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ZHANG Li, JIANG Cheng, CHEN Simin, YAO Ting, Xiang Ningling, SU Mengxiang, DI Bin. Determination of plasma protein binding of peptide drug candidates by dextran-coated charcoal[J]. Journal of China Pharmaceutical University, 2020, 51(5): 522-529. DOI: 10.11665/j.issn.1000-5048.20200503
Citation: ZHANG Li, JIANG Cheng, CHEN Simin, YAO Ting, Xiang Ningling, SU Mengxiang, DI Bin. Determination of plasma protein binding of peptide drug candidates by dextran-coated charcoal[J]. Journal of China Pharmaceutical University, 2020, 51(5): 522-529. DOI: 10.11665/j.issn.1000-5048.20200503
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Determination of plasma protein binding of peptide drug candidates by dextran-coated charcoal

Funds: This study was supported by the National Natural Science Foundation of China (No.81872833, No.81773693)
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  • Received Date: June 01, 2020
  • Revised Date: July 03, 2020
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    • Abstract
  • The conventional equilibrium dialysis and ultrafiltration methods cannot be used to determine the protein binding of some peptides because of their non-specific adsorption on the semipermeable membrane or poor stability in the plasma. The method of dextran-coated charcoal adsorption combined with LC-MS/MS were used. Based on the kinetic principle of initial rate of candidate drugs absorbed to dextran-coated charcoal, seven phosphorylated peptides with the same amino acid sequence and different configurations in rat plasma were selected as the study model using; the protein binding in rat plasma were determined; the amino acid distribution rules affecting the changes in protein binding rates of peptide candidate drugs were summarized. The results suggest that the dextran charcoal adsorption method, as a supplementary method for the determination of plasma protein binding, is suitable for peptides or organic drug candidates that cannot be determined by traditional techniques.
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    • References (8)
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