The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers

• Published in: Drug design, development and therapy Vol. 13; pp. 3625 - 3634
• Main Authors: Cheng, Yu, Lin, Bi-Juan, Guo, Jin-Hua, Huang, Bing-Lin, Fang, Lin-Ping, Que, Wan-Cai, Liu, Mao-Bai, Chen, Xin-Feng, Qiu, Hong-Qiang
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.01.2019; Taylor & Francis Ltd; Dove; Dove Medical Press
• Subjects: Absorption; Administration, Oral; Adolescent; Adult; Alcohol; Allergies; Analysis; Area Under Curve; Asthma; Bioavailability; bioequivalence; Biological Availability; Blood & organ donations; Cetirizine - administration & dosage; Cetirizine - adverse effects; Cetirizine - pharmacokinetics; Chromatography, High Pressure Liquid; Confidence intervals; Cross-Over Studies; Drug dosages; Drugs, Generic - administration & dosage; Drugs, Generic - adverse effects; Drugs, Generic - pharmacokinetics; Evaluation; Fasting; Female; Food; food effect; Food intake; Food-Drug Interactions; Generic drugs; Glycoproteins; healthy Chinese volunteers; Histamine H1 Antagonists, Non-Sedating - administration & dosage; Histamine H1 Antagonists, Non-Sedating - adverse effects; Histamine H1 Antagonists, Non-Sedating - pharmacokinetics; Hospitals; Humans; Laboratories; Laboratory testing; Levocetirizine; Male; Mathematical analysis; Original Research; Pharmacokinetics; Pharmacology; Pharmacy; Pilot Projects; Quality; Tandem Mass Spectrometry; Therapeutic Equivalency; Young Adult; China; United States > US; pharmacokinetics; healthy Chinese volunteers; levocetirizine; food effect; bioequivalence
• ISSN: 1177-8881; 1177-8881
• DOI: 10.2147/DDDT.S215316

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. 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. 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. 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.