A NOVEL FORMULATION OF ALBENDAZOLE SOLUTION - ORAL BIOAVAILABILITY AND EFFICACY EVALUATION

To improve the oral bioavailability of albendazole, a poorly water-sol uble drug, a new liquid formulation was investigated in mice. The liqu id formulation studied was a solvent system of Transcutol(R) (40% w/w) in 1.2 pH buffer. A significant (p < 0.05) increased relative bioavai lability was obtained with this albendazole solution as compared with an albendazole suspension. A Trichinella/mouse model was used to evalu ate the efficacy of the formulation against the different stages of th e parasite. The higher concentration-time plasma profile of the albend azole solution would explain the greater therapeutic effect obtained w ith this new formulation against the systemic phases of the Trichinell a model studied. This albendazole solution presented an efficacy again st the migrating larvae phase twice that of the albendazole suspension . The efficacy of the solution (95.5%) in the encysted phase was signi ficantly (p < 0.05) higher than the efficacy obtained with the albenda zole suspension (2.4%). (C) 1997 Elsevier Science B.V.