Simultaneous evaluation of apovincaminic acid esters and their metabolite apovincaminic acid by solvent partition and GLC in biological samples. Preliminary data with MR 711.
Apovincaminic acid (AVA) esters are eburnamenine derivatives with a vasodilating action that are mainly metabolized to AVA by enzymatic hydrolysis, in the rat in particular. In an organic solvent/water partition, AVA and AVA ester were quantitatively separated. AVA ester was then chemically hydrolysed into AVA. Unchanged AVA and AVA hydrolysed from its ester were separately methylated and quantitatively analysed by GLC. Using a flame ionisation detector, this method has a sensitivity of 20 ng making possible metabolic investigations to be carried out in vitro and in the urine and can be applied to any AVA ester. The method was applied in a preliminary investigation to MR 711, a methylene-methoxy-apovincaminic acid ester. When incubated in vitro with rat plasma, MR 711 was enzymatically converted into AVA. The urine of rats p.o. treated with 10 mg/kg of MR 711 contained AVA as the main metabolite.
D000818:Animals; D001711:Biotransformation; D002849:Chromatography, Gas / Q000379:methods; D008958:Models, Molecular; D051381:Rats; D014665:Vasodilator Agents / Q000032:analysis*; D014748:Vinca Alkaloids / Q000032:analysis*
D014665:Vasodilator Agents; D014748:Vinca Alkaloids; C032858:apovincaminic acid; C032859:methoxymethyl apovincaminate