Effects of vegetable oils on the biological disposition of ethchlorvynol. I. the effects on the distribution of ethchlorvynol in rat.

Abstract

Distribution of ethchlorvynol (EC) to the blood, liver, jejunum, lung, kidney, adipose tissue and brain of rat were studied after oral administration of 150 mg/kg of EC in two dosage forms. The peaks of blood and tissue levels appeared more rapidly after dosing EC suspended in 5% polyethylene glycol 400 aqueous solution (PEG-sol.) than with vegetable oils, while the peak values were almost similar. The most remarkable effect of the oils used was shown in the brain levels of EC. The peak values of brain EC levels were 3.0, 5.9, and 5.9 μg/g wet tissue after dosing with corn oil, peanut oil and soybean oil, respectively, while 19.5 μg/g wet tissue with PEG-sol. The ED50 and LD50 of EC in mice were calculated as 138 mg and 357 mg/kg, respectively, when dosed as PEG-sol., while as 185 mg and 424 mg/kg when dosed together with corn oil. Thus, the vegetable oils were shown to inhibit the transport of EC into rat brain.