BIOPHARMACEUTIC PROPERTIES OF DRUGS: NEW TOOLS TO FACILITATE DRUG DISCOVERY AND DEVELOPMENT

Properties of a good drug include safety, efficacy, half-life and bioavailability. With the current approach to drug discovery based on receptor-based and cell-based screening methods, compounds are frequently moved into development with poor bioavailability. With low bioavailability, drug administration is typically limited to parenteral routes, thus limiting the potential wide-spread utility of these therapeutic agents. The first and most important factor limiting a drug's bioavailability is the intestinal membrane permeability which in turn determines the maximum fi:action of the dose administered that can be absorbed. We have recently utilized new intubation methods for performing permeability measurements in humans and establishing a fundamental human data base for correlating intestinal jejunal membrane permeabilities with permeabilities determined in other systems, e.g., animals, tissue culture, as well as physical chemical properties.