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目的 研究国人在硬膜外阻滞时罗哌卡因和布比卡因的药代动力学特征。方法 选择１４ 例手术病人、随机分为两组。硬膜外阻滞时，分别注入罗哌卡因２．０ｍ ｇ／ｋｇ 或布比卡因２．０ｍ ｇ／ｋｇ。用气相色谱法测定血浆药物浓度。结果 罗哌卡因和布比卡因的药－时曲线均符合二室开放模型。ｔ１／２ｋａ分别为０．２２ 小时和０．１４ 小时，Ｔｐｅａｋ 分别为０．５１ 小时和０．４７ 小时，Ｃａｍ ｘ 分别为１．０６ｍ ｇ·Ｌ－ １和１．４４ｍ ｇ·Ｌ－ １ 。另外发现，其主要药代动力学参数，ＡＵＣ分别为２．６ｍ ｇ·Ｌ－ １·ｈ－ １ 和５．２ｍ ｇ·Ｌ－ １·ｈ－ １ ，ｔ１／２ β分别为１．７ 小时和２．８ 小时，ＣＬ分别为７５７ｍ ｌ·ｍ ｉｎ－ １ 和３８２ｍ ｌ·ｍ ｉｎ－ １，两组间均具有显著差异（Ｐ＜ ０．０５）。结论 罗哌卡因比布比卡因较少发生中枢神经系统及心血管的蓄积，主要是由于罗哌卡因在体内消除代谢能力较强所致。
Objective To study the pharmacokinetics of ropivacaine and bupivacaine in Chinese during epidural block. Methods 14 cases of surgical patients were randomly divided into two groups. Epidural block was infused with ropivacaine 2.0 m g / kg or bupivacaine 2.0 m g / kg, respectively. Determination of Plasma Drug Concentration by Gas Chromatography. Results The drug-time curves of ropivacaine and bupivacaine all fit the two-compartment open model. t1 / 2ka were 0.22 hours and 0.14 hours respectively, Tpeak was 0.51 hours and 0.47 hours respectively, Camx was 1.06 m g · L-1 and 1.44 g · L-1, respectively. In addition, the main pharmacokinetic parameters were found to be 2.6 m g · L-1 · h-1 and 5.2 m g · L-1 · h-1 for AUC and t1 / 2 β were 1.7 h And 2.8 hours, with CL of 757 m l · m-1 and 382 m l · m-1, respectively, with significant differences between the two groups (P <0.05). Conclusions Ropivacaine produces less central nervous system and cardiovascular accumulation than bupivacaine, mainly due to its ability to eliminate metabolism in vivo.