Abstract

Aims: The aims of this study were to evaluate and compare the pharmacokinetic profiles and establish bioequivalence of test and reference metoprolol succinate extended-release (ER) tablets in healthy Chinese subjects under fasting and fed conditions.
Materials and methods: Subjects were randomly assigned to either the fasting or the fed group and also to one of the two treatment sequences (test-reference or reference-test), according to which they received a single 47.5-mg dose of the test or reference metoprolol ER tablet in the study periods. During each period, blood samples were collected at pre-dose and at intervals up to 48 hours after dosing. Plasma concentrations of metoprolol were determined by liquid chromatography. The safety of both ER tablets was monitored throughout the study. Results: 60 subjects were enrolled and all completed the study, with 30 participants each in the fasting and fed groups. In both groups, the 90% confidence intervals for AUC_0–48h, AUC_0–inf, and C_max were within the acceptable bioequivalence range (80 – 125%). There were no significant differences in adverse event (AE) reporting between the subjects receiving test or reference ER tablet. No serious AEs occurred during the study period.
Conclusion: The test metoprolol ER tablet was bioequivalent to the reference metoprolol ER tablet (Betaloc ZOK) in healthy Chinese subjects measured under both fasting and fed conditions. Both formulations were well tolerated by all study participants.

Author Details

Authors

• Xiding Yang^{1, 4}
• Ronghua Zhu^{1, 4}
• Xiaojun Chen²
• Jingjing Li¹
• Guirong Luo²
• Lingfeng Yang^{3, 4}
• Xiao Fan^{1, 4}
• Qiangyong Yan¹
• Wenxing Peng¹
• Pingfei Fang^{1, 4}

Departments

• ¹ Department of Pharmacy, The Second Xiangya Hospital of Central South University, Changsha,
• ² Guangxi Houde Health Industry Co. Ltd., Guangxi,
• ³ Department of Metabolism and Endocrinology, and
• ⁴ Phase I Clinical Trial Center, The Second Xiangya Hospital of Central South University, Changsha, China

Address

Ronghua Zhu
Department of Pharmacy
The Second Xiangya Hospital of Central South University
Changsha, Hunan 410011, China
Email: [email protected]

Citation