上海交通大学学报（医学版）

›› 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

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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