达沙替尼片在中国健康人体内的药代动力学.pdf

文档介绍：达沙替尼片在中国健康人体内的药代动力学
苏浩明1,宋敏 1,陆平波 2,马晓娟 2,张维威 2,杨林 3,文爱东 3,杭太俊 1
(,江苏南京 210009;
院,江苏南京 210042;,西安,710032)

[摘要] 目的:建立人血浆中达沙替尼浓度的液-质联用(LC-MS/MS)测定法,研究达沙替
尼片在中国健康人体内的药代动力学。方法:24 名男性健康受试者单剂量空腹口服 100 mg
达沙替尼片(江苏正大天晴药业股份有限公司研制), 0 ~ 48 h 间隔采集肘静脉血,分离血浆
测定达沙替尼血药浓度, 软件计算药动学参数。结果:达沙替尼的主要药动学参数:
-1
Cmax 为( ± ) ng•mL ,Tmax 为( ± ) h,t1/2 为( ± ) h,AUC0~48
-1 -1 -1
为(668 ± 207) ng•h•mL ,AUC0~¥为(684 ± 208) ng•h•mL ,CL 为( ± ) L•h ,
V 为(1341 ± 1022) L。结论:建立的 LC-MS/MS 测定法专属、灵敏,满足达沙替尼片药
动学研究的要求。测得达沙替尼片在健康中国人体内的吸收明显高于美国人。
[关键词] 达沙替尼;药动学;液相色谱-串联质谱法
[中图分类号] [文献标识码] A [文章编号]

ics of dasatinib tablets in Chinese healthy volunteers
SU Hao-ming1, SONG Ming1, HANG Tai-jun1, LU Ping-bo2, MA Xiao-juan2, Zhang Wei-wei2,
YANG Lin3, WEN Ai-dong3
( of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009,
China; 2. Jiangsu Chia-tai Tianqing Pharmaceutical Co. Ltd.; R&D Center; Nanjing 210042,
China; 3. Xijing Hospital Affiliated to the Fourth Military Medical University; Xi’an 710032,
China )

[Abstract] Objective: To establish a LC-MS/MS method for the determination of plasma
concentration of dasatinib and to study the ics of dasatinib tablets in healthy male
Chinese volunteers. Methods: Twenty four volunteers were given a single oral dose