Preformulation Studies

Preformulation studies play a significant role in optimizing formulation development plans. Our scientists have performed these exploratory activities for more than one hundred clinical candidates, providing the necessary groundwork for formulation and dosage form development by:

  • Evaluating the feasibility of drug product development
  • Facilitating the dosage form development strategy
  • Identifying the feasibility of the parenteral (liquid or lyophilized)
  • Developing excipient screening tools

We offer two preformulation studies: Stability Fingerprinting®, for biotherapeutics, and Solubility FingerprintingTM, for small molecules.

Stability Fingerprinting®

Developing a biological product with the desired stability, efficacy, and clinical presentation can be challenging. Our Stability Fingerprinting® identifies the specific environmental conditions that destabilize your protein, allowing our scientists to account for variations in:

  • pH
  • Ionic strength
  • Temperature
  • Shear stress
  • Freeze/thaw cycles

During development, product conformational integrity and stability is monitored using techniques such as intrinsic and extrinsic fluorescence, right-angle light scattering, SDS-PAGE, SE-HPLC, IEX-HPLC, HIC-HPLC. The conditions and assays used to identify product instabilities will also become important tools used during formulation development. The goal of this process is to prevent product degradation and loss of activity due to hydrolysis, aggregation, multimer formation, deamidation, oxidation, denaturation, or conformational changes.

Stability Fingerprinting® also helps identify stability indicating assays and contributes to excipient screening.

Solubility Fingerprinting™

Formulation development strategies can be developed based on the solubility of the small molecules, some of the essential preformulation studies also includes understanding the following characteristic of the small molecules, some of the information can be obtained based on the release characterization of the API.

Preformulation characterization of small molecules can include:

  • Solubility screening
  • Phase transitions, melting points and microscopic changes
  • Investigation into polymorphic and or crystal forms
  • pKa determination
  • Dissolution
  • Forced degradation studies
  • Oxidation
  • Hydrolysis
  • Hygroscopicity
  • Identification of degradation products
  • Excipient and active compatibility studies
  • Particle size measurements
  • Physical characterization of drug delivery systems and vehicle optimization
  • Problem solving of existing processes and formulations
  • Partition co-efficient determination