Abstract
K203 is an experimental bis–pyridinium mono–aldoxime type cholinesterase reactivator of potential use in organophosphate⁄ organophosphonate poisoning. Pharmacokinetics of K203 were examined in Wistar rats and beagle dogs using ion–pair HPLC. Serum and cerebrospinal fluid concentrations of K203 were determined using ion–pair reversedphase chromatography on octadecyl silica column. HPLC with ultraviolet detection was used for determination of serum concentration of K203 higher than 0.1 μg⁄mL while its low concentrations in cerebrospinal fluid required electrochemical detection (0.015 through 4 μg⁄mL range). In rats the serum levels of K203 followed zero order pharmacokinetics from 15 to 120 minutes post administration. Zero order pharmacokinetics was also observed in beagle dogs after low dose (15 μmol⁄kg) of K203 administration. High dose administration (250 μmol⁄kg) led to subsequent hindered elimination from both cerebrospinal fluid and serum.
Keywords: Amperometric detection, beagle dogs, HPLC, K203, pharmacokinetics, rats, serum level, UV detection
Current Medicinal Chemistry
Title:Study on Medicinal Chemistry of K203 in Wistar Rats and Beagle Dogs
Volume: 20 Issue: 16
Author(s): H. Kalasz, P. Szegi, G. Janoki, L. Balogh, Z. Postenyi, K. Musilek, G.A. Petroianu, A. Siddiq and K. Tekes
Affiliation:
Keywords: Amperometric detection, beagle dogs, HPLC, K203, pharmacokinetics, rats, serum level, UV detection
Abstract: K203 is an experimental bis–pyridinium mono–aldoxime type cholinesterase reactivator of potential use in organophosphate⁄ organophosphonate poisoning. Pharmacokinetics of K203 were examined in Wistar rats and beagle dogs using ion–pair HPLC. Serum and cerebrospinal fluid concentrations of K203 were determined using ion–pair reversedphase chromatography on octadecyl silica column. HPLC with ultraviolet detection was used for determination of serum concentration of K203 higher than 0.1 μg⁄mL while its low concentrations in cerebrospinal fluid required electrochemical detection (0.015 through 4 μg⁄mL range). In rats the serum levels of K203 followed zero order pharmacokinetics from 15 to 120 minutes post administration. Zero order pharmacokinetics was also observed in beagle dogs after low dose (15 μmol⁄kg) of K203 administration. High dose administration (250 μmol⁄kg) led to subsequent hindered elimination from both cerebrospinal fluid and serum.
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Cite this article as:
Kalasz H., Szegi P., Janoki G., Balogh L., Postenyi Z., Musilek K., Petroianu G.A., Siddiq A. and Tekes K., Study on Medicinal Chemistry of K203 in Wistar Rats and Beagle Dogs, Current Medicinal Chemistry 2013; 20 (16) . https://dx.doi.org/10.2174/0929867311320160006
DOI https://dx.doi.org/10.2174/0929867311320160006 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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