Pharmacokinetics of 9 -fluorhydrocortisone

Vogt, W.; Fischer, I.; Ebenroth, S.; Appel, S.; Knedel, M.; Lücker, P.W.; Rennekamp, H.

Arzneimittel-Forschung 21(8 Suppl): 1133-1143

1971


ISSN/ISBN: 0004-4172
PMID: 5109328
Document Number: 5603
Clinical trials concerning pharmacokinetics of 9aRuoro-11/3,17a,21-trihydroxy-4-pregnene - 3,20- dione (9afluorohydrocortisone) are reported. The blood level fluctuations after oral as well as intravenous application of the drug were measured in five voluntary subjects. In one of these subjects the permeability of the drug into the liquor was examined. In another subject the protein binding and the shift between the single protein fractions was measured. The results of the trial are as follows: 1. The absorption of the drug sets in very fast. 2. The highest blood level was measured after 1.7 h. 3. Elimination half-life time of the pure drug after intravenous application was 30 min. 4. The calculation of the absorption ratio resulted in about 100%. 5. The ratio concentration of the drug in liquor to that in plasma was 1 :6. 6. The cumulation maximum for z-=8 h will be readied after 33 h. It is 1.4 times as high as the maximum after oral application of the drug. When dosing the drug every 12 h the Limit maximum is reached after 25 h, amounting to the 1.30fold of the maximum obtained after single oral application.

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Pharmacokinetics of 9 -fluorhydrocortisone