Monitoring the Level of 14C-Labelled Selegiline Following Oral Administration



Huba Kalász1, *, Kornélia Tekes2, Erzsébet B. Faigl3, Zita Pöstényi1, Eszter Berekméri1, Gellért Karvaly4, Ernest Adeghate5
1 Department of Pharmacology and Pharmacotherapy, Semmelweis University, Budapest, Hungary
2 Department of Pharmacodynamics, Semmelweis University, Budapest, Hungary
3 Laboratory of Synthesis, Institute of Isotopes, Budapest, Hungary
4 Department of Laboratory Medicine, Semmelweis University, Budapest, Hungary
5 Department of Anatomy, College of Medicine and Health Sciences, United Arab Emirates University, Al Ain, United Arab Emirates


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© Kalász et al.; Licensee Bentham Open

open-access license: This is an open access article licensed under the terms of the Creative Commons Attribution-Non-Commercial 4.0 International Public License (CC BY-NC 4.0) (https://creativecommons.org/licenses/by-nc/4.0/legalcode), which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.

* Address correspondence to this author at the Department of Pharmacology and Pharmacotherapy, Semmelweis University, H-1089 Budapest, Nagyvárad tér 4, Hungary; Tel: +36-30-274-7486; E-mail: drkalasz@gmail.com


Abstract

Background:

Selegiline [(-)-deprenyl] is widely used for the treatment of Parkinson’s disease in humans.

Objective:

Time-dependence of tissue distribution of selegiline following per os administration to rats.

Method:

Oral administration of radiolabeled selegiline to rats resulted in a pattern of tissue distribution similar to that following intraperitoneal injection. Analyses were done using both reversed-phase HPLC and also by counting radioactivity in various body compartments of rats.

Results:

As a consequence of oral administration of 30 mg/kg of selegiline, its level in the stomach was extremely high (179.57 µg/g tissue through 54.67 µg/g at 15 min to 120 min), that is one magnitude higher than that in the serum level. High selegiline concentrations were also detected in the lacrimal glands (7.45 µg/g), kidneys (6.87 µg/g), livers (6.01 µg/g) and lungs (3.47 µg/g) after 30 minutes of application, which were higher than after intraperitoneal injections.

Conclusion:

The relatively high tissue levels remained for 120 min monitoring. Selegiline levels in the brain (1.69 µg/g) and in the testes (1.88 µg/g) were also considerably higher than following intraperitoneal administration during the entire period of observation (15 to 120 min).

Keywords: Selegiline, (-)-Deprenyl, Rats, Distribution, HPLC, Oral administration.