.16 h. This study with oral ergometrine shows such a large interindividual variability in bioavailability that the oral route of administration does not seem not to be the most reliable means of accurate dosing in preventing post-partum haemorrhage.


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