In the article, "Formulating with Less API: Exploring the Application of API Sparing Techniques in Oral Drug Development," we discuss API-sparing in vitro techniques that can effectively support oral drug development, focusing on those associated with optimizing solubility. Of the three factors that define oral bioavailability – solubility, permeability, and metabolism – low aqueous solubility is a concern for approximately 75% of the new molecules coming out of discovery.
Since formulators are most able to impact solubility, API-sparing methods are particularly valuable for solubility enhancement studies when developing enabled formulations. We examine the technological advances that are enabling faster, smaller volume testing and present their value through the applications of these techniques.
Using state-of-the-art technology, formulators with the requisite know-how are now able to apply a raft of API-sparing techniques to advance with confidence, even when API is limited. Via the careful use of such techniques, APIs, excipients, and prototype formulations can be thoroughly characterized to effectively identify the most promising candidates for oral drug development earlier in the development lifecycle.
