Rapid potentiometric determination of cholinesterases in plasma and red cells: Application to eptastigmine monitoring
Autor: | Luigi Zecca, Massimo Luzzana, Davide Radice, B. P. Imbimbo, E. Cazzola, Andrea Mosca, N. Lattuada, A. Auteri |
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Rok vydání: | 1993 |
Předmět: |
Physostigmine
Erythrocytes Potentiometric titration Administration Oral Pharmacology Toxicology chemistry.chemical_compound Pharmacokinetics Oral administration medicine Cholinesterases Humans Aged Cholinesterase Aged 80 and over Chromatography biology Red Cell Chemistry General Medicine Hydrogen-Ion Concentration Middle Aged Acetylcholinesterase Enzyme inhibitor Potentiometry biology.protein Cholinesterase Inhibitors Drug Monitoring medicine.drug |
Zdroj: | Chemico-Biological Interactions. 87:265-268 |
ISSN: | 0009-2797 |
DOI: | 10.1016/0009-2797(93)90053-2 |
Popis: | Eptastigmine (MF 201) is a new physostigmine derivative with potent inhibitory activity on cholinesterases. Here we present a new potentiometric cholinesterase activity assay suitable for MF 201 monitoring. The analysis is performed on a differential pH system and has the following characteristics: (a) within-run precision: C.V. 2.0% (plasma cholinesterase), 1.8% (red cell cholinesterase); (b) between-run precision: C.V. 4.0% (plasma cholinesterase); (c) linearity: 1-10 kU/l (plasma cholinesterase), 6-70 U/g Hb (red cell cholinesterase); (d) comparison with a reference method (x, HITACHI 737 Boerhinger Mannheim, Italy): y = 0.785x - 0.07; n = 37; r = 0.998. The assay has been applied to the determination of plasma and red cell cholinesterase activity in volunteers over 60 years of age treated with a single oral dose of 30 mg eptastigmine. We found that red cell cholinesterase is selectively inhibited after MF 201 administration with the following kinetics (time, % of inhibition, mean +/- S.E., n = 6): 0 h, 0; 1 h, 17 +/- 4.6; 2 h, 24 +/- 4; 4 h, 23 +/- 4.4; 12 h, 14 +/- 3. Eptastigmine plasma levels were also determined by a HPLC method: maximum concentration was found one hour after drug administration. |
Databáze: | OpenAIRE |
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