A method was developed to measure bioavailability of lidocaine by simultaneous peroral and intravenous dosing. Lidocaine hydrochloride corresponding to 125 mg base was given perorally. Simultaneously, 30 mg of deuterated lidocaine-d, were injected intravenously. Blood samples were taken at intervals for 270 min. Plasma samples were spiked with mepivacaine hydrochloride as internal standard, alkalinized to pH 11.7 and extracted with diethyl ether. The extracts were analysed by capillary GC ammonia CI MS using a 15 m X 0.32 mm i.d. glass capillary column coated with SE-54. The ion source pressure was 0.4 Torr of ammonia as reagent gas. Quasimolecular ions were monitored at m / z 235, 238 and 247 for lidocaine, lidocaine-d, and mepivacaine, respectively.
Calibration curves were linear from 0.2 to 5.0 nmol lidocaine ml-' plasma. Interday reproducibility of this method was 6.9% for lidocaine-d, ( n = 16; 1.90f0.13 nmol ml-'). Bioavailability of lidocaine in 5 normal volunteers ranged from 26 to 36% (mean 31 f SD 5%) and in a cirrhotic with an end-to-side portacaval shunt it approached loo%, as anticipated. The method is well suited for determination of bioavailability of lidocaine after simultaneous administration of rather small and safe doses both intravenously and perorally.