In:
Clinical and Translational Science, Wiley, Vol. 12, No. 1 ( 2019-01), p. 66-76
Abstract:
Orally dispersible tablet ( ODT ) formulations of levo praziquantel ( L‐PZQ ) and racemic PZQ (rac‐PZQ) are being developed to treat schistosomiasis in preschool‐aged children. Two crossover studies ( N = 32 and 36, respectively) assessed the relative bioavailability of these ODT s vs. Cysticide in adults. Bioavailability for L‐ PZQ of ODT rac‐ PZQ and Cysticide at 40 mg/kg was comparable (L‐ PZQ area under the concentration‐time curve from zero to infinity ( AUC 0–∞ ) test/reference ratio (90% confidence interval (CI)): 96% (84–111%)), whereas relative bioavailability of ODT L‐ PZQ 20 mg/kg was ~40% that of Cysticide 40 mg/kg (test/reference: 40% (35–46%)). AUC 0‐∞ and peak plasma concentration (C max ) were highly variable in both studies. For both ODT s, L‐ PZQ AUC 0–∞ showed greater than dose‐proportional increase over the ranges tested and a significant food effect. Safety was comparable among formulations. The lower bioavailability of ODT L‐ PZQ , as well as the high variability and nondose‐proportionality of pharmacokinetic (PK) parameters, highlighted the need for a dedicated pediatric dose‐finding study for the selection of the most appropriate formulation and dose (L‐ PZQ ODT or rac‐ PZQ ODT ).
Type of Medium:
Online Resource
ISSN:
1752-8054
,
1752-8062
Language:
English
Publisher:
Wiley
Publication Date:
2019
detail.hit.zdb_id:
2433157-0
