A Gradient HPLC Method for Quantitation of Cyclosporine and Its Metabolites in Blood and Bile

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Abstract
A quantitative gradient high performance liquid chromatographic method is reported for both cyclosporine and its metabolites. The identity of the metabolites was confirmed by radiolabelled products of rat liver perfusion studies and by chromatography of several pure standards. Recoveries of 95 and 97% were obtained for metabolite 17 and 1 using a diethyl ether extraction scheme in both blood and bile. Separation of cyclosporine and its metabolites in whole blood and plasma indicate that there is a significant temperature-dependent partitioning of these compounds between the erythrocyte and the plasma compartments of blood.