Low Density, Unstable Drug for Controlled Release Delivery

Case Study 7: Formulation of Low Density and Unstable Drug for Controlled Release Delivery

The characteristics of the API included low density, low melting point, cohesive nature and unstable in presence of water in addition to lot-to-lot variation.

An API densification process was used to make the API suitable for uniform filling into hard capsules for Phase 1 pharmacokinetics studies.

The PK data and pre-formulation characterization of the API (determination of pKa, solubility in various solvents, moisture uptake and DSC and TGA) were used to design and develop a controlled-release tablet for continued clinical study.

A suitable dosage form has been developed and the sponsor has filed a patent to protect their intellectual property.