Luo Hong-Yu, Xu Shuo-Guo, Gao Li-Chen, Long Hui-Zhi, Zhou Zi-Wei, Li Feng-Jiao, Dai Shang-Ming, Hu Jin-Da, Su Yu, Cheng Yan
Department of Pharmacy, School of Pharmacy, Phase I Clinical Trial Centre, The Affiliated Changsha Central Hospital, Hengyang Medical School, University of South China, Changsha, China.
Affiliated Changsha Hospital of Hunan Normal University (The Fourth Hospital of Changsha), Changsha, China.
Drugs R D. 2024 Mar;24(1):81-87. doi: 10.1007/s40268-024-00455-9. Epub 2024 Feb 12.
Potassium bismuth citrate is a gastric mucosal protector and a key drug for treating peptic ulcers.
To evaluate the pharmacokinetic characteristics and safety of 120-mg bismuth potassium citrate formulations administered orally under fasting conditions in healthy Chinese subjects.
A single-center open two-cycle trial was conducted on 12 healthy subjects who received a single oral dose of 120 mg of bismuth potassium citrate. The plasma concentration of bismuth was determined using a validated inductively coupled plasma mass spectrometry (ICP‒MS) method. The pharmacokinetic parameters, including maximum serum concentration (C) and area under the curve concentration-time curve (AUC and AUC), and safety were evaluated via noncompartment analysis.
The ratios of the least square geometric mean ratio between the test (T) and reference (R) formulations for C, AUC, and AUC were 44.8%, 55.5%, and 64.4%, respectively; the bilateral 95% confidence intervals (Cis) for these parameters were 20.2-99.6%, 24.1-127.5%, and 23.7-175.0%, respectively, and the non-inferior limits for these parameters were 169.4%, 198.8%, and 200.5%, respectively. The upper limits of the one-sided 97.5% confidence interval for the least squares geometric mean ratio (T/R) were lower than the non-inferior limits. No serious adverse reactions or adverse reactions leading to detachment were observed among the subjects.
The concentration of bismuth in the blood of healthy subjects in the T formulation was not greater than that in the R formulation. Similarly, the safety of oral administration of 120 mg of bismuth potassium citrate formulations to healthy subjects was good. The trial registration number (TRN) was [2018] 013, 6 December 2018.
枸橼酸铋钾是一种胃黏膜保护剂，是治疗消化性溃疡的关键药物。
评估120毫克枸橼酸铋钾制剂在健康中国受试者空腹条件下口服的药代动力学特征和安全性。
对12名健康受试者进行单中心开放两周期试验，受试者单次口服120毫克枸橼酸铋钾。采用经过验证的电感耦合等离子体质谱法（ICP-MS）测定铋的血浆浓度。通过非房室分析评估药代动力学参数，包括最大血清浓度（C）、曲线下面积浓度-时间曲线（AUC和AUC）以及安全性。
试验（T）制剂与参比（R）制剂的C、AUC和AUC的最小二乘几何平均比值分别为44.8%、55.5%和64.4%；这些参数的双侧95%置信区间（Cis）分别为20.2-99.6%、24.1-127.5%和23.7-175.0%，这些参数的非劣效限度分别为169.4%、198.8%和200.5%。最小二乘几何平均比值（T/R）的单侧97.5%置信区间上限低于非劣效限度。受试者中未观察到严重不良反应或导致停药的不良反应。
T制剂中健康受试者血液中的铋浓度不高于R制剂。同样，健康受试者口服120毫克枸橼酸铋钾制剂的安全性良好。试验注册号（TRN）为[2018]013，2018年12月6日。
