›› 2011, Vol. 31 ›› Issue (5): 584-.doi: 10.3969/j.issn.1674-8115.2011.05.013

• 论著(基础研究) • 上一篇    下一篇

甲磺酸罗哌卡因和盐酸罗哌卡因硬膜外阻滞的药代动力学特征比较

蔡美华1,2, 张马忠2, 荣征星1, 江 涛1, 王玉梅3, 崔永耀1   

  1. 1.上海交通大学 基础医学院药理学教研室, 上海 200025; 2.上海交通大学 医学院附属上海儿童医学中心儿科转化医学研究所, 上海 200127; 3.江苏恩华药业股份有限公司 临床医学部, 江苏 221007
  • 出版日期:2011-05-28 发布日期:2011-05-27
  • 通讯作者: 崔永耀, 电子信箱: yongyaocui@yahoo.com.cn。
  • 作者简介:蔡美华(1978—), 女, 主管药师, 学士;电子信箱: helen-cai@hotmail.com。

Comparision of pharmacokinetics between ropivacaine methanesulfonate and ropivacaine hydrochloride during epidural block

CAI Mei-hua1,2, ZHANG Ma-zhong2, RONG Zheng-xing1, JIANG Tao1, WANG Yu-mei3, CUI Yong-yao1   

  1. 1.Department of Pharmacology, Basic Medical College, Shanghai Jiaotong University, Shanghai 200025, China;2.Institute for Pediatric Translational Medicine, Shanghai Children's Medical Center, Shanghai Jiaotong University School of Medicine, Shanghai 200127, China;3.Department of Clinical Medicine, Jiangsu Nhwa Pharmaceutical Coporation Limited, Jiangsu 221007, China
  • Online:2011-05-28 Published:2011-05-27

摘要:

目的 比较0.894%甲磺酸罗哌卡因和0.75%盐酸罗哌卡因的药代动力学特征。方法 40例择期下腹部、下肢手术病例,随机分为甲磺酸罗哌卡因组(n=20)和盐酸罗哌卡因组(n=20)。于给药前和给药后2、5、10、20、30、45、60、90、120、180、240、300、360、720、1440 min抽取肘前静脉血,采用反相高效液相色谱紫外法,测定血浆中甲磺酸或盐酸罗哌卡因浓度。采用DAS 2.0软件计算药代动力学参数,并比较两组药代动力学参数的特征。结果 甲磺酸罗哌卡因和盐酸罗哌卡因组的表观分布容积(Vd/F)分别为(2.1±0.7)和(2.7±1.1)L/kg,消除半衰期(T1/2β)分别为(333±89)和(378±112)min,药时曲线下总面积(AUC0-∞)分别为(480±168)和(425±126)mg·min/L,清除率(CL/F)分别为(4.6±1.3)和(5.1±1.3)mL/(min·kg),达峰时间(Tpeak)分别为(26±13)和 (29±20)min,峰浓度(Cmax)分别为(1732±833)和(1 345±341)ng/mL,两组药代动力学参数比较差异无统计学意义(P>0.05)。结论 0.894%甲磺酸罗哌卡因和0.75%盐酸罗哌卡因药代动力学特征近似,符合二室模型;盐基的改变对罗哌卡因的代谢无影响。

关键词: 甲磺酸罗哌卡因, 盐酸罗哌卡因, 色谱紫外法, 反相高效液相, 药代动力学

Abstract:

Objective To compare the pharmacokinetics between 0.894% ropivacaine methanesulfonate and 0.75% ropivacaine hydrochloride. Methods Forty patients undergoing lower abdominal or lower limb surgery were randomly divided into ropivacaine methanesulfonate group (n=20) and  ropivacaine hydrochloride group (n=20). Blood samples were collected from an antecubital vein before administration and 2, 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300, 360, 720 and 1 440 min after administration, and the concentrations of ropivacaine methanesulfonate or ropivacaine hydrochloride were determined by reversed phase high performance liquid chromatography-ultraviolet method. The pharmacokinetic parameters were calculated by DAS 2.0 software and were compared between groups. Results The apparent volumes of distribution (Vd/F) of ropivacaine methanesulfonate and ropivacaine hydrochloride were (2.1±0.7) L/kg and (2.7±1.1) L/kg, respectively; the elimination half life time (T1/2β) were (333±89) min and (378±112) min, respectively; the total areas under the concentration-time curve (AUC0-∞) were (480±168) mg·min/L and (425±126) mg·min/L, respectively; the clearance rates (CL/F) were (4.6±1.3) mL/(min kg) and (5.1±1.3) mL/(min kg), respectively; the peak time (Tpeak) were (26±13) min and (29±20) min, respectively; and the maximum concentrations (Cmax) were (1 732±833) ng/mL and (1 345±341) ng/mL, respectively. There was no significant difference in pharmacokinetic parameters between groups (P>0.05). Conclusion The pharmacokinetics of 0.894% ropivacaine methanesulfonate are similar to those of 0.75% ropivacaine hydrochloride, and the pharmacokinetic data are consistent with two-compartment model. In addition, the metabolism of ropivacaine is not influenced by the change of base.

Key words: ropivacaine methanesulfonate, ropivacaine hydrochloride, ultraviolet, reversed phase high performance liquid chromatography, pharmacokinetics