Determination of bromperidol in serum by automated column-switching high-performance liquid chromatography.

A column-switching high-performance liquid chromatographic method with ultraviolet detection is described for the simple and rapid determination of bromperidol, a neuroleptic drug, in dog and human sera. The drug in serum and trifluperidol added to the serum as an internal standard were extracted with hexane-chloroform, and the extract was subjected to automated column-switching high-performance liquid chromatography using a hydrophilic metaacrylate polymer column (TSK gel PW precolumn) for sample clean-up and a reversed-phase column (TSK gel ODS-80TM) for separation. The detection limit of bromperidol is 0.3 ng/ml serum and the recovery of bromperidol added to serum (2.7-16.0 ng/ml) was satisfactory with a standard deviation of 3% or less.

Pharmacokinetic study of iminodibenzyl antipsychotic drugs, clocapramine and Y-516 in dog and man.

The pharmacokinetic properties of the iminodibenzyl antipsychotic drugs clocapramine (CCP, 3-chloro-5-[3-(4-carbamoyl-4-piperidino piperidino) propyl]-10, 11-dihydro-5H-dibenzo[b, f]azepine) and Y-516 (3-chloro-5-[3-(2-oxo-1, 2, 3, 5, 6, 7, 8, 8a-octahydroimidazo [1,2-a] pyridine-3-spiro-4'-piperidino) propyl]-10, 11-dihydro-5H-dibenzo[b, f]azepine) were investigated in dog and man. Dogs were administered CCP and Y-516 intravenously, intraperitoneally, and orally, and the concentrations of the parent drugs and their metabolites in the plasma and urine were determined. Half-life (t1/2) was approximately the same by all three administration routes, being approximately 5 h for CCP and 3 h for Y-516. Bioavailability following oral administration was 0.16 +/- 0.01 (mean +/- SD, n = 3) for CCP and 0.29 +/- 0.07 for Y-516. The fractions of dose absorbed following oral administration were 0.43 +/- 0.07 and 0.79 +/- 0.24, and the fractions of dose metabolized in the liver due to the first-pass effect were 0.63 +/- 0.05 and 0.63 +/- 0.04 for CCP and Y-516, respectively. Y-516 was detected in the plasma after intraperitoneal and oral administration of CCP. The ratio of the AUC of Y-516 to that of CCP was 0.06 following intraperitoneal administration and 0.40 following oral administration. This indicated that while the metabolism of CCP into Y-516 may occur partly in the liver due to the first-pass effect, it occurs mostly within the gastrointestinal tract itself or its mucosa.(ABSTRACT TRUNCATED AT 250 WORDS)

Spectroscopic imaging by dephasing amplitude changing (SIDAC).

A technique for spectroscopic imaging based on a new concept of dual encoding (i.e., both phase and frequency encoding) of position along the direction of the read-out gradient is proposed. The phase encoding is produced by changing the amplitude of the dephasing gradient as in conventional phase encoding. High-resolution spectroscopic images of a normal human thigh obtained by a 2.0 Tesla whole body MR imaging system are presented.