Urinary concentrations of trimethoprim (TMP) and its metabolites were measured in eight healthy subjects after oral administration of 160 mg of TMP in two tablets of Septra® (trimethoprim-sulfamethoxazole). Improved procedures for extraction of polar metabolites and for enzymic cleavage of conjugated products were applied. The 1-oxide and conjugates of demethylated metabolites were found in substantially higher concentrations than those previously reported. A new metabolite, the 3-oxide of TMP, was identified, and urinary levels of this product were also measured.
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Sigel et al. (1973) studied this question.
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