ABSORPTION IMPROVEMENT OF 2'-HYDROXY-5'-M ETHYL-LAUROPHENONOXIME (FLM-5011) BY USING PRODRUGS AND GALENIC FORMULATIONS

Methods to improve the absorption of problem drugs are presented for t he strongly lipophilic, poorly water-soluble, potential lipoxygenase i nhibitor FLM 5011 (1). The water-solubility is improved by using prodr ugs or by solubilizing. The characterization of solubility has been ch aracterized with an suitable in vitro model system. The bioavailabilit y of 1 in rabbits after oral administration is markedly increased usin g 1-prodrugs studied. The good correlation between the ABC measured in vitro and the AUC estimated in vivo demonstrates that it is possible to predict the bioavailability at the rabbit of highly lipophilic drug s such as 1 using the flow through model system.