Overcoming Formulation Hurdles

Our solid form screening and selection can be seamlessly progressed into preclinical formulation studies with the right crystal form and the right formulation which can further be integrated into our drug product development plan.

Every drug molecule exhibits intrinsic physicochemical properties which needs to be considered before development of pharmaceutical formulation. Evaluation and selection of solid forms for an API also reduces the risk of possible formulation issues arising in future development. With successful API form screening and isolation process development, selection of the right solid state and strategy for pre- and early formulation studies aligns closely with both a fundamental understanding of the drug compound and fit-for-purpose demand for development of the drug product.

Early formulation development requires integration of API properties (such as crystallinity and form transformation) with drug product design (such as solubility, dissolution and stability). At CfPC, the form screen and selection criteria incorporate attributes of the API as well as the demands of formulation requirements. We have the experience in screening and developing PK and Tox formulation, such as solution, suspension and enabling formulations. We also develop most appropriate FIH formulations, including powder in bottle, powder in capsule, formulated forms and injectable formulation. We apply various formulation technologies to improve bioavailability through solubility enhancement, such as in situ salt formation, pH adjustment, co-solvents, cyclodextrin complexation, particle size reduction, amorphous solid dispersions, lipid-based formulation and nanosuspension.

With meticulous planning, CfPC anticipates that potential concerns may occur throughout all stages of pre-and early formulation development, as shown by toxicology and pharmacokinetics (tox/PK) and first-in-human (FIH) service. This approach allows CfPC to strategize solutions and contingencies for most of the critical events that may be encountered during formulation research and regulatory phases. For this purpose, the development of an API at CfPC is aimed at not only improved properties of drug compound but also synchronized support for formulation design and progress at various stages of drug development.

Drug developability assessment

Equilibrium solubility and pH solubility profiles

Chemical and physical stability investigation under various conditions

Excipient compatibility to support formulation design

PK and Tox formulation screening

Enabling formulation design for poorly soluble compounds

Dissolution testing in aqueous and biorelevant media