Abstract

Pascal St-Laurent* and François-Xavier Lacasse

ABSTRACT

The dissolution test is a test that is mandatory for any molecular entity formulated under a solid dosage form such as hard/ soft gelatin capsules or tablets. Performing a dissolution test is not, per se, a challenge since dissolution apparatus type one (1) or two (2) have been well designed for this purpose. Numerous dissolution methods exist for generic and innovator drugs. These methods are developed daily. During the 80’s and the beginning of the 90’s, drug substances were classified highly soluble and permeable (BCS1); Formulation and dissolution method developments were not as challenging as they are nowadays. However, over the past 20 years, since molecules have become more and more hydrophobics, not soluble (BCS 2, 4) and permeable (BCS2) or not (BCS4), the formulation development became increasingly important to make these drug substances more soluble or at least to show a “workable” solubility rate for dissolution method development. It is one thing to generate solubility profile for a drug substance, but it is completely different for a drug product (formulated product) to get the same profile. The best scenario would be that the formulation is not held responsible for any differences in the drug substance’s profile. The authors of this short communication, an analytical chemist, and a formulator show more than 40 years of experience in drug development and have been through these challenges with different kinds of drug substances. They will try to expose, based on their experiences, expertise and proven track records that formulation development combined with dissolution method development should be considered artistry, as getting a discriminatory dissolution method is not as easy as it seems.