Efficient strategy of oral drug development based on the risk assessment and risk avoidance

Abstract

For streamlining the development of oral drug products, it is quite important to assess the risk in oral drug absorption based on the physicochemical properties of candidate compounds. Especially, poorly water-soluble compounds often show nonlinear absorption kinetics due to the saturated solubility in the gastrointestinal tract. This might terminate the project because of the difficulty to obtain enough drug exposure in the blood for evaluating the toxicity and safety of the compound. As the method to avoid such risks, supersaturable formulations are now attracting a lot of attentions from pharmaceutical industries. By introducing such appropriate formulation technologies, it is possible to increase the efficacy in oral drug development.