Case Study: Bioavailability Enhancement

Poor bioavailability is a problem often faced in the drug development process. It is, in fact, one of the main reasons why companies work with Aptuit and SSCI Inc., its solid state chemistry company. Purdue Pharma brought a compound to SSCI that demonstrated poor water solubility and low in vivo concentrations when tested orally in dogs. In order to improve bioavailability, a more water soluble form of the active pharmaceutical ingredient (API) was required.

After preliminary testing and screening without forming a salt, Aptuit scientists decided that the next course of action to solve this bioavailability problem would be to examine the potential of forming cocrystals for the specific purpose of increasing the dissolution rate. Cocrystallization is a fairly new approach within the pharmaceutical industry that can produce alternative, viable solid forms when a more standard approach of salt and polymorph formation fails to deliver. In the Purdue case, 5 new solid phases were identified and confirmed to be cocrystals. The cocrystal with the most promising physical properties and characteristics was selected for further testing.