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The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers.
- Source :
-
Drug design, development and therapy [Drug Des Devel Ther] 2019 Oct 18; Vol. 13, pp. 3625-3634. Date of Electronic Publication: 2019 Oct 18 (Print Publication: 2019). - Publication Year :
- 2019
-
Abstract
- 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.<br />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 <superscript>®</superscript> 7.0 software.<br />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.<br />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.<br />Competing Interests: The authors report no conflicts of interest in this work.<br /> (© 2019 Cheng et al.)
- Subjects :
- Administration, Oral
Adolescent
Adult
Area Under Curve
Biological Availability
Cetirizine adverse effects
Cetirizine pharmacokinetics
Chromatography, High Pressure Liquid
Cross-Over Studies
Drugs, Generic adverse effects
Drugs, Generic pharmacokinetics
Female
Histamine H1 Antagonists, Non-Sedating adverse effects
Histamine H1 Antagonists, Non-Sedating pharmacokinetics
Humans
Male
Pilot Projects
Tandem Mass Spectrometry
Therapeutic Equivalency
Young Adult
Cetirizine administration & dosage
Drugs, Generic administration & dosage
Food-Drug Interactions
Histamine H1 Antagonists, Non-Sedating administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1177-8881
- Volume :
- 13
- Database :
- MEDLINE
- Journal :
- Drug design, development and therapy
- Publication Type :
- Academic Journal
- Accession number :
- 31695330
- Full Text :
- https://doi.org/10.2147/DDDT.S215316