PMID: 11321673Apr 26, 2001Paper

Partition coefficients of beta-blockers in bile salt/lecithin micelles as a tool to assess the role of mixed micelles in gastrointestinal absorption

Biophysical Chemistry
B de CastroS Reis

Abstract

The objective of this study was to develop non-invasive spectroscopic methods to quantify the partition coefficients of two beta-blockers, atenolol and nadolol, in aqueous solutions of bile salt micelles and to assess the effect of lecithin on the partition coefficients of amphiphilic drugs in mixed bile salt/lecithin micelles, which were used as a simple model for the naturally occurring mixed micelles in the gastrointestinal tract. The partition coefficients (Kp) at 25.0 +/- 0.1degreesC and at 0.1 M NaCl ionic strength were determined by spectrofluorimetry and by derivative spectrophotometry, by fitting equations that relate molar extinction coefficients and relative fluorescence intensities to the partition constant Kp. Drug partition was controlled by the: (i) drug properties, with the more soluble drug in water (atenolol) exhibiting smaller values of Kp, and with both drugs interacting more extensively in the protonated form; and by (ii) the bile salt monomers, with the dihydroxylic salts producing larger values of Kp for the beta-blockers, and with glycine conjugation of the bile acid increasing the values of Kp for the beta-blockers. Addition of lecithin to bile salt micelles decreases the values of Kp of the beta-blocke...Continue Reading

References

Apr 1, 1991·Journal of Pharmaceutical Sciences·J H de SmidtD J Crommelin
Nov 1, 1972·Journal of Pharmaceutical Sciences·L MartisA L Thakkar
May 1, 1970·Journal of Pharmaceutical Sciences·M Gibaldi, S Feldman
Aug 1, 1969·Journal of Pharmaceutical Sciences·C H NightingaleM Gibaldi
Aug 1, 1968·Canadian Journal of Biochemistry·J P Kratohvil, H T DelliColli
Sep 1, 1984·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·M C Carey
Nov 1, 1983·Chemical & Pharmaceutical Bulletin·J ImaiM Hanano
May 1, 1995·Pharmaceutical Research·M P Grosvenor, J E Löfroth
Feb 1, 1996·Journal of Pharmaceutical Sciences·M R WenkJ Seelig
Jan 27, 1999·Journal of Pharmaceutical and Biomedical Analysis·B de CastroS Reis

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Citations

Dec 31, 2011·Chemistry Central Journal·Dejan M CirinVeljko S Krstonošić
Apr 4, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Elenaz NaderkhaniGøril Eide Flaten
Apr 3, 2016·Biomedical Chromatography : BMC·Laura J WatersGareth M B Parkes
Jun 30, 2005·Analytical Sciences : the International Journal of the Japan Society for Analytical Chemistry·Abdel-Aziz Y El-Sayed, Najeb A El-Salem
Jul 29, 2006·The Journal of Pharmacy and Pharmacology·Mariangeles Perez de la Cruz MorenoPatrick Augustijns
Mar 4, 2005·Langmuir : the ACS Journal of Surfaces and Colloids·Annegret HildebrandAlfred Blume
Jul 4, 2007·Journal of Pharmaceutical and Biomedical Analysis·Salette ReisJosé L F C Lima

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