Document Detail


Medium-throughput pKa screening pharmaceuticals by pressure-assisted capillary electrophoresis.
MedLine Citation:
PMID:  11358135     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Z Jia; T Ramstad; M Zhong
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Electrophoresis     Volume:  22     ISSN:  0173-0835     ISO Abbreviation:  Electrophoresis     Publication Date:  2001 Apr 
Date Detail:
Created Date:  2001-05-18     Completed Date:  2001-12-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8204476     Medline TA:  Electrophoresis     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  1112-8     Citation Subset:  IM    
Affiliation:
Pharmacia Corporation, Pharmaceutics, Pharmaceutical Sciences, Kalamazoo, MI, USA.
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MeSH Terms
Descriptor/Qualifier:
Acetone
Buffers
Dimethyl Sulfoxide
Electrophoresis, Capillary / methods*
Hexanones
Hydrogen-Ion Concentration
Methanol
Pharmaceutical Preparations / analysis
Time Factors
Chemical
Reg. No./Substance:
0/Buffers; 0/Hexanones; 0/Pharmaceutical Preparations; 141-79-7/mesityl oxide; 67-56-1/Methanol; 67-64-1/Acetone; 67-68-5/Dimethyl Sulfoxide

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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