Metabolism of Simeconazole in Rats

Abstract

C-Simeconazole was diluted as required by the addition of appropriate quantities of non-radiolabeled simeconazole. The solutions for dosing were prepared by dissolving or suspending 14 C-simeconazole in a 10% aqueous solution of Tween 80. Rats were orally administered 14 C-simeconazole at a dose of 5 mg/kg b.w. (low dose) and 70 mg/kg b.w. (high dose) using a gastric tube. The high-dose level was one-tenth the acute oral LD 50 for male and female rats. Rats were fasted overnight pre-dosing and fed approximately 2 hr post-dosing. 3. Excretion Five male and five female rats were orally administered 5 and 70 mg/kg b.w. of 14 C-simeconazole. The treated animals were

Organosilicon Molecules with Medicinal Applications

“…The initial interest in the metabolism of organosilicon molecules stems from the reports on the stability of silicones in the environment . The metabolism of organosilanes has been studied and in many cases shown to follow standard metabolic and clearance pathways expected for related carbon analogues. , Similar metabolic rates and standard oxidation products have been identified where oxidation typically occurs at carbons adjacent to silicon, including some eventual cleavage of the Si–C bonds. In the case of siloxanes, oxidation products including silanols are observed.…”

Environmental Chemistry of Organosiloxanes

“…Another reaction cycle resulted in the corresponding silanediol. In addition, the Si–CH 2 bond was cleaved, possibly by an analogous mechanism; see Scheme …”