Anesthetics;
local—lidocaine;
concentration in parotid saliva and in blood;
single dose and continuous infusion;
rats;
Lidocaine—concentration in parotid saliva and in blood;
Saliva—lidocaine concentration after single dose and continuous infusion;
compared to serum;
Serum—lidocaine concentration after single dose and continuous infusion;
compared to saliva;
D O I:
10.1002/jps.2600680940
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
The concentration ratios of parotid saliva to plasma lidocaine [antiarrhythmic agent] were determined in rats after a single dose (10 mg of lidocaine/kg) and constant infusion (60 .mu.g of lidocaine/kg per 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, but 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. During constant lidocaine infusion, a steady-state concentration was achieved within 70 min, as demonstrated by the constant saliva/plasma concentration ratios.