Pre-Formulation Development

With a very small quantity of active pharmaceutical ingredients (API) or drugable candidate molecules,
WuXi AppTec’s pre-formulation service can provide valuable information and expertise to guide the compounds to next steps. WuXi’s pre-formulation team has extensive experience handling a wide range of compounds and can suggest the path forward for early success.

Preclinical candidate characterization

Solubility:

  • pH solubility profile
  • Solubility in organic solvents
  • Solubility in Fasted State Simulated Intestinal Fluid (FaSSIF), Fed State Simulated Intestinal Fluid (FeSSIF) and Simulated Gastric Fluid (SGF)

Stability:

  • Solution stability, solid state stability, ICH photostability

Inherent properties:

  • pKa, Log p/Log D, Intrinsic dissolution, etc.

Enabling formulation development for screening

  • Vehicle selection
  • pH adjustment and co-solvent
  • Surfactant solubilization
  • Nanosuspension
  • Microemulsion
  • Amorphous solid dispersion

CMC Support service

Solid State Characterization

A full spectrum of solid state characterization including PXRD, TGA, DSC, Polarized light microscope (PLM), dynamic vapor sorption (DVS/hygroscopicity), particle size analysis (PSA) and water content is provided to ensure the solid form is well characterized for various aspects.

Polymorph Screening

Polymorph screening is provided to help clients identify as many polymorphs as possible at an early stage to avoid any surprise later in development. The thermodynamically most stable form is determined and recommended to clients. Several packages of polymorph screening are provided to give full flexibility to meet client priority and timelines requirements.

Crystallization Process Development

WuXi provides full support on crystallization process including but not limited to polymorphism investigation, crystal size distribution measurement and drying investigation to ensure a robust crystallization process able to deliver API with desired properties.

Formulation Support:

  • Excipient compatibility studies
  • Micromeritics (powder properties evaluation)