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Pharmacokinetic Evaluation of Ethionamide Suppositories
Author(s) -
Peloquin Charles A.,
James Gordon T.,
McCarthy Eileen,
Goble Marian
Publication year - 1991
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1991.tb02645.x
Subject(s) - suppository , bioavailability , pharmacokinetics , crossover study , ethionamide , rectal administration , oral administration , placebo , bioequivalence , medicine , pharmacology , absorption (acoustics) , dosage form , anesthesia , mycobacterium tuberculosis , tuberculosis , physics , alternative medicine , ethambutol , pathology , acoustics
The absorption and elimination of ethionamide (ETA) after oral tablets and rectal suppositories were determined in 12 healthy, adult male volunteers. A randomized, double‐blind, double‐dummy, crossover design was used. Treatments compared 250‐mg ETA tablets and a placebo suppository to a 500‐mg ETA suppository and two placebo tablets, given 7 days apart. Blood samples were collected at predetermined intervals for 12 hours after the dose. Serum concentrations of ETA were determined using high‐performance liquid chromatography. The area under the serum concentration‐time curve was used to compare the relative bioavailability of ETA from the two preparations. Relative bioavailability after rectal administration was 57.3% of that after oral administration. The maximum serum concentration after rectal administration was 33% of that after oral administration. Higher doses of ETA and serum concentration monitoring are recommended whenever the suppositories are used.