Pharmacokinetics and Bioequivalence Evaluation of Two Acipimox Tablets: A Single-Dose, Randomized-Sequence, Two-Way Crossover Study in Healthy Chinese Male Volunteers

J. Huang; R. Chen; C. Wei; R. Li; G. Yuan; X. Liu; B. Wang; R. Guo

doi:10.1055/s-0032-1333228

Drug Research, Table of Contents

Drug Res (Stuttg) 2013; 63(02): 79-83
DOI: 10.1055/s-0032-1333228

Original Article

Pharmacokinetics and Bioequivalence Evaluation of Two Acipimox Tablets: A Single-Dose, Randomized-Sequence, Two-Way Crossover Study in Healthy Chinese Male Volunteers

J. Huang

¹The Institute of Pharmacology, Medical Faculty of Shandong University, Jinan, China

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

R. Chen

¹The Institute of Pharmacology, Medical Faculty of Shandong University, Jinan, China

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

C. Wei

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

R. Li

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

G. Yuan

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

X. Liu

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

B. Wang

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

,

R. Guo

²The Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China

› Author Affiliations

Abstract

Objective:

The study was designed to compare the pharmacokinetic parameters and relative bioavailability of a newly generic acipimox 250-mg tablets (test formulation) with a branded 250-mg tablets (reference formulation).

Methods:

A single-dose, randomized-sequence, 2-way crossover study was conducted in 20 healthy Chinese male volunteers in the fasted state. Plasma samples were collected over 12 h after a single oral dose of 250-mg acipimox test or reference, followed by a 7-day washout period. Plasma concentrations of acipimox were analyzed by high-performance liquid chromatography. Drug And Statistical-Version 2.0 was used to calculate the pharmacokinetic parameters and assess bioequivalence of the 2 formulations. It is considered bioequivalent if the 90% CIs of the mean ratios (test: reference) for C_max, AUC_0–t and AUC_0–∞ are all within the range from 80% to 125%.

Results:

No period, formulation, or sequence effects were observed on any pharmacokinetic parameters. The main pharmacokinetic parameters for the test and reference were as follows: t_1/2 were 1.412±0.168 h and 1.390±0.162 h; T_max were 1.850±0.462 h and 1.800±0.571 h; C_max were 4.035±1.055 μg · ml^-1 and 3.858±0.986 μg · ml^-1; AUC_0–12 were 14.006±2.564 μg · ml^-1 · h and 13.345±2.128 μg · ml^-1 · h, and the AUC_0–∞ were 14.147±2.568 μg · ml^-1 · h and 13.486±2.117 μg · ml^-1 · h. The 90% CIs for the ratios (test/reference) of C_max, AUC_0–12, and AUC_{0 − ∞} were 98.0–111.2%, 100.8–108.5%, and 100.8–108.3%, respectively.

Conclusions:

In this small study, a single 250-mg oral dose of an acipimox tablet (test formulation) is bioequivalent to the established reference formulation.

Key words

determination - acipimox - HPLC

Full Text

References

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