Zielgruppe

This seminar is aimed at all pharma professionals engaged in the development and evaluation of drug formulations, in particular in early development phase. The seminar will cover all aspects of this topic starting from the solid state characteristics of drug substances of significance, the basics for the different formulation principles, guidance as to which principle to choose for which type of API, and recent development in the testing and evaluation of formulations with respect to bioavailability. Relevant case studies presented by experts in the field will open up the discussion of connected issues in groups. These group discussions may suggest alternative approaches or strategies and add to the profit for each participant. There is also room to discuss further cases coming from the audience.

Zielsetzung

Preformulation is the key to successful drug development. In the preformulation phase, the physicochemical properties of APIs are characterized, potential liabilities are identified, and step by step various formulation approaches are screened and compared in order to turn Active Pharmaceutical Ingredients (APIs) into drugs which progress into (pre-)clinical programs. This requires a critical set of compound sparing assays that gain information about solid state properties (e.g. crystallinity, melting point, hygroscopicity, polymorphism), solubility (thermodynamic and respectively kinetic), dissolution (intrinsic dissolution and from powder), permeability, and stability (chemical, physical). This sound data pakkage is the basis for the rational choice of formulation principles and for (preclinical) formulation development that takes bioavailability, manufacturability, and potential development risks into account. Formulations considered during the course range from conventional to enabling formulations such as solubility (e.g. cosolvents, cyclodextrins, lipids), dissolution (e.g. salts, amorphous solid dispersions), permeability-enhancing (e.g. Pg-p inhibitors) formulations or formulations stabilizing supersaturated states.
This course covers the “whys” and “hows” of preformulation work and provides guidance for efficient preclinical formulation development.