Successful Formulation Strategies: Modifying the micro-environment to improve dissolution rate.

 

The Challenges

Solubility is a problem in the development of formulations of poorly soluble drugs.

Limited solubility can lead to formulations with inadequate oral bioavailability.

 

The Solution

Option 1: Use a spray drying process to form an amorphous solid dispersion. The process can be tricky and typically results in longer project timelines and higher costs.

Option 2: Make water soluble salts of poorly soluble (BCS II or IV) acidic or basic drugs. However, upon contact with water in GI fluids, these salts can undergo dissociation and spontaneous precipitation if the pH generated during dissolution is not sufficient to maintain solubility of the free acid or free base.

Option 3: Use excipients to modify the pH or solubility conditions at the surface of the dissolving salt to minimize precipitation. This approach utilizes conventional methods of manufacture, i.e., a high shear granulation and compression process.