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Absorption and Disposition of Ethambutol in Rabbits
Ist Teil von
Journal of pharmaceutical sciences, 1984-08, Vol.73 (8), p.1053-1055
Ort / Verlag
Washington: Elsevier Inc
Erscheinungsjahr
1984
Quelle
Wiley-Blackwell Journals
Beschreibungen/Notizen
The absorption and disposition of ethambutol was examined in six rabbits in a three-way crossover study. Each rabbit received 45-mg/kg doses of ethambutol in three treatments: one intravenous injection, and two oral solutions, ethambutol alone and ethambutol in the presence of aluminum hydroxide (40 mg/kg). Half-lives of ethambutol ranged from 2.26 to 5.20h when administered alone and 2.18 to 4.00h when coadministered with the antacid; the difference was not significant (p > 0.3). Mean clearance after the oral administrations (189.2 mL/min/kg) was significantly greater than the mean intravenous clearance (43.7 mL/min/kg) (p < 0.01), suggesting a first-pass metabolism of ethambutol when administered nonparenterally to rabbits. The volume of distribution ranged from 5.5 to 17.8 L/kg, suggesting an extensive distribution of ethambutol outside the central compartment and, possibly, a localized deposit within the body tissues. Mean bioavailability of ethambutol was ∼28% and was not affected by the presence of aluminum hydroxide. The rate of ethambutol absorption, however, was slightly delayed by the antacid.