文章摘要
李彩云,居希同,王菁,等.不同规格苹果酸法米替尼胶囊在中国健康受试者中的生物等效性研究[J].中国临床保健杂志,2025,28(4):539-544.
不同规格苹果酸法米替尼胶囊在中国健康受试者中的生物等效性研究
Bioequivalence study of famitinib malate capsules in Chinese healthy subjects with different specifications
投稿时间：2025-02-26  
DOI：10.3969/J.issn.1672-6790.2025.04.020
中文关键词: 苹果酸法米替尼胶囊  剂量效应关系,药物  药代动力学  等效性试验
英文关键词: Famitinib malate capsules  Dose-response relationship,drug  Pharmacokinetics  Equivalence trial
基金项目:
作者单位E-mail
李彩云 安徽医科大学临床药理研究所抗炎免疫药物教育部重点实验室,合肥 230031 lcy06092000@126.com 
居希同 安徽医科大学临床药理研究所抗炎免疫药物教育部重点实验室,合肥 230031
江苏恒瑞医药股份有限公司,江苏连云港 222000 		 
王菁 江苏恒瑞医药股份有限公司,江苏连云港 222000  
李少荣 江苏恒瑞医药股份有限公司,江苏连云港 222000  
沈爱宗 .中国科学技术大学附属第一医院安徽省立医院Ⅰ期临床试验研究室,合肥 230001  
杨昭毅 安徽医科大学临床药理研究所抗炎免疫药物教育部重点实验室,合肥 230031
.中国科学技术大学附属第一医院安徽省立医院Ⅰ期临床试验研究室,合肥 230001 		young2382@163.com 
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中文摘要:
      目的 评估健康受试者在空腹条件下口服同剂量不同规格的苹果酸法米替尼胶囊的生物等效性。方法 本研究为单中心、单剂量、随机、开放、两周期、交叉的生物等效性研究,研究时间为2022年5月至6月。共入组28例健康受试者(男女各半),受试者被随机分配至2个序列组,第1周期分别在空腹条件下单剂量口服苹果酸法米替尼胶囊受试规格(5 mg/粒,共4粒)或参比规格(20 mg/粒,共1粒),第2周期在相同条件下口服另一规格药物。用液相色谱-串联质谱(LC-MS/MS)对血浆中苹果酸法米替尼及其代谢物SHR116637的药物浓度进行检测分析。采用Phoenix WinNonlin 8.3和SAS 9.4软件计算各受试者的药代动力学参数以及评价生物等效性。结果 单次空腹口服受试规格和参比规格的苹果酸法米替尼胶囊后,血浆法米替尼的tmax为6.00(4.98,8.00)h和6.00(4.98,8.02)h,t1/2分别为(35.70±6.81)h和(36.00±6.79)h,Cmax分别是(31.20±1.29)μg/L和(29.80±1.29)μg/L,AUC0~t分别是(1 039.00±1.38)h·ng·mL-1和(1 003.00±1.32)h·ng·mL-1。血浆代谢物SHR116637的tmax分别为5.05(3.00,8.00)h和6.00(4.98,12.00)h,t1/2分别为(55.20±10.50)h和(53.60±8.31)h,Cmax分别是1.42(1.09,1.67) μg/L和1.35(1.07,1.48)μg/L,AUC0~t分别是(79.90±1.53)h·ng·mL-1和(77.20±1.46)h·ng·mL-1。对法米替尼及其代谢物SHR116637进行分析,其Cmax和AUC0~t几何均值比值的90%CI均在80.00%～125.00%。结论 苹果酸法米替尼胶囊受试规格和参比规格在空腹条件下具有生物等效性。
英文摘要:
      Objective To evaluate the bioequivalence of oral administration of different specifications but the same dose of famitinib malate capsules in healthy subjects under fasting conditions.Methods This trial was a single-center,single-dose,randomized,open-label,two-cycle,crossover bioequivalence study.The study was from May to June 2022.A total of 28 healthy subjects (half male and half female) were enrolled,and the subjects were randomly assigned to two sequence groups,the first cycle was a single-dose oral famitinib malate capsules test (5 mg/capsule,4 capsules) or reference (20 mg/capsule,1 capsule) specifications under fasting conditions,and the second cycle was oral administration of another specification of drug under the same conditions.Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was used to detect and analyze the drug concentration of famitinib malate and its metabolite SHR116637 in plasma.Phoenix WinNonlin 8.3 and SAS 9.4 software were used to calculate the pharmacokinetic parameters and evaluate the bioequivalence.Results The tmax of famitinib in plasma were 6.00 (4.98,8.00) h and 6.00 (4.98,8.02) h,t1/2 were (35.70±6.81) h and (36.00±6.79) h,Cmax were (31.20±1.29) μg/L and (29.80±1.29) μg/L,and AUC0-t were (1 039.00±1.38) h·ng·mL-1 and (1 003.00±1.32) h·ng·mL-1,respectively.The tmax of metabolite SHR116637 in plasma were 5.05 (3.00,8.00) h and 6.00 (4.98,12.00) h,t1/2 were (55.20±10.50) h and (53.60±8.31) h,the Cmax were 1.42(1.09,1.67) μg/L and 1.35(1.07,1.48) μg/L,and the AUC0-t were (79.90±1.53) h·ng·mL-1 and (77.20±1.46) h·ng·mL-1,respectively.The 90% confidence interval of the geometric mean ratio of Cmax and AUC0-t of famitinib and metabolite SHR116637 were in the range of 80.00%-125.00%.Conclusions The test specifications and reference specifications of famitinib malate capsules are bioequivalent under fasting conditions.
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