DiGregorio G J, Piraino A J, Ruch E
J Pharm Sci. 1979 Sep;68(9):1192-3. doi: 10.1002/jps.2600680940.
The concentration ratios of parotid saliva to plasma lidocaine were determined in rats after a single dose (10 mg of lidocaine/kg) and constant infusion (60 micrograms of lidocaine/kg/min). Parotid saliva and plasma samples were obtained at 10, 20, and 30 min after single-dose lidocaine administration and at 70, 80, and 90 min after the initiation of a lidocaine infusion. The saliva/plasma concentration ratios for lidocaine after single-dose administration decreased from 1.13 +/- 0.03 at 10 min to 0.51 +/- 0.06 at 30 min, whereas the ratios determined during the lidocaine infusion remained constant (0.43 +/- 0.03, 0.45 +/- 0.03, and 0.43 +/- 0.04) over the time period tested. The variable saliva/plasma concentration ratios obtained after single-dose administration may be associated with rapid drug distribution between the plasma and peripheral compartments and variation in lidocaine binding to plasma proteins. However, during constant lidocaine infusion, a steady-state concentration was achieved within 70 min, as demonstrated by the constant saliva/plasma concentration ratios.
在大鼠单次给药(利多卡因10毫克/千克)和持续输注(利多卡因60微克/千克/分钟)后,测定腮腺唾液与血浆中利多卡因的浓度比。在单次给予利多卡因后10、20和30分钟以及开始输注利多卡因后70、80和90分钟采集腮腺唾液和血浆样本。单次给药后利多卡因的唾液/血浆浓度比从10分钟时的1.13±0.03降至30分钟时的0.51±0.06,而在利多卡因输注期间测定的浓度比在测试时间段内保持恒定(0.43±0.03、0.45±0.03和0.43±0.04)。单次给药后获得的唾液/血浆浓度比变化可能与药物在血浆和外周隔室之间的快速分布以及利多卡因与血浆蛋白结合的变化有关。然而,在持续输注利多卡因期间,70分钟内达到了稳态浓度,这通过恒定的唾液/血浆浓度比得以证明。