Abstract
Parallel experiments were conducted with equivalent doses of chloral hydrate and HY-185 in animals and man. Larger quantities of trichlorethanol and trichlonacetic acid were formed from chloral hydrate than from HY-185, as shown by the tissue levels and excretion products in the urine. High levels of HY-185 were found in the blood serum of the rat and dog, while chloral hydrate was present in low concentrations. The results indicate that HY-185 is more stable than chloral hydrate in the body, breaking down slowly to yield trichlorethanol and trichloracetic acid. Trichlonethanol was found in rat brain after the administration of HY-185 or chloral hydrate, but no appreciable amounts of unchanged drug were detected.
The principal metabolic product of HY-185 was isolated from human urine by countercurrent separation and identified as the glucuronide from microanalytical data on the isolated material and on its triacetyl methyl ester derivative. Glucuronic acid and HY-185 were also identified in the acid hydrolysate by paper chromatography. The excretion of this conjugate clearly indicates that the intact drug is absorbed from the intestinal tract without need for preliminary hydrolysis.
Footnotes
- Received May 6, 1957.
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