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Stability, blood partition, and protein binding of a chemoprotective agent, 2-(allylthio)pyrazine.
- Source :
-
Research communications in molecular pathology and pharmacology [Res Commun Mol Pathol Pharmacol] 1998 Aug; Vol. 101 (2), pp. 171-8. - Publication Year :
- 1998
-
Abstract
- The stability of 2-AP, a chemoprotective agent, in various pH solutions and human gastric juice, the blood partition of 2-AP between plasma and blood cells, and the factors influencing the binding of 2-AP to 4% human serum albumin (HSA) were evaluated. 2-AP was stable in human gastric juice and pH solutions ranging from 1 to 12, however, 2-AP was unstable in pH 13 solution; the disappearance rate constant was 0.00759/h. 2-AP reached equilibrium rapidly between plasma and blood cells of rabbit blood. The equilibrium plasma/blood cells partition ratios were independent of initial rabbit blood concentrations of 2-AP, 1, 5, and 10 micrograms/ml; the values were in the range of 5.99-11.8. Binding of 2-AP to 4% HSA was dependent on HSA concentration, incubation temperature, 'the buffer' pH, and addition of acetylsalicylic acid. The binding of 2-AP was independent of buffers containing various concentrations of chloride ion, heparin, and alpha-1-acid glycoprotein.
- Subjects :
- Animals
Chromatography, High Pressure Liquid
Drug Stability
Enzyme Inhibitors blood
Enzyme Inhibitors pharmacokinetics
Gastric Juice chemistry
Humans
Hydrogen-Ion Concentration
Pyrazines blood
Pyrazines pharmacokinetics
Rabbits
Enzyme Inhibitors metabolism
Pyrazines metabolism
Serum Albumin metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1078-0297
- Volume :
- 101
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Research communications in molecular pathology and pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 9821213