注射用盐酸尼非卡兰的健康人体药动学研究

张恒;王本杰;郭瑞臣

中国药学杂志 ›› 2009, Vol. 44 ›› Issue (02) : 136-140.

中国药学杂志 ›› 2009, Vol. 44 ›› Issue (02) : 136-140.
论著

注射用盐酸尼非卡兰的健康人体药动学研究

  • 张恒;王本杰;郭瑞臣
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Pharmacokinetics of Nifekalant Hydrochloride in Chinese Healthy Volunteers

  • ZHANG Heng1, WANG Ben-jie2, GUO Rui-chen2
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摘要

目的研究注射用盐酸尼非卡兰在健康人体的药动学。方法24名健康志愿者,男女各半,按体重配对,随机分为3组,以奥硝唑为内标,采用HPLC-UV测定尼非卡兰0.3,0.4mg·kg-1单次静脉推注和0.4mg·kg-1静脉推注后0.4mg·kg-1·h-1连续静脉输注6h给药尼非卡兰经时血浓度,采用DAS2.0程序计算其主要药动学参数。结果志愿者注射用盐酸尼非卡兰0.3,0.4mg·kg-1静脉推注,0.4mg·kg-1负荷剂量后0.4mg·kg-1·h-1连续6h静脉输注,尼非卡兰ρmax分别为(230.95±54.02),(358.62±73.98)和(444.30±88.12)μg·L-1;t1/2分别为(1.55±0.38)、(1.344±0.19)和(1.35±0.23)h;AUC0-t分别为(193.53±45.19),(285.61±46.57)和(2609.02±498.20)μg·h·L-1。结论血浆内源性物质不干扰尼非卡兰测定,方法简单,操作方便;尼非卡兰静脉注射给药人体内呈线性药动学特征;整个试验过程顺利,静脉推注和静脉输注给药志愿者无不良反应发生。

Abstract

OBJECTIVE To study the pharmacokinetics of nifekalant in Chinese healthy volunteers. METHODS Twenty-four qualified healthy volunteers (half male and half female) were randomly divided into three groups. The patients in first two groups received single intravenous dose of 0.3 and 0.4 mg·kg-1 within 5 min,and then 4 mL blood was smpled before and at 5, 10,15,30,45 min,1,2,3,4,5,6,7,8 h after the administration began. The patients in third group were given a single intravenous loading dose of 0.4 mg·kg-1, then, intravenous infusion of 0.4 mg·kg-1·h-1 for 6 h. 4 mL blood was smpled before and after the administration began. Nifekalant concentrations in plasma were detected by HPLC-UV method with ornidazole as internal standard. The main pharmacokinetic parameters were calculated by DAS 2.0. RESULTS The main pharmacokinetic parameters of nifekalant after single intravenous dose of 0.3 and 0.4 mg·kg-1 within 5 min and intravenous infusion of 0.4 mg·kg-1·h-1 for 6 h with single intravenous loading dose of 0.4 mg·kg-1 were as follows ρmax were (230.95±54.02), (358.62±73.98) and (444.30±88.12) μg·L-1; t1/2 were (1.55±0.38), (1.34 ±0.19) and (1.35± 0.23)h; AUC0-t were (193.53±45.19), (285.61±46.57) and (2 609.02±498.20) μg·h·L-1; respectively. CONCLUSION Nifekalant was not interfered by the endogenous compounds. The method is simple and convenient, and suitable for nifekalant determination and its pharmacokinetic studies. The ρmax and AUC were linear within giving doses. No serious side effects occurred during studies.

关键词

注射用尼非卡兰 / 药动学 / 液相色谱-紫外

Key words

nifekalant hydrochloride injection powder / pharmacokinetics / HPLC-UV

引用本文

导出引用
张恒;王本杰;郭瑞臣. 注射用盐酸尼非卡兰的健康人体药动学研究[J]. 中国药学杂志, 2009, 44(02): 136-140
ZHNG Heng;WNG en-jie;GUO Rui-chen. Pharmacokinetics of Nifekalant Hydrochloride in Chinese Healthy Volunteers [J]. Chinese Pharmaceutical Journal, 2009, 44(02): 136-140

参考文献

[1] KAMIYA J, ISHII M, KATAKAMI T, et al. Antiarrhythmic effects of MS-551, a new class Ⅲ antiarrhythmic agent, on canine models of ventricular arrhythmia[J]. Japan J Pharmacol, 1992,58(2):107-115. [2] ZHANG D P, HUANG C L. Determination of nifikalant hydrochloride by HPLC[J]. Nothwest Pharm J(西北药学杂志),2004(3):99-101.

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