关键词: 比卡鲁胺, 比卡鲁胺, 比卡鲁胺, 药动学, 药动学, 药动学, HPLC, HPLC, HPLC, 生物等效性, 生物等效性, 生物等效性

Abstract:

Aim To establish a HPLC method for the determination of bicalutamide plasma concentration and to evaluate the bioequivalence of bicalutamide capsules (test) and tablets (reference). Methods A single oral dose of 50 mg bicalutamide capsules or tablets were given to 48 Chinese healthy volunteers in a one period parallel design test. Bicalutamide in plasma was analyzed using a XB-C18 column with a mobile phase of acetonitrile-water (60:40, V/V) and the dectection wavelength of272 nm and it is pharmacokinetic parameters were calculated and evaluated using DAS2.0. Results The linear range of bicalutamide was 10 – 1200 ng·mL^-1. The main pharmacokinetic parameters of the test and reference were as the followings, t1/2 (138.36 ± 32.03) and (146.12 ± 27.04) h, Tmax (17.17 ± 4.65) and (16.92 ± 4.85) h, Cmax (910.83 ± 130.49) and (868.71 ± 115.35) ng·mL^-1, AUC0-672 (172437.08 ± 3986.07) and (176842.34 ± 35733.85) ng·mL^-1·h, and AUC0-∞ (179456.55 ± 43127.65) and (185270.39 ± 39688.63) ng·mL^-1·h, respectively. The two-one side t-test analysis showed that the confidence intervals of Cmax, AUC0-672 and AUC0-∞ were (98.9% – 100.7%), (98.8% – 100.6%) and (99.7% – 101.7%), respectively. Conclusion The relative bioavailability of bicalutamide capsules was 97.51%. The bioequivalence was demonstrated by the two-one side t-test.

Key words: Bicalutamide, Bicalutamide, Pharmacokinetics, Pharmacokinetics, HPLC, HPLC, Bioequivalence, Bioequivalence