Case Study: Poor Solubility and Rapid Degradation in Acid

Irisys was challenged to formulate for oral administration a compound characterized by low solubility in both water and oil, which also degraded rapidly in acid. As might be expected, bioavailability in preliminary trials was poor.

A semi-solid matrix was developed that withstood heating to liquify for capsule filling. Capsules were enteric-coated to protect the active ingredient from degradation in acid.

Preclinical and human studies showed significant improvement in bioavailability.