Biopharm Drug Dispos. 1990 Aug-Sep;11(6):533-41. doi: 10.1002/bdd.2510110607.

Pharmacokinetics of aditoprim in goats using a radioassay.

Biopharmaceutics & drug disposition

M P Iqbal, N Mahboobali, S K Niazi, M A Mahmood

PMID: 2207303 DOI: 10.1002/bdd.2510110607

Abstract

A simple, highly sensitive radioassay was developed for the activity of a newly discovered inhibitor of dihydrofolate reductase (DHFR), aditoprim. The procedure is based on the inhibition of binding of [3H]-methotrexate ([3H]MTX) with bacterial dihydrofolate reductase by the antifolate, aditoprim. The analytic sensitivity using this binding inhibition method was less than 5 ng in plasma. The procedure developed requires no extraction of the drug from the plasma. The variation of simultaneous duplicate determinations was 6.3 per cent, whereas the variability of plasma samples assayed on different days was less than 11 per cent. The assay developed was applied to study the pharmacokinetics of aditoprim in the goat. In comparison with trimethoprim (TMP), the new inhibitor of DHFR, aditoprim, had a longer half-life and a larger volume of distribution, suggesting enhanced and prolonged antibacterial activity of aditoprim over TMP.

Substances

• Folic Acid Antagonists
• aditoprim
• Trimethoprim

MeSH terms

• Animals
• Folic Acid Antagonists*
• Goats
• Half-Life
• Models, Biological
• Radioligand Assay
• Sheep
• Trimethoprim / analogs & derivatives
• Trimethoprim / blood
• Trimethoprim / pharmacokinetics

Publication Types

• Journal Article

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