Wang Bingna, Huang Chen, Xu Lang, Fu Xihua, Ma Xiaojun, You Guoxing, Su Jianfen
The Affiliated Panyu Central Hospital, Guangzhou Medical University, No. 8 Fuyu East Road, Panyu District, Guangzhou, China.
School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, China.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Jun 19. doi: 10.1007/s00210-025-04365-8.
Dexamethasone palmitate injection is used mainly in the treatment of severe rheumatoid arthritis. This study aimed to compare the bioequivalence and safety profiles of two (1 mL:4 mg) dexamethasone palmitate injections in the fasting arm in healthy Chinese volunteers. A random, open, single-dose, two-preparation, two-sequence, two-period crossover design was conducted. Twenty-four healthy volunteers participated in the study. Each participant received an intravenous injection of either the test (imitation) or reference (original) formulation of dexamethasone palmitate in the fasting arm during each study period, with a 7-day washout period between administrations. The results showed that, under the fasting condition, the pharmacokinetic parameters of the test and reference formulations were within the acceptable limits for bioequivalence. The 90% confidence intervals for the ratios of C and AUC and AUC fell within the bioequivalence range of 80-125%, achieving 100% power. No serious adverse events were observed, and no participants withdrew from the study. All safety parameters remained within normal limits throughout the study. The imitation preparation of dexamethasone palmitate injections is bioequivalent to the original formulation when administered as a single intravenous injection under fasting conditions to healthy Chinese volunteers. This finding supports the interchangeability of the imitation and original formulations, potentially offering a cost-effective alternative in clinical practice. This study was registered in the Chinese Clinical Trial Registry (registration number: ChiCTR2500098690; date of registration: March 12, 2025).
棕榈酸地塞米松注射液主要用于治疗重度类风湿关节炎。本研究旨在比较两种（1毫升：4毫克）棕榈酸地塞米松注射液在健康中国志愿者空腹状态下的生物等效性和安全性。采用随机、开放、单剂量、双制剂、双序列、双周期交叉设计。24名健康志愿者参与了该研究。在每个研究周期，每位参与者在空腹状态下接受一次静脉注射，注射的是棕榈酸地塞米松的试验（仿制品）或参比（原研）制剂，两次给药之间有7天的洗脱期。结果显示，在空腹条件下，试验制剂和参比制剂的药代动力学参数在生物等效性的可接受范围内。Cmax和AUC的比值的90%置信区间落在80 - 125%的生物等效范围内，检验效能达100%。未观察到严重不良事件，也没有参与者退出研究。在整个研究过程中，所有安全参数均保持在正常范围内。对于健康中国志愿者，在空腹条件下单次静脉注射时，棕榈酸地塞米松注射液的仿制品与原研制剂生物等效。这一发现支持了仿制品和原研制剂的互换性，可能在临床实践中提供一种具有成本效益的替代方案。本研究已在中国临床试验注册中心注册（注册号：ChiCTR2500098690；注册日期：2025年3月12日）。
