甲磺酸罗哌卡因注射液病人体内药代动力学研究

Research on pharmacokinetics of ropivacaine methanesulfonate in patients

目的:研究甲磺酸罗哌卡因注射液病人体内的药代动力学过程及药动学参数的性别差异。方法:单剂量硬膜外给药15 mL,采用HPLC测定血浆中罗哌卡因的浓度。用DAS软件计算其药代动力学参数。结果:单剂量使用甲磺酸罗哌卡因注射液后男性和女性的消除半衰期t1/2β分别为(4.050±2.548)、(2.088±0.135)h;吸收半衰期t1/2ka分别为(0.085±0.045)、(0.107±0.069)h;达峰时间分别为(0.333±0.118)、(0.417±0.167)h;峰浓度分别为(1.066±0.135)、(1.113±0.317)mg/L;吸收程度(AUC0-tn,统计矩法)分别为(2.856±0.321)、(2.369±0.386)mg.L-1.h;MRT0-tn分别为(2.070±0.113)、(2.022±0.089)h。结论:本试验建立了甲磺酸罗哌卡因注射液血药浓度的固相萃取-HPLC测定方法,提供了单剂量使用的药动学参数,试验结果表明各药动学参数性别间差异无统计学意义。

AIM： To study the phannacokinetic profiles of ropivacaine methanesulfonate in patients and research the sex differences between these parameters. METHODS： 15 mL ropivacaine methanesulfonate injection was given when the patient had an epidural anesthesia. The concentrations of ropivacaine in plasma were determined by HPLC. The parameters of pharma- cokinetics were calculated by DAS software. RESULTS： The pharmacokinetic parameters of male and female after administration with ropivacaine methane-sulfonate injection were as follows： the t1/2β were （4.050±2.548） and （2.088 ± 0. 135） h; the t1/2Ka were （0.085±0.045） and （0.107±0.069） h; the tmax were （0.333 ± 0. 118） and （0.417±0. 167） h; the Cmax, were （1.066±0.135） and （1.113±0.317） mg/L; the AUC0-tn were （2.856 ± 0.321） and （2.369 ±0.386） mg.L^-1.h; the MRT0-tn were （2.070± 0.113） and （2.022±0.089） h, respectively. CONCLUSION： The methodology to determine plasma con- centration by HPLC and pharmacokinetic profiles of ropivacaine methanesulfonate injection were achieved. The results showed that there were no sex differences statistically between the pharmacokinetic parameters.