Analytics of dissolution testing of products containing nanosized drugs with a view to predicting plasma profiles

The oral bioavailability of a drug substance is strongly related to its aqueous solubility.

Only complete dissolution during the GI-passage can maintain an optimal

bioavailability. Poor aqueous drug solubility results, according to the Nernst-Brunner

equation into a slow dissolution rate, sometimes too slow for complete dissolution in

the GI tract. The dissolution rate increases with decreasing particle size and therefore

increasing surface area of the drug particles. In consequence,, micronization of the

drug is applied to increase oral bioavailability, but often meets with modest success.

Recently developed techniques were applied to decrease the particle size into the

nanometer range. For some substances, pharmacokinetic parameters could be

influenced decisively, e.g. the obviation of a food effect for the drugs aprepitant and

fenofibrate.