Prolonged presence of isoxsuprine in equine serum after oral administration

Abstract

1. Isoxsuprine [1-(4-hydroxyphenyl)-2-(1-methyl-2-phenoxyethylamino)-1-propanol] serum concentrations after single- and multiple-dose administration to horse were investigated using immunoenzymatic ELISA, HPLC-UV and thermospray HPLC-MS methods.

2. Using HPLC-MS, isoxsuprine was detected up to 72 h after a single administration (1.2 mg/kg by gastric probe) and up to 96 h after the end of serial administration (1.2 mg/kg every 12 h for 7 days).

3. ELISA detected the drug up to 96 h after a single dose and up to 6 days after the end of prolonged administration.

4. Isoxsuprine is present in horse serum almost totally in conjugated form very likely as glucuronide.

5. It is concluded the administration of this drug must be suspended much earlier than previously presumed if race horse antidoping tests for the drug are to be negative.