Transformation and Excretion of Drugs in Biological Systems. II. Transformation of Metoclopramide in Rabbits

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In order to understand the transformation metoclopramide, 4-amino-5-chloro-N-[2-(diethylamino)-ethyl]-2-methoxybenzamide (M), in the body, the excrements in the urine of rabbits after the oral administration were examined. As a result, the five transformation products were revealed together with the parent compound. The urine was adjusted to pH 11-12,followed by extracting with ethylene dichloride ; thus, unchanged M and the two transformation products were found in the organic layer : One of the transformates was an oxidation product of the primary amino group so that the reduction of this product resulted in the parent compond. The other was identified to be 4-amino-5-chloro-N-[2-(ethylamino)-ethyl]-2-methoxybenzamide corresponding to M deethylated. At pH 4-5,a compound which was preferably extracted into ethylene dichloride was confirmed as 4-amino-5-chloro-2-methoxy benzoic acid resulting form rupture of the acid amide bond. Water-soluble products, on the other hand, were established as N^4-glucuronide and N^4-sulfonate of M. These two conjugates and unchanged M were detected to be the major urinary constituents on the thin-layer chromatogram. However, no evidence was obtained for the presence of N^4-acetyl conjugate.
公益社団法人日本薬学会の論文
1970-08-25