PDF(Pubmed)
Abstract：
Candesartan is an antihypertensive agent that acts on an angiotensin II receptor. Candesartan cilexetil is a prodrug that is converted into the active form of candesartan during intestinal absorption. This study aimed to assess the pharmacokinetics and bioequivalence of a reference and a test formulation of candesartan cilexetil tablets in healthy Chinese volunteers. A randomized, open-label, single-dose, crossover study was conducted with two treatment periods. Forty-eight healthy Chinese volunteers participated under fasted conditions. Qualified subjects were randomly divided into two groups (1:1 ratio) to receive either the test or reference formulation first. A washout period of 14 days separated the administration of the two formulations. Blood samples were collected at specific time points and analyzed for candesartan concentration using Ultra High-Performance Liquid Chromatography Tandem Mass Spectrometry (UPLC-MS/MS). The maximum concentration (Cmax), the AUC from time zero to the last measured time point (AUC0-t) and the AUC from time zero to infinity (AUC0-∞) fell within the bioequivalence range of 80% to 125%. These results suggest that the test and reference formulations of candesartan cilexetil tablets are bioequivalent, meaning they have similar rates and extents of absorption in healthy Chinese volunteers. No serious adverse events or side effects were reported throughout the study.
摘要：
坎地沙坦是一种抗高血压药，作用于血管紧张素II受体。坎地沙坦西酯是在肠吸收期间转化为坎地沙坦的活性形式的前药。本研究旨在评估坎地沙坦酯片参比和试验制剂在健康中国志愿者中的药代动力学和生物等效性。一个随机的，开放标签，单剂量,交叉研究进行了两个治疗期。48名健康中国志愿者在禁食条件下参加。将合格的受试者随机分成两组(1:1比例)以首先接受测试或参考制剂。14天的洗脱期分开两种制剂的施用。在特定时间点收集血液样品,并使用超高效液相色谱串联质谱法(UPLC-MS/MS)分析坎地沙坦浓度。最大浓度（Cmax），从时间零到最后测量时间点的AUC（AUC0-t）和从时间零到无穷大的AUC（AUC0-∞）落在80％至125％的生物等效性范围内。这些结果表明，坎地沙坦西酯片的试验配方和参考配方是生物等效的，这意味着它们在健康的中国志愿者中具有相似的吸收率和吸收程度。在整个研究中没有报告严重的不良事件或副作用。
