In vitro and in vivo studies on degradation of quinalphos in rats

Abstract

A pharmacokinetic in vitro and in vivo degradation study has been carried out in rat to evaluate the deleterious effects of exposure to quinalphos on a target population. Degradation of quinalphos in simulated gastric and intestinal phases has been investigated. The metabolic intermediates of quinalphos in serum and urine of albino rats at different time intervals were identified after dosing the animals with 5mgkg -1 body weight. All the samples were lyophilised, extracted and analysed by HPLC and GC-MS. The rate of degradation of quinalphos was accelerated in the presence of the enzymes pepsin and pancreatin contained in the gastric and intestinal simulations, respectively. Quinalphos oxon, O-ethyl-O-quinoxalin-2-yl phosphoric acid, 2-hydroxy quinoxaline and ethyl phosphoric acid are among the important metabolites identified both in in vitro and in vivo investigations. In simulated in vitro study some isomerised derivatives which were missing in the blood and urine of treated animals were identified. This could possibly be either due to non-formation or faster decay of the isomerised derivatives because of slightly different conditions prevailing in the two cases. The results also indicate that the metabolites, 2-hydroxy quinoxaline and oxon, which are more toxic than the parent compound, seem to persist for a longer time. © 2012.