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J.Health Sci., 51(3), 308-316, 2005
Pharmacokinetics of Indomethacin, a Metabolite of Acemetacin, Following a Single dose and Multiple doses Administered as Acemetacin Sustained-Release Tablets in Healthy Male Volunteers
Dong-Mei Li, Wan-Liang Lu,* Xue-Qing Wang, Jian-Cheng Wang, Hua Zhang, Rui-Juan Zhang, Gui-Lin Wang, Xuan Zhang, and Qiang Zhang
Department of Pharmaceutics, Peking University School of Pharmaceutical Sciences, Xueyuanlu 38, Beijing 100083, P.R. China
The objective of this study was to estimate the pharmacokinetics of the newly developed once-daily acemetacin sustained-release tablets compared with those of the commercial acemetacin sustained-release capsules. Ten male healthy Chinese volunteers were included in the study. The administration schedule was a randomized crossover design. Each volunteer received 90 mg of the tablet or the capsule in the single-dose study, and each received 90 mg of the tablet or the capsule once daily for 6 consecutive days in the multiple-dose study. The areas under the concentration-time curve (AUC0-24 hr), maximal concentrations of indomethacin (Cmax), time to reach peak concentration (Tmax), and elimination half-life (T1/2) values of indomethacin (an active metabolite of acemetacin) were 6.72 ± 0.99 mu g.hr/ml, 0.82 ± 0.08 mu g/ml, 4.2 ± 0.6, and 10.1 ± 4.2 hr, respectively. The steady-state AUC120-144 hr and steady-state maximal concentration of the tablets increased to 10.33 ± 1.06 mu g.hr/ml and 1.14 ± 0.10 mu g/ml, respectively. The pharmackinetic parameters (AUC0-24 hr, Cmax, T1/2, and mean residence time) for two formulations were not significantly different but the average Tmax of the tablets was delayed by 1 hr compared with that of the capsules (4.2 ± 0.6 vs. 3.2 ± 0.6 hr, p < 0.05). The mean relative bioavailability of the tablets was 97.9 ± 14.8% compared with that of the capsules. It could be concluded that the pharmacokinetic parameters of the newly developed sustained-release tablets are similar to those of the sustained-release capsules, excluding the Tmax value. A significant correlation was obtained between the in vivo mean absorption rate and the in vitro mean dissolution rate for the newly developed sustained tablets.
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