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Original Article

Pharmacokinetics of a new imidazoline receptor agonist in rat plasma after intragastric and intravenous administration

Kulikov Aleksandr, Avtina Tatyana, Pokrovsky Mikhail, Korokin Mikhail.

3-(1h-benzimidazol-2-yl)-1,2,2- trimethylcyclopentancarboxylic acid (C7070) is a novel synthetic imidazoline receptor agonist - potential antidiabetic agent. This study aimed to obtain the pharmacokinetic profiles in rats. Additionally, an HPLC MS/MS method was developed and validated to quantify C7070 in rat plasma. The pharmacokinetic profiles of intragastric and intravenous administration routes at singles doses of 50 mg/kg, were studied in rats. The elimination half-life of intravenously administered C7070 was approximately 154,1 min. The maximum plasma level of C7070 was reached approximately 170 min (2,8 h) after intragastric administration, with a Cmax value of 17,6 μg/mL and an AUC (o-t) value of 6964 μg*min-1/mL; the oral bioavailability was approximately 18%.

Key words: New antidiabetic agent; HPLC MS/MS; Pharmacokinetics; Imidazoline receptor agonist; C7070; Rat.

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