CAJ | 학술논문

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272 nm.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50 mg,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10～1200 ng·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.
목적 본문건립HPLC법측정비잡로알혈농도,연구비잡로알효낭(시험제제)여비잡로알편(삼비제제)재건강인체적약동학특정,평개2제제생물등효성.채용XB-C18색보주,류동상을정-수(60∶40,Ⅴ/Ⅴ),검측파장272 nm.48명건강지원자,수궤분위2조,채용단주기평행시험설계,단제구복비잡로알시험제제혹삼비제제50 mg,채용고효액상색보법측정비잡로알혈농도,DAS2.0연건계산비잡로알주요약대동역학삼수.시험결과표명비잡로알선성범위10～1200 ng·mL-1.비잡로알시험제제화삼비제제주요약동학삼수분별위:t1/2(138.36±32.03)화(146.12±27.04)h,Tmax(17.17±4.65)화(16.92±4.85)h,Cmax(910.83±130.49)화(868.71±115.35)ng·mL-1,AUC0～672(172437.08±3986.07)화(176842.34±35733.85)ng·mL-1·h,AUC0～∞(179456.55±43127.65)화(185270.39±39688.63)ng·mL-1·h.Cmax,AUC0～672화AUC0～∞가신구간분별위(98.9%～100.7%),(98.8%～100.6%)화(99.7%～101.7%).비잡로알효낭상대생물이용도F위97.51%.비잡로알시험제제화삼비제제구유생물등효성.
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 eters 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±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.