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Comparison of the pharmacokinetics and tolerability of montelukast/levocetirizine administered as a fixed-dose combination and as separate tablets.
- Source :
-
International journal of clinical pharmacology and therapeutics [Int J Clin Pharmacol Ther] 2018 Sep; Vol. 56 (9), pp. 443-450. - Publication Year :
- 2018
-
Abstract
- Objective: A novel fixed-dose combination (FDC) capsule of 10/5 mg of montelukast/levocetirizine may lead to better compliance than two separate tablets taken together. The aim of this study was to evaluate the pharmacokinetics (PK) and tolerability of an FDC of montelukast and levocetirizine compared to separate tablets.<br />Materials and Methods: A randomized, open-label, single-dose, two-sequence, two-period, crossover study was conducted with healthy male subjects. In each period, either an FDC or separate tablets were administered orally, and serial blood samples were collected for PK analysis for up to 34 hours after dosing. PK parameters were calculated using noncompartmental methods. The 90% confidence intervals (CIs) of the geometric mean ratios (GMRs) of the maximum plasma concentration (Cmax) and the area under the curve to the last measurable concentration (AUClast) for the two interventions were estimated. Tolerability assessments were performed for all the subjects who received the drug at least once.<br />Results: The PK profiles of the two interventions were comparable. For montelukast, the GMRs and 90% CIs for the Cmax and AUClast were 0.9800 (0.8903 - 1.0787) and 1.0706 (0.9968 - 1.1498), respectively. The corresponding values for levocetirizine were 0.9195 (0.8660 - 0.9763) and 1.0375 (1.0123 - 1.0634), respectively. Both interventions were well tolerated.<br />Conclusion: The PK and tolerability profiles of montelukast and levocetirizine after a single oral administration were comparable between the FDC and separate tablets. For patients with allergic rhinitis who require a combination treatment, the FDC of montelukast and levocetirizine will be a convenient therapeutic option. .
- Subjects :
- Acetates adverse effects
Acetates blood
Administration, Oral
Adult
Area Under Curve
Biological Availability
Cetirizine adverse effects
Cetirizine blood
Cross-Over Studies
Cyclopropanes
Drug Compounding
Half-Life
Healthy Volunteers
Histamine H1 Antagonists, Non-Sedating adverse effects
Histamine H1 Antagonists, Non-Sedating blood
Humans
Leukotriene Antagonists adverse effects
Leukotriene Antagonists blood
Male
Metabolic Clearance Rate
Middle Aged
Quinolines adverse effects
Quinolines blood
Republic of Korea
Sulfides
Tablets
Young Adult
Acetates administration & dosage
Acetates pharmacokinetics
Cetirizine administration & dosage
Cetirizine pharmacokinetics
Histamine H1 Antagonists, Non-Sedating administration & dosage
Histamine H1 Antagonists, Non-Sedating pharmacokinetics
Leukotriene Antagonists administration & dosage
Leukotriene Antagonists pharmacokinetics
Quinolines administration & dosage
Quinolines pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 0946-1965
- Volume :
- 56
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- International journal of clinical pharmacology and therapeutics
- Publication Type :
- Academic Journal
- Accession number :
- 30021691
- Full Text :
- https://doi.org/10.5414/CP203265