比卡鲁胺胶囊/片健康人体生物等效性研究

目的本文建立HPLC法测定比卡鲁胺血浓度,研究比卡鲁胺胶囊（试验制剂）与比卡鲁胺片（参比制剂）在健康人体的药动学特征,评价2制剂生物等效性。采用XB-C18色谱柱,流动相乙腈-水（60：40,V/V）,检测波长272nm。48名健康志愿者,随机分为2组,采用单周期平行试验设计,单剂口服比卡鲁胺试验制剂或参比制剂50mg,采用高效液相色谱法测定比卡鲁胺血浓度,DAS2.0软件计算比卡鲁胺主要药代动力学参数。试验结果表明比卡鲁胺线性范围10-1200ng·mL^–1。比卡鲁胺试验制剂和参比制剂主要药动学参数分别为：t1/2（138.36±32.03）和（146.12±27.04）h,Tmax（17.17±4.65）和（16.92±4.85）h,Cmax（910.83±130.49）和（868.71±115.35）ng·mL^–1,AUC0～672（172437.08±3986.07）和（176842.34±35733.85）ng·mL^–1·h,AUC0～∞（179456.55±43127.65）和（185270.39±39688.63）ng·mL^–1·h。Cmax,AUC0～672和AUC0～∞可信区间分别为（98.9%～100.7%）,（98.8%～100.6%）和（99.7%～101.7%）。比卡鲁胺胶囊相对生物利用度F为97.51%。比卡鲁胺试验制剂和参比制剂具有生物等效性。

Bioequivalence of bicalutamide capsules and tablets in Chinese healthy volunteers

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 of 272 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 Crux, A UC0-672 and A UC0-∞ 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