中国临床药理学与治疗学2012，Vol.17Issue(8)：896-900,5.
冻干重组胰高血糖素样肽-1受体激动剂在中国健康成年受试者中皮下给药药代动力学研究
Pharmacokinetics of rE-4 (Lyophilized Recombinant Exendin-4) in healthy volunteers after multiple subcutaneous injections
杨巍 1冯婉玉 2纪立农 2邵宏 3方翼 1朱丽霞 2张春燕 4闫记灵 2王茜 4刘一 2程远国 2张明霞 5徐佳3
作者信息
- 1. 北京大学医学部药学院,北京100191
- 2. 北京大学人民医院药剂科,北京100044
- 3. 北京大学人民医院内分泌科,北京100044
- 4. 石药集团中奇制药技术(石家庄)有限公司临床医学部,石家庄050035,河北
- 5. 军事医学院科学院药代动力学重点实验室,北京100071
- 折叠
摘要
Abstract
AIM: To study the pharmacokinetics of rE-4 ( Lyophilized Recombinant Exendin-4) injection after single and multiple s. c administration in Chinese healthy volunteers METHODS; rE-4 injection was administrated s. c. to 6 male and 6 female Chinese adult healthy volunteers at the single dose of 5 μg once a day for 8 days, RESULTS: After the administration of the 1st and the 8th day, the pharmaco-kinetic parameters AUC0-t was 690.2, 718.0 ng·h·L-1; AUC0-∞ was 779.8, 797.9 ng · h · L-1 ; tmax was 0. 89, 0. 79 h, Cmax was 201,4, 212. 7 ng/L; t1/2z was 2.38, 2. 31 h; CLz/F was 6.7, 6.5 L/h, respectively. The AUC0-t,Cmax and t1/2z of the single and multiple administration were not statistically different and the accumulation index was 1. 0017. There were no serious adverse events observed but only one case of mild adverse reaction. CONCLUSION: The rE-4 was well tolerated in Chinese healthy volunteers. The concentration-time profiles of rE-4 were shown to fit the one-compartment model. No systemic accumulation appeared after the multiple-dose administration. Further phase Ⅱclinical trials towards rE-4 could be recommended,关键词
rE-4/药代动力学/安全性/中国健康受试者/皮下给药Key words
rE-4/ Pharmacokinetics/ Safety/ Chinese healthy volunteers/ Subcutaneous administration分类
医药卫生引用本文复制引用
杨巍,冯婉玉,纪立农,邵宏,方翼,朱丽霞,张春燕,闫记灵,王茜,刘一,程远国,张明霞,徐佳..冻干重组胰高血糖素样肽-1受体激动剂在中国健康成年受试者中皮下给药药代动力学研究[J].中国临床药理学与治疗学,2012,17(8):896-900,5.
