Methadyl acetate was metabolized by microsomal preparations of rat liver to yield nor-methadyl acetate and 64dimethylamino)-4,4-diphenyl-3-heptanol. The identification and separation of these three compounds was established by TLC, using iodoplatinate spray as a visualizing agent.
Keyphrases Methadyl acetate-TLC analysis, metabolism by rat liver microsomal preparations TLC-analysis and separation of methadyl acetate from metabolites, rat liver microsomes 0 Analgesics-methadyl acetate, TLC analysis and separation from metabolites, rat liver microsomes Methadyl acetate, a potent, long-acting, narcotic analgesic (l), is currently under clinical evaluation for the treatment of opiate addiction (2, 3). Its usefulness as a substitute for methadone prompted the development of a simple, accurate, and sensitive method for its identification using TLC.
Few methods to identify methadyl acetate and its metabolites have been reported (4, 5). Sung and Way (6) reported a colorimetric determination from tissue homogenates. Kaiko and Inturrisi (7, 8) reported the detection of methadyl acetate [6-(dimethylamino)-4,4-diphenyl-3-heptanol acetate], 6-(methylamino)-4,4-diphenyl-3-heptanol acetate (nor-methadyl acetate), 6-(dimethylamino)-4,4-diphenyl-3-heptanol, and 6-(methylamino)-4,4-diphenyl-3-heptanol by GLC using 3% SE-30 on Gas Chrom Q, 3.8% W-98 on Diatoport S, 5% OV-17 on Gas Chrom Q, 4% XF-1112 on Chromosorb W, 3% XE-60 on Gas Chrom Q, 3% 8BP on Gas Chrom Q, and 3% OV-225 on Gas Chrom Q. Billings and McMahon (1) identified the trichloroacetamide derivative of nor-methadyl acetate using GLC with an electron-capture detector.
This paper describes a highly sensitive TLC method for the detection of methadyl acetate, 6-(dimethylamino)-4,4-diphenyl-3-heptanol, and nor-methadyl acetate.