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In vitro metabolism of galanthamine hydrobromide (Nivalin®) by rat and rabbit liver homogenate

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Summary

The metabolism of galanthamine hydrobromide (Nivalin®) was investigated in rat and rabbit liver homogenates. Experiments were carried out varying several parameters of incubation: substrate (galanthamine hydrobromide, galanthamine, galanthaminone and epigalanthamine), cofactor enrichment (NADPH, NADP/G-6-P, NAD), pH (7.4 and 9.3), time of incubation. Substrates and metabolites were identified and quantitatively determined by GC/MS. In vitro metabolism in rat liver homogenate was negligible. The experiments with rabbit liver homogenate indicated, that galanthamine was actively metabolised the major metabolites being the oxidised product — galanthaminone, and the isomer of galanthamine — epigalantamine. The experimental results show that the metabolism of galanthamine is substrate and product stereoselective.

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Authors and Affiliations

  1. Department of Physical Chemistry, Faculty of Pharmacy, Medical Academy, Exs. Josif Str. 15, 1000, Sofia, Bulgaria

    Dia Mihailova, Mitko Velkov & Zvetanka Zhivkova

Authors
  1. Dia Mihailova
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  2. Mitko Velkov
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  3. Zvetanka Zhivkova
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Mihailova, D., Velkov, M. & Zhivkova, Z. In vitro metabolism of galanthamine hydrobromide (Nivalin®) by rat and rabbit liver homogenate. European Journal of Drug Metabolism and Pharmacokinetics 12, 25–30 (1987). https://doi.org/10.1007/BF03189858

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  • DOI: https://doi.org/10.1007/BF03189858

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