中国临床药理学杂志2024，Vol.40Issue(13)：1948-1952,5.DOI:10.13699/j.cnki.1001-6821.2024.13.021
Etripamil鼻喷雾剂在中国健康成年受试者中单次给药的药代动力学研究
Pharmacokinetics of single-dose of Etripamil nasal spray in healthy adult Chinese subjects
摘要
Abstract
Objective To evaluate the pharmacokinetics characteristics of single-dose of Etripamil nasal spray 70 mg in healthy adult Chinese subjects.Methods This was a single-center,randomized,double-blind,placebo-controlled study.Twelve healthy adult Chinese subjects were randomized to receive single-dose of Etripamil nasal spray 70 mg(n=10)or placebo nasal spray(n=2).Blood and urine samples were collected prior and post dose.Etripamil in plasma and urine were analyzed by liquid chromatography-tandem mass spectrometry.The pharmacokinetic parameters were calculated by WinNonlin non-compartmental model.Results Following the single-dose of Etripamil nasal spray 70 mg in healthy adult Chinese subjects,the peak concentration of Etripamil in plasma was quickly attained,with a Cmax of(66.76±56.61)ng·mL-1 and a median(range)tmax of 4.00(3.00-5.00)min.The plasma concentrations of Etripamil had fallen approximately 65％from peak value at 25 min after dosing,and close to 80％within 50 min.The AUC0-last and AUC0-∞ were(3 104.16±2 654.46)and(4 048.77±2 682.38)ng·min·mL-1,respectively.The urine excretion percentage of Etripamil during 24 h was(0.01±0.01)％.Among the 12 subjects who were treated with Etripamil or placebo,10 subjects reported a total of 29 treatment-emergent adverse events(TEAEs).All of the TEAEs were mild in severity.The most common TEAEs were rhinorrhoea and lacrimation increased.Conclusion Etripamil was quickly absorbed after intranasal administration,followed by rapid distribution and elimination(not primarily excreted by renal);Etripamil 70 mg was safe and well tolerated by the healthy Chinese adult subjects.关键词
Etripamil/鼻喷雾剂/药代动力学/健康受试者Key words
Etripamil/nasal spray/pharmacokinetics/healthy volunteer分类
医药卫生引用本文复制引用
刘薇,李媛,张菁,曹国英,余姝彦,奚悦文,罗璟卉,刘波,何钰,房同勇,陈晓文..Etripamil鼻喷雾剂在中国健康成年受试者中单次给药的药代动力学研究[J].中国临床药理学杂志,2024,40(13):1948-1952,5.基金项目
复旦复星护理科研基金资助项目(FNF202163) （FNF202163）
