西洛他唑片在中国健康受试者中的生物等效性研究  

Bioequivalence study of cilostazol tablets in Chinese healthy subjects

作　　者：王彦荣[1] 裴莹子 陈然[1] 王莹 解明月 WANG Yan-rong;PEI Ying-zi;CHEN Ran;WANG Ying;XIE Ming-yue(Drug Clinical Trial Institution Office,Cangzhou Central Hospital,Cangzhou 061017,Heibei Province,China;Beijing Fuyuan Pharmaceutical Company Limited,Beijing 101113,China)

机构地区：[1]沧州市中心医院药物临床试验机构办公室,河北沧州061017 [2]北京福元医药股份有限公司,北京101113

出　　处：《中国临床药理学杂志》2024年第16期2383-2387,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评估2种西洛他唑片50 mg在中国健康受试者中的生物等效性及安全性。方法本研究用开放、随机、双周期、双交叉、空腹给药的设计,共纳入32例健康成年受试者,分别单次口服西洛他唑片受试制剂或参比制剂50 mg。用液相色谱-质谱(LC-MS/MS)法测定血浆中西洛他唑的浓度,用SAS 9.4处理血浆中西洛他唑的浓度-时间数据,用非房室模型法计算西洛他唑的药代动力学参数,并进行生物等效性及安全性评价。结果受试制剂和参比制剂的西洛他唑C_(max)分别为(358.10±125.80)和(346.90±115.30)ng·mL^(-1),tmax分别为3.50和4.00 h,t1/2分别为(9.63±7.12)和(8.57±5.15)h,AUC_(0-t)分别为(5235.00±2268.00)和(5190.00±1747.00)h·ng·mL^(-1),AUC_(0-∞)分别为(5377.00±2367.00)和(5308.00±1848.00)h·ng·mL^(-1)。受试制剂和参比制剂主要药代动力学参数的几何均值比值的90%置信区间均落在80.00%~125.00%。结论中国健康受试者单次口服受试和参比西洛他唑片具有生物等效性,且安全性良好。Objective To evaluate the bioequivalence and safety of two cilostazol tablets 50 mg in healthy Chinese subjects.Methods This study was an open-lable,randomized,two-period crossover design.A total of 32 subjects respectively for fasting state were given a single oral dose of test or reference tedizolid phosphate tablets 50 mg.The plasma concentration of cilostazol was determined by liquid chromatography tandem mass spectrometry(LC-MS/MS),and the concentration-time data was processed by SAS 9.4,the model method of the non-compartmental was used to calculate the pharmacokinetic parameters of tedizolid and to evaluate the bioequivalence.Results The C_(max)of cilostazol test and reference were(358.10±125.80)and(346.90±115.30)ng·mL^(-1);t_(max)were 3.50 and 4.00 h;t_(1/2)were(9.63±7.12)and(8.57±5.15)h;AUC_(0-t)were(5235.00±2268.00)and(5190.00±1747.00)h·ng·mL^(-1);AUC_(0-∞)were(5377.00±2367.00)and(5308.00±1848.00)h·ng·mL^(-1).The 90%confidence intervals of the geometric mean ratios of the main pharmacokinetic parameters of the test drug and reference drug were within the range of 80.00%to 125.00%.Conclusion Single oral test and reference cilostazol tablets were bioequivalent and safe in healthy Chinese subjects.

关 键 词：西洛他唑片 健康受试者 生物等效性 药代动力学 液相色谱-质谱法 

分 类 号：R972[医药卫生—药品]