Comparison of levocetirizine pharmacokinetics after single doses of levocetirizine oral solution and cetirizine dry syrup in healthy Japanese male subjects

Figures & data

Figure 1. Mean (+SD) plasma concentration-time plots of levocetirizine after single dose of levocetirizine OS 5 mg (○) and cetirizine DS 10 mg (•) under the fasting condition in 20 healthy Japanese male subjects. OS, oral solution; DS, dry syrup; hr, hour.

Table 1. Plasma levocetirizine pharmacokinetic parameters following a single oral administration of levocetirizine OS 5 mg and cetirizine DS 10 mg in 20 healthy Japanese male subjects.

Treatment	Cmax (ng/mL)	tmax (h)	AUC0–48 (ng.h/mL)	AUC0–∞ (ng.h/mL)	%AUCex (%)	t1/2 (h)
Levocetirizine OS 5 mg	203.3 (42.49)	0.75 (0.50–1.50)	1814.9 (304.22)	1844.7 (317.56)	2.19 (0.77)	7.91 (1.00)
Cetirizine DS 10 mg	196.5 (31.31)	1.00 (0.50–1.50)	1710.5 (263.31)	1737.1 (278.99)	2.35 (0.71)	7.85 (1.00)

All parameters are reported as arithmetic mean (SD), except t_max as median (range).

OS, oral solution; DS, dry syrup; C_max, maximum concentration; t_max, time to reach the maximum concentration; AUC_0–48, plasma concentration-time curve from dosing until 48 h post-dose; AUC_0–∞, AUC from dosing to infinity; %AUCex, percentage of the extrapolation from AUC_0–t to AUC_0–∞; t_1/2, terminal half-life; h, hour.

Table 2. Comparison of the geometric least squares mean ratio and 90% confidence interval of AUC_0-48 and C_max for levocetirizine OS 5 mg and cetirizine DS 10 mg in twenty healthy Japanese male subjects.

Pharmacokinetic parameter	Geometric LS mean		Ratio* of geometric LS mean	90% CI of ratio*
	Levocetirizine OS 5 mg	Cetirizine DS 10 mg
Cmax (ng/mL)	199.57	194.27	1.027	0.968–1.091
AUC0–48 (ng h/mL)	1791.58	1692.55	1.059	1.024–1.094

*Ratio = Geometric LS mean of levocetirizine oral solution 5 mg/Geometric LS mean of cetirizine dry syrup 10 mg.

OS, oral solution; DS, dry syrup; LS mean, Least Square mean; C_max, maximum concentration; AUC_0–48, plasma concentration-time curve from dosing until 48 h post-dose; CI, confidence interval; h, hour.