Safety, Tolerability and Bioequivalence Assessment of a Dispersible Tablet Formulation of Pyrazinamide

Abstract

Pyrazinamide is a widely used drug for the treatment of tuberculosis. A 150 mg Dispersible Tablet (DT) formulation of the drug was prepared by Micro Labs, a generic drug company. The formulation was developed for easy administration into paediatric patients. It was tested for bioequivalence in healthy adult human volunteers in fasting condition. A total of 36 subjects were enrolled in the study and all the 36 subjects completed both the two periods of the study without showing major adverse events. The pharmacokinetic parameters determined for bioequivalence were Cmax and AUC0-t. The two parameters were within the limit of bioequivalence criteria. The 150 mg DT formulation developed by Micro Labs was found to be bioequivalent to 500 mg immediate release tablet formulation of Riemser Pharma. Both the formulations were safe and well tolerated among the tested human subjects. No major adverse events were observed.

Bioequivalence and Pharmacokinetic Evaluation of 2 Pyrazinamide Formulations in Healthy Chinese Adults: A Single‐Dose, Open‐Label, Randomized‐Sequence, 2×2 Crossover Study

“…There are a few reports on the pharmacokinetics of PZA, but most of the reports did not evaluate the bioequivalence of PZA alone. In a safety, tolerability, and bioequivalence assessment of a dispersible tablet formulation of PZA, 8 a total of 36 subjects were enrolled and the bioequivalence of 2 formulations were tested under fasting condition. The C max and AUC 0‐t of reference formulation of PZA (0.5 g/tablet) were 13.925 μg/mL and 161.053 μg • h/mL , respectively, which were slightly lower than our study.…”