|
Carvedilol is a nonselective β-blocking agent with vasodilating properties that are attributed mainly to its blocking activity at α₁-receptors. Carvedilol is used in the treatment of mild to moderate hypertention and angina pectoris and is often used in combination with other drugs. This study was carried out to evaluate the bioequivalence and pharmacokinetics of two carvedilol 25 mg tablet formulations according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty healthy volunteers are enrolled and received a single dose (25 mg as carvedilol) of each drug in the fasting state, in a randomized 2-way crossover design. After oral administration, blood samples were collected for a period of 30 hours. Plasma concentrations of carvedilol were determined by a rapid and sensitive HPLC method with spectrofluorometric detection. The maior pharmacokinetic parameters such as AUC_(0- 30hr), AUC_inf, C_max, T_max,t_(1/2), Cl/F and V_(β)/F were calculated. ANOVA test and t-test were utilized for the statistical analysis of each parameter. The results showed that the differences in AUC_(0-30hr) C_max, and T_max, between two tablets were ∼5.66, 1.74 and 0.00%, respectively. Minimum detectable differences (△) at α=0.05 were less than ± 20% except T_max : (8.44, 18.36, and 33.86%, respectively). The 90% confidence intervals of all parameters were within ± 20% (-10.60 ∼-0.72, -9.00∼ 12.49 and -19.81 ~ 19.81%, respectively). Therefore, it is concluded that the two formulations are bioequivalent for both the extent and the rate of absoftion after single dose administration.
|