14 January 2019

Publication: Relative bioavailability of two novel orally dispersible tablet formulations of praziquantel

In January 2019, researchers from the Pediatric Praziquantel Consortium published the results of two Phase I pharmacokinetic studies in healthy adult volunteers. 

The aim was to assess relative bioavailability of praziquantel (PZQ) in two novel orally dispersible tablet (ODT) formulations (levo‐ and racemic PZQ) compared with that of a reference (racemic) PZQ formulation (Cysticide) after single oral administration of 40 mg per kg of body weight.

For the novel racemic PZQ ODT, relative bioavailability was comparable to that of reference PZQ. For levo-PZQ ODT, it was ~40% of the reference. With both ODTs, mean plasma concentration-time profiles were erratic and exposure increased non-dose‐proportionally. There were no safety signals with either formulation.

The studies show that it may not be possible to construct appropriate models for pediatric extrapolation for products like PZQ with variable and erratic pharmacokinetic profiles. Limits in the understanding of dose‐exposure relationships for PZQ and its enantiomers have also become apparent.

Publication in Clinical and Translational Science: https://ascpt.onlinelibrary.wiley.com/doi/full/10.1111/cts.12601