Pharmacokinetics of long-acting (LA) capsule of carteolol hydrochloride were investigatedin healthy adult male volunteers. The LA group received 15 mg/person once daily whilethe comparison group received conventional tablets (CT), 5 mg/person, three times a day, for 9 days of repeated administration.
The plasma concentrations of both the LA and CT groups reached a steady-state on Day3.
Although the pharmacokinetic parameters, AUC, Cmax, Cmin, and Cmax/Cmin in the steadystaterevealed no significant differences between the two groups, t1/2 was significantlydifferent between LA (9.3hr), and CT (6.9hr).
The plasma concentration profile on the LA repeated adminitsration corresponded wellto the prediction curves estimated from the LA single administration study. T1/2 in thesteady-state of LA dosing was quite similar to that of a single adminitsration of LA. Thesefacts reveal that the prolongation of plasma concentration maintained by LA administrationdid not cause any accumulation of carteolol nor any change in the pharmacokinetics.
In conclusion, a once-daily administration by LA capsule is proposed as being clinicallyuseful.