title: Oral bioavailability of a poorly aqueous drug from three different SBE7-β-cyclodextrin based formulations in beagle dogs.
abstract: Oral administration of Lu 35-138, a low aqueous soluble compound, was investigated in three different formulations containing sulfobutylether β-cyclodextrin (SBE7βCD) in fasted beagle dogs. The evaluated formulations was (i) a SBE7βCD solution, (ii) a spray dried solution filled into hard gelatine capsules, and (iii) a direct compressible tablet containing SBE7βCD. The three formulations did not lead any significant differences in the obtained AUCs, though a trend was observed for the highest absorption when Lu 35-138 was dosed in the cyclodextrin solution. These results demonstrate that a solid formulation with a relative low content of cyclodextrins can be used to increase the bioavailability of a low water soluble compound to a relative high level when compared to a cyclodextrin solution.
authors.affiliation: Preformulaton, H.Lundbeck A/S, Ottilavej 9, Valby 2500, Denmark.
authors.forename: René
authors.initials: R
authors.lastname: Holm
authors.affiliation: Pharmaceutical Development, H.Lundbeck A/S, Ottilavej 9, Valby 2500, Denmark.
authors.forename: Lene
authors.initials: L
authors.lastname: Andresen
authors.affiliation: Early Development Pharmacokinetics, H.Lundbeck A/S, Ottilavej 9, Valby 2500, Denmark.
authors.forename: Claus
authors.initials: C
authors.lastname: Strange
keywords: Bioavailability; Complexation; Cyclodextrins; Oral absorption; Solubility enhancement