比卡鲁胺片人体生物等效性研究

目的 研究国产比卡鲁胺片在健康人体的药代动力学特征，比较其与同规格进口片剂的生物等效性。方法 20名健康男性志愿者单剂量交叉口服两种比卡鲁胺片，在每次服药前，服药后1、3、4、6、9、12、16、20、24、28、32、36、40、48 h，3、7、14、21、28 d分别采集血样，用HPLC法测定血浆中药物浓度，用3P97软件拟合药代动力学参数，并用SAS软件进行等效性检验。结果 试验组口服国产比卡鲁胺片50 mg后，平均C_max为691.50 μg/L，平均T_max为20.65 h，平均AUC_0～∞为148 124 μg·h/L，平均消除半衰期为127.46 h；对照组口服进口比卡鲁胺片Casodex 50 mg后，平均C_max为697.30 μg·L^-1，平均T_max为24.10 h，平均AUC_0～∞为153 782 μg·h/L，平均消除半衰期为131.06 h。统计分析表明两种制剂生物等效，受试制剂与参比制剂的相对生物利用度为99.43%。结论 两种比卡鲁胺片剂具有生物等效性。

Bioequivalence of bicalutamide tablet in healthy volunteers

Objective To study the pharmacokinetic characteristics and bioequivalence of bicalutamide tablets in healthy volunteers. Methods A single oral dose of 50 mg bicalutamide test(domestic) or control(import) tablets was given to 20 healthy volunteers in an open randomized cross-over study. The concentrations of bicalutamide were determined with HPLC. The pharmacokinetic parameters were calculated with 3P97 and the bioequivalent test was performed with SAS. Results The main pharmacokinetic parameters of the test and control drug were as follows: C_max, 691.50 vs 697.30 μg/L; T_max, 20.65 vs 24.10 h; AUC_0～∞, 148 124 vs 153 782 μg·h/L; t_1/2, 127.46 vs 131.06 h,respectively. The relative bioavailability was 99.43%. Conclusion The test bicalutamide tablet is bioequivalent to the control formulation.