Comparative pharmacokinetics of a montelukast/levocetirizine fixed-dose combination chewable tablet versus individual administration of montelukast and levocetirizine after a single oral administration in healthy Korean male subjects
| Autor: | Seol Ju Moon, Yong Il Kim, Kyung Sang Yu, Jina Jung, Min-Gul Kim |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Cyclopropanes
Male 050101 languages & linguistics Fixed-dose combination Cmax Administration Oral 02 engineering and technology Acetates Sulfides Bioequivalence Pharmacology Levocetirizine Pharmacokinetics Oral administration Republic of Korea 0202 electrical engineering electronic engineering information engineering medicine Humans 0501 psychology and cognitive sciences Pharmacology (medical) Montelukast Cross-Over Studies business.industry 05 social sciences Crossover study Cetirizine Healthy Volunteers Drug Combinations Therapeutic Equivalency Area Under Curve Quinolines 020201 artificial intelligence & image processing business Tablets medicine.drug |
| Zdroj: | Int. Journal of Clinical Pharmacology and Therapeutics. 58:354-362 |
| ISSN: | 0946-1965 |
| Popis: | Objective Asthma patients often have co-existing symptoms of allergic rhinitis and are often prescribed with both asthma and rhinitis treatments such as montelukast and levocetirizine. The objective of this study was to compare the pharmacokinetic profiles of a montelukast/levocetirizine fixed-dose combination chewable tablet with individual administration of montelukast and levocetirizine in healthy subjects. Materials and methods A randomized, open-label, single-dose crossover study was conducted in healthy male subjects. One of the following treatments was administered in each period: co-administration of 1 chewable tablet of montelukast 5 mg and 1 tablet of levocetirizine 5 mg or administration of 1 chewable tablet of montelukast/levocetirizine 5/5 mg fixed-dose combination. Serial blood samples were collected up to 48 hours post dose. Plasma drug concentrations were measured by liquid chromatography/tandem mass spectrometry. Pharmacokinetic parameters, including maximum plasma concentration (Cmax) and area under the plasma concentration versus time curve from dosing to the last measurable concentration (AUClast), were determined by non-compartmental analysis. The geometric least-square mean (GLSM) ratios and associated 90% confidence intervals (CIs) of Cmax and AUClast were calculated to evaluate pharmacokinetic equivalence. Results A total of 22 subjects were included in pharmacokinetic analysis. The GLSM ratios and 90% CIs of Cmax and AUClast were 1.0054 (0.9535 - 1.0601) and 1.0628 (1.0013 - 1.1281) for montelukast and 1.0105 (0.9488 - 1.0764) and 1.0396 (0.9935 - 1.0879) for levocetirizine, respectively. Conclusion The pharmacokinetic parameters of montelukast and levocetirizine when administered as separate tablets or as a fixed-dose combination were compared, and the parameters met the pharmacokinetic equivalence criteria. (ClinicalTrials.gov Identifier: NCT03371849). |
| Databáze: | OpenAIRE |
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