Using capillary electrophoresis/frontal analysis to screen drugs interacting with human serum proteins

Electrophoresis
P A McDonnellJ A Masucci

Abstract

We have used capillary electrophoresis in the frontal analysis mode (CE/FA) to determine the binding capacity of beta-adrenoceptor blocking drugs to individual serum proteins, serum protein mixtures and human serum. The free drug concentration was directly measured from the height of the frontal peak and used to calculate the bound drug concentration. From the bound drug concentration, the percentage of drug bound to the serum proteins alpha1-acid glycoprotein (AGP) and human serum albumin (HSA) was then determined. In addition to determining the percent of a drug bound to a protein, the drug-protein association constant (Ka) was determined for AGP binding to beta-blockers. The data-estimated association constants were consistent with literature values. The CE/FA studies on the beta-adrenoceptor blocking drugs and the serum proteins indicated that HSA, AGP, high density lipoprotein (HDL), and low density lipoprotein (LDL) were the main contributors to serum binding for this series of compounds. The serum-drug binding data sorted the beta-adrenoceptor blocking drugs into high and low binding categories. The protein mixture (AGP + HSA + HDL + LDL) resulted in dividing the beta-blockers into the same high/low rankings. The protein...Continue Reading

References

Apr 1, 1977·Journal of Pharmaceutical Sciences·J J Vallner
Sep 11, 1992·Journal of Chromatography·J C KraakH Poppe
Jan 1, 1982·European Journal of Clinical Pharmacology·F M BelpaireM Rosseneu
Sep 1, 1983·British Journal of Clinical Pharmacology·E PikeP K Lunde
Jan 1, 1984·Clinical Pharmacokinetics·W F BowersJ Thompson
Sep 1, 1981·Biochemical Pharmacology·M L KornguthB S Eichelman

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Citations

May 31, 2001·Electrophoresis·K L Rundlett, D W Armstrong
Mar 29, 2002·Electrophoresis·Yasushi IshihamaNaoki Asakawa
Nov 25, 2003·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·C BertucciV Andrisano
Apr 10, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Yoshihide Tanaka, Shigeru Terabe
Oct 29, 1998·Journal of Chromatography. B, Biomedical Sciences and Applications·N H HeegaardN A Guzman
Jan 5, 2002·Journal of Pharmaceutical and Biomedical Analysis·Takanori OhnishiMicheal E El Kommos
Oct 9, 2002·Journal of Pharmaceutical and Biomedical Analysis·Zhongjiang JiaMin Zhong
Jan 24, 2004·Vojnosanitetski pregled. Military-medical and pharmaceutical review·Gordana Zunić
Aug 10, 2001·Drug Metabolism Reviews·Z H Israili, P G Dayton
Apr 26, 2008·Journal of Pharmaceutical and Biomedical Analysis·Qin-hua LuDong-ying Chen
Mar 7, 2007·Journal of Chromatography. a·M A Martínez-GómezM J Medina-Hernández
Sep 1, 2006·Electrophoresis·María A Martínez-GómezMaria J Medina-Hernández
May 30, 2006·Electrophoresis·Jesper Ostergaard, Niels H H Heegaard
Dec 30, 2009·Electrophoresis·Chunxia Jiang, Daniel W Armstrong
Apr 17, 2016·Journal of Pharmaceutical and Biomedical Analysis·Klára L Valkó
Mar 29, 2002·Electrophoresis·Niels H H HeegaardDavid D Y Chen
Feb 24, 2001·Electrophoresis·R M Guijt-van DuijnE Baltussen

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