카베딜를(25 mg)정제의 생물학적 동등성 및 약물동태연구

Bioequivalence and Pharmacokinetics of Carvedilol (25 mg) Tablets in Volunteers

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 Feod 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 AUC0- 30hr, AUCinf, Cmax, Tmax, t1/2, Cl/F and VβF were calculated. ANOYA test and t-test were utilized for the statistical analysis of each parameter. The results showed that the differences in AUC0-30hr C,sub>max, and Tmax, between two tablets were ∼5.66, 1.74 and 0.00%, respectively, Minimum detectable differences (△) at u=0.05 were less than +/- 20% except Tmax: (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.