Tjandrawinata Raymond R, Setiawati Arini, Nofiarny Dwi, Susanto Liana W, Setiawati Effi
Dexa Laboratories of Biomolecular Sciences Unit, Dexa Medica Group, Cikarang, West Java, Indonesia.
Department of Pharmacology and Therapeutics, Medical Faculty, University of Indonesia, Jakarta, Indonesia.
Clin Pharmacol. 2018 Apr 6;10:43-51. doi: 10.2147/CPAA.S161024. eCollection 2018.
The current study aimed to evaluate whether a generic product of etoricoxib 120 mg film-coated tablet (the test drug) was bioequivalent to the reference product (Arcoxia® film-coated tablet 120 mg).
This was a randomized, open-label, two-sequence, crossover study under fasting condition, with a 14-day washout period, involving 26 healthy adult male and female subjects. Blood samples were taken and analyzed for plasma concentrations of etoricoxib (Chemical Abstracts Service [CAS] 202409-33-4) using a high-pressure liquid chromatography-ultraviolet detector (HPLC-UV) system capable of measuring etoricoxib concentrations ranging from 5.00 to 5002.90 ng/mL, with the lowest limit of quantitation of 5.00 ng/mL. A noncompartmental method was used to determine the pharmacokinetic parameters of a single-dose administration of the drug, including the area under plasma concentration-time curve from time zero to the time of last observed concentration (AUC ), the area under plasma concentration-time curve from time zero to infinity (AUC), the maximum plasma concentration (), the time to reach the maximum plasma concentration (), and the terminal half-life ().
After a single-dose administration of etoricoxib 120 mg film-coated tablet, the mean (SD) values for the AUC and of the test drug were 45913.42 (13142.19) ng·h/mL and 3155.93 (752.81) ng/mL, respectively; the values for the reference drug were 44577.20 (13541.85) ng·h/mL and 2915.13 (772.81) ng/mL, respectively. The geometric mean ratios (90% CIs) of the test drug/reference drug were 103.40% (98.70%-108.32%) for AUC and 109.26% (100.18%-119.18%) for . No clinically significant differences in and values were found between the test drug and the reference drug. No adverse events were experienced by the subjects during this study.
The present study demonstrated that the evaluated generic etoricoxib 120 mg film-coated tablets were bioequivalent to the reference drug.
本研究旨在评估依托考昔120 mg薄膜包衣片（受试药物）的仿制产品与参比产品（安康信薄膜包衣片120 mg）是否生物等效。
这是一项在禁食条件下进行的随机、开放标签、双序列、交叉研究，洗脱期为14天，纳入26名健康成年男性和女性受试者。采集血样，使用能够测量依托考昔浓度范围为5.00至5002.90 ng/mL、最低定量限为5.00 ng/mL的高压液相色谱 - 紫外检测器（HPLC - UV）系统分析血浆中依托考昔（化学文摘社[CAS]编号202409 - 33 - 4）的浓度。采用非房室模型方法确定单剂量给药后药物的药代动力学参数，包括从零时间到最后观察浓度时间的血浆浓度 - 时间曲线下面积（AUC）、从零时间到无穷大的血浆浓度 - 时间曲线下面积（AUC）、最大血浆浓度（）、达到最大血浆浓度的时间（）和末端半衰期（）。
单次口服依托考昔120 mg薄膜包衣片后，受试药物的AUC和的均值（标准差）分别为45913.42（13142.19）ng·h/mL和3155.93（752.81）ng/mL；参比药物的值分别为44577.20（13541.85）ng·h/mL和2915.13（772.81）ng/mL。受试药物/参比药物的几何平均比值（90%置信区间）AUC为103.40%（98.70% - 108.32%），为109.26%（100.18% - 119.18%）。受试药物与参比药物在和值方面未发现临床显著差异。本研究期间受试者未发生不良事件。
本研究表明，所评估的依托考昔120 mg薄膜包衣片仿制产品与参比药物生物等效。
