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Rahman M, Prianka F, Shohel M, et al. Interaction of palmitic Acid with metoprolol succinate at the binding sites of bovine serum albumin. Adv Pharm Bull. 2014;4(4):379-83doi: 10.5681/apb.2014.056.
Rahman, M., Prianka, F., Shohel, M., & Mazid, M. A. (2014). Interaction of palmitic Acid with metoprolol succinate at the binding sites of bovine serum albumin. Advanced pharmaceutical bulletin, 4(4), 379-83. https://doi.org/10.5681/apb.2014.056
Rahman, Mashiur, et al. "Interaction of palmitic Acid with metoprolol succinate at the binding sites of bovine serum albumin." Advanced pharmaceutical bulletin vol. 4,4 (2014): 379-83. doi: https://doi.org/10.5681/apb.2014.056
Rahman M, Prianka F, Shohel M, Mazid MA. Interaction of palmitic Acid with metoprolol succinate at the binding sites of bovine serum albumin. Adv Pharm Bull. 2014 Dec;4(4):379-83. doi: 10.5681/apb.2014.056. Epub 2014 Aug 10. PMID: 25436195; PMCID: PMC4137429.
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Adv Pharm Bull. 2014 Dec;4(4):379-83. doi: 10.5681/apb.2014.056. Epub 2014 Aug 10.

Interaction of palmitic Acid with metoprolol succinate at the binding sites of bovine serum albumin.

Advanced pharmaceutical bulletin

Mashiur Rahman, Farzana Prianka, Mohammad Shohel, Md Abdul Mazid

Affiliations

  1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka-1000, Bangladesh.
  2. Department of Pharmacy, North South University, Dhaka- 1229, Bangladesh.

PMID: 25436195 PMCID: PMC4137429 DOI: 10.5681/apb.2014.056

Abstract

PURPOSE: The aim of this study was to characterize the binding profile as well as to notify the interaction of palmitic acid with metoprolol succinate at its binding site on albumin.

METHODS: The binding of metoprolol succinate to bovine serum albumin (BSA) was studied by equilibrium dialysis method (ED) at 27°C and pH 7.4, in order to have an insight in the binding chemistry of the drug to BSA in presence and absence of palmitic acid. The study was carried out using ranitidine as site-1 and diazepam as site-2 specific probe.

RESULTS: Different analysis of binding of metoprolol succinate to bovine serum albumin suggested two sets of association constants: high affinity association constant (k1 = 11.0 x 10(5) M(-1)) with low capacity (n1 = 2) and low affinity association (k2 = 4.0×10(5) M(-1)) constant with high capacity (n2 = 8) at pH 7.4 and 27°C. During concurrent administration of palmitic acid and metoprolol succinate in presence or absence of ranitidine or diazepam, it was found that palmitic acid displaced metoprolol succinate from its binding site on BSA resulting reduced binding of metoprolol succinate to BSA. The increment in free fraction of metoprolol succinate was from 26.27% to 55.08% upon the addition of increased concentration of palmitic acid at a concentration of 0×10(-5) M to 16×10(-5) M. In presence of ranitidine and diazepam, palmitic acid further increases the free fraction of metoprolol succinate from 33.05% to 66.95% and 40.68% to 72.88%, respectively.

CONCLUSION: This data provided the evidence of interaction at higher concentration of palmitic acid at the binding sites on BSA, which might change the pharmacokinetic properties of metoprolol succinate.

Keywords: Binding sites; Bovine serum albumin; Equilibrium dialysis; Metoprolol succinate; Palmitic acid

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