Medium-throughput pKa screening pharmaceuticals by pressure-assisted capillary electrophoresis.
Electrophoresis
; 22(6): 1112-8, 2001 Apr.
Article
in En
| MEDLINE
| ID: mdl-11358135
ABSTRACT
A fast screening method for the determination of the dissociation constants (pKa) of acidic, basic, and multivalent compounds was developed by using pressure-assisted capillary electrophoresis (PACE). External air pressure was applied to shorten the analysis time. The separation efficiency decreases as air pressure increases. However, it was found that air pressure does not affect the measurement of electrophoretic mobility and pKa significantly when it is less than 2 psi. The method was evaluated in terms of accuracy, precision, and ruggedness by using a set of 48 compounds with literature pKa values ranging from 2 to 10. The difference between the measured pKa values and literature values is less than 0.2 units. The throughput is approximately 20 compounds per day with a 12-point measurement ranging from pH 2.5 to 11. It was demonstrated that this method is applicable for pKa screening of pharmaceuticals with diverse chemical structures.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Electrophoresis, Capillary
Type of study:
Diagnostic_studies
/
Screening_studies
Language:
En
Journal:
Electrophoresis
Year:
2001
Document type:
Article
Affiliation country:
United States
Country of publication:
ALEMANHA
/
ALEMANIA
/
DE
/
DEUSTCHLAND
/
GERMANY