The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers
Authors Cheng Y, Lin BJ, Guo JH, Huang BL, Fang LP, Que WC, Liu MB, Chen XF, Qiu HQ
Received 10 May 2019
Accepted for publication 30 August 2019
Published 18 October 2019 Volume 2019:13 Pages 3625—3634
Checked for plagiarism Yes
Review by Single-blind
Peer reviewer comments 2
Editor who approved publication: Dr Qiongyu Guo
Yu Cheng,1 Bi-Juan Lin,1 Jin-Hua Guo,1 Bing-Lin Huang,1 Lin-Ping Fang,1 Wan-Cai Que,1 Mao-Bai Liu,1 Xin-Feng Chen,1 Hong-Qiang Qiu1,2
1Department of Pharmacy, Fujian Medical University Union Hospital, Fuzhou 350001, People’s Republic of China; 2College of Pharmacy, Fujian Medical University, Fuzhou 350004, People’s Republic of China
Correspondence: Hong-Qiang Qiu; Xin-Feng Chen
Department of Pharmacy, Fujian Medical University Union Hospital, 29 Xin Quan Road, Gulou, Fuzhou 350001, Fujian, People’s Republic of China
Tel +86 591 8621 8591; +86 591 8621 8371
Fax +86 591 8621 8591
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Purpose: The aim of this study is to assess the bioequivalence of a new generic formulation and the branded formulation of levocetirizine dihydrochloride in healthy Chinese volunteers under fasting and fed conditions, and food-intake effect on the pharmacokinetic properties is also evaluated.
Patients and methods: Volunteers were randomly allocated into two groups to receive a single oral dose of generic formulation and branded formulation under fasting or fed conditions, respectively. Blood samples were collected at designated time points. Plasma concentrations of levocetirizine were determined by UFLC-MS/MS. Safety evaluations were carried out through the study. The main pharmacokinetic parameters of the two formulations of levocetirizine were calculated using non-compartmental analysis incorporated in WinNonlin® 7.0 software.
Results: Forty-nine volunteers were enrolled; 46 completed the studies. Under fasting and fed conditions, the 90% confidence intervals for the geometric mean of generic/branded ratios were in the range of 94.75–107.24% and 99.98–114.69% for the maximum observed concentration, and 97.13–102.50% and 98.36–103.98% for the area under the concentration–time curve. As a result of food intake before administration, the reduced rate and extent of absorption of levocetirizine were observed. Both formulations were generally well tolerated, with no serious adverse reactions reported.
Conclusion: The two formulations demonstrated essentially identical pharmacokinetic profiles and were all well within the FDA/CFDA bioequivalence standards. Meanwhile, food intake can delay the absorption rate and reduced the bioavailability of levocetirizine in healthy Chinese volunteers.
Keywords: levocetirizine, pharmacokinetics, bioequivalence, food effect, healthy Chinese volunteers
Erratum for this paper has been published
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