Oral bioavailability of a poorly aqueous drug from three different SBE7-β-cyclodextrin based formulations in beagle dogs

摘要

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.