In vitro pH dependent passive transport of ketoprofen and metformin

  • Alisa Elezović University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Amina Marić University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Amila Biščević University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Jasmina Hadžiabdić University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Selma Škrbo University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Selma Špirtović-Halilović University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Ognjenka Rahić University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Edina Vranić University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
  • Amar Elezović Control laboratory of the Agency for Medicinal Products and Medical Devices, Sarajevo, Bosnia and Herzegovina
In vitro pH dependent passive transport of ketoprofen and metformin

Abstract

The kinetics of passive transport of ketoprofen and metformin, as model substances for high and low permeability, respectively, across the artificial membrane under the influence of the pH of donor solution was investigated. There was an upward trend in the apparent permeation coefficient (Papp) of ketoprofen with the decrease in pH to a value close to pKa. At the pH value below pKa the permeation coefficient had lower value, due to the higher retention of ketoprofen in the artificial membrane. Metformin is a low permeable compound, and the highest permeation values were recorded at pH 7.4. Two dissociation constants determine that metformin at physiological pH exists as a hydrophilic cationic molecule, i.e. predominantly in ionized form. At pH values below 2.8, metformin mainly exists in diprotonated form, and it was, thus, very poorly permeable. The highest retention, i.e. affinity of both ketoprofen and metformin to the membrane, was at the lowest pH values, which is explained by different mechanisms. At higher pH values of the donor compartment, the substances showed significantly less affinity to the membrane. The obtained values of apparent permeation coefficients at studied pH values showed a good correlation with the obtained experimental values by other in vitro methods.

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Published
08-12-2020
Section
Original Scientific Articles