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ADMET and DMPK, Vol. 9 No. 1, 2021.

Original scientific paper

https://doi.org/10.5599/admet.916

In vitro pH dependent passive transport of ketoprofen and metformin

Alisa Elezović orcid id orcid.org/0000-0003-0559-1463 ; 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 orcid id orcid.org/0000-0001-5738-9588 ; University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
Selma Špirtović-Halilović orcid id orcid.org/0000-0001-8845-969X ; University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
Ognjenka Rahić orcid id orcid.org/0000-0003-0183-1124 ; University of Sarajevo, Faculty of Pharmacy, Bosnia and Herzegovina
Edina Vranić orcid id orcid.org/0000-0002-5067-8181 ; 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

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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.

Keywords

dynamic diffusion cell model; artificial membrane; in vitro permeation; BCS II; BCS III

Hrčak ID:

247494

URI

https://hrcak.srce.hr/247494

Publication date:

8.12.2020.

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