Bioavailability and pharmacokinetic studies in the development of an oral formulation of stobadine dipalmitate

The pyridoindole stobadine is a novel drug with antioxidant and cardioprote ctive properties. The objective of this study was to compare the bioavailab ility and the main pharmacokinetic parameters of two different stobadine do sage forms, STBtest and STBref ; after single oral dosing in the form ofgel atine capsules to 6 dogs. The dose ranged from 2.9 to 4.7 mg/kg and a rando mized two-period crossover design was applied To quantify the drug in plasm a, a GC/MS method was developed with a quantification limit of I ng/inl. Th e time profiles of stobadine plasma concentrations were fitted by pharmacok inetic models. The extent of relative bioavailability ranged between 0.71 t md 1.56. practically no difference,was found between the bioavailability ra te of the two capsules, expressed as C-max/AUC, with values ranging from 0. 0022-0.0047 min(-1) for STBtest and 0.0022-0.0045 min(-1) for STBref: In co nclusion, the technological difference of the capsules investigated did not yield deviations in either their extent or rare of absorption. Therefore t he two stobudine formulations were concluded to be bioequivalent. (C) 1999 Prous Science. All rights reserved.