Abstract

Dosage form (formulation) and enabling technologies play a vital role for the success of new chemical entities transitioning from preclinical to clinical development through commercialization. The majority of new chemical entities being discovered in many disease areas have a poor aqueous and biorelevant solubility. These are often available in the amorphous and chemically impure form for in-vitro enzyme assays, pharmacokinetic, pharmacological and toxicological studies in animal models.  These molecules are often dosed as a suspension/solution orally/parenterally respectively and candidate selection is based on results obtained from these studies.  Therefore, it is very important to select a physical form as early as possible so that the same form can be used for preclinical and clinical studies, as changes in physical form or formulation principle could significantly affect the pharmacokinetic performance and formulation characteristics (i.e. stability/solubility/compatibility) and toxicity. The selected candidate must exhibit adequate physical and chemical stability during the formulation development process with desirable pharmacokinetic parameters. If pharmacokinetics parameters of these molecules are different due to different physical form or formulation selection, a significant delay may occur during development. It’s important to explore enabling technologies with existing molecules depending on the clinical/market need.  This presentation will cover early formulation strategies And novel technologies to improve bioavailability of poorly soluble drugs.