Formulation Strategies For Poorly Soluble Molecules

As the number of poorly soluble compounds continues to increase in the industry development pipeline, conventional formulation strategies may not be sufficient to achieve acceptable levels of solubility in the gastrointestinal tract and hence absorption into the systemic circulation. Scientists will need to utilize advanced formulation technologies to maximize oral bioavailability.

Our team understands that there are multiple formulation approaches available to address poor aqueous solubility and the Developability Classification System (DCS) provides a robust framework to help aid the technology selection process. We have developed an extensive internal Formulation Handbook, which incorporates the use of the DCS along with other key decision trees, developed by our senior formulation, analytical and manufacturing scientists globally. For poorly soluble molecules, our formulators gather a clear understanding of the physiochemical and biopharmaceutic characteristics of the molecule and determine whether it falls into a Class IIa or IIb category depending on their solubility being related to either dissolution or a true solubility challenge. The understanding of the mechanism behind the poorly soluble nature of the molecule allows appropriate formulation strategies to be applied, resulting in the targeted use of more complex formulation approaches.