Measurement of desipramine in brain tissue by a radioisotope derivative technique
Riva, E.; Hrdina, P.D.; Morselli, P.L.
Journal of Pharmacy and Pharmacology 27(10): 797-799
1975
ISSN/ISBN: 0022-3573 PMID: 241803 Document Number: 94664
Concentrations of desipramine in rat plasma and brain tissue simultaneously measured 15 and 60 min after i.p. administration of 10 mg kg-1 dose of the drug were: at 15 min plasma 259 .+-. 33 (n = 6), brain 1510 .+-. 170 (n = 5) brain:plasma ratio 5.8; at 60 min plasma 161 .+-. 13 (n = 8), brain 4060 .+-. 140 (n = 6) brain:plasma ratio 25.2. The brain concentrations of drug 60 min after injection (4.06 .+-. 0.14 .mu.g g-1) determined by using the radioisotope derivative technique are concordant with that (4.24 .mu.g g-1) measured spectrophotofluorometrically by Jori and others 1 h after the administration of 8 mg kg-1 of desipramine. The brain tissue to plasma ratio of drug increased from 5.8 at 15 min to 25.2 at 60 min after administration of a single dose which indicates that this tricyclic antidepressant rapidly leaves the blood and is accumulated in the brain. It is hoped that the adaptation of the radioisotope derivative technique of Hammer and Brodie for estimation of desipramine in brain tissue will be of help in studies concerning the brain distribution, brain to plasma ratios and pharmacokinetics of secondary amino tricyclic antidepressant compounds.