Rutten A J, Mather L E, Plummer J L, Henning E C
Department of Anaesthesia and Intensive Care, Flinders University of South Australia, Bedford Park.
J Pharm Pharmacol. 1992 Apr;44(4):355-8. doi: 10.1111/j.2042-7158.1992.tb03620.x.
The plasma protein binding of the 2,6-xylidide local anaesthetic agents lignocaine, ropivacaine and bupivacaine enantiomers was determined by equilibrium dialysis in plasma obtained from chronically catheterized sheep before and up to 21 days after surgery. Three concentrations (1, 5 and 10 mg L-1), were used for each agent. Concentration-dependent binding was evident for each agent throughout the study period. R(+)-Bupivacaine was more extensively bound than S(-)-bupivacaine at the higher concentrations. Compared with pre-surgery, binding of each agent was less on the first postoperative day but did not differ significantly from days 8 to 21.
采用平衡透析法,测定了利多卡因、罗哌卡因和布比卡因对映体这三种2,6-二甲基苯胺类局部麻醉药在慢性插管绵羊术前及术后长达21天采集的血浆中的蛋白结合率。每种药物均采用三种浓度(1、5和10 mg L-1)。在整个研究期间,每种药物的结合均呈现浓度依赖性。在较高浓度下,R(+)-布比卡因的结合比S(-)-布比卡因更广泛。与术前相比,每种药物在术后第一天的结合较少,但在第8至21天与术前无显著差异。