Pharmacokinetic evaluation of an azithromycin controlled release dosage form in healthy human volunteers: a single dose study.

Azithromycin (AZI) follows a two-compartment model pharmacokinetically. The purpose of this study was to evaluate the in vivo performance of a controlled release (CR) formulation of AZI, which would eliminate the risk of high peak plasma concentrations obtained within 2-3 h after peroral administration of immediate release (IR) products. The study was conducted in twelve healthy male human volunteers to compare an experimental NIPER product (CR tablets) with Vicon (IR tablets) at the same dose level as a single-dose, randomized, one-period, two-treatment, and parallel-study. Concentrations of AZI in serum samples were assessed using the validated HPLC method. From the serum concentration-time profiles various pharmacokinetic parameters (AUC(0-96), AUC(0-inf), C(max) and T(max)) were calculated for both products. Results showed that the high peak concentration obtained by administration of a conventional IR formulation were eliminated with the CR product. A mean dosage form index (DI) of 1.17 with fluctuations of 7.57% was obtained with the CR product at steady state level, indicating reduced fluctuations at the steady state serum concentrations. Elimination of the pronounced peak as well as fluctuations reduced or minimized AZI adverse effects associated with the IR product.

RCT Entities:   Population Interventions Outcomes