Objective: to estimate the perfluorane adsorption capacity of the drugs belonging to different pharmacological groups. Materials and methods. The binding of perfluorane to 50 drugs at concentrations of 12.5 to 100 ^M was studied in vitro using equilibrium dialysis. Results. Interactions of ligands with the particles of perfluorane emulsion were found to be of three types. Type 1 substances were characterized by negative affinity to perfluorane; type 2 ligands acted indifferently with the emulsion; type 3 compounds were reversibly adsorbed with the particles of the blood substitute by the affinity constants ( Kaff) of 104 M-1. Conclusion. The perfluorane adsorption capacity is ambiguous and seems to depend on the properties of ligands. Type 3 interactions, which may lead to an increase in blood adsorption capacity and change in the pharmacokinet-ics of drugs used in combination with perfluorane, appear to be the most important. Key words: perfluorane, binding, drugs, drug interactions.
The relationships between drug affinity constant (Kag) for the particles of perfluorane nanoemulsion and physicochemical properties of ligands were studied by correlation and multiple regression analyses. The following parameters were applied: lipophilicity (LogP), molecular weight (MW), topological polar surface area (TPSA), the number of hydrogen donors (Don) and acceptors (Acc) in the formation of a hydrogen bonds, the number of rotating bonds (Rot), and drug molecule ionization constant (pKa). The Kaf — physicochemical properties relationships were found to be mainly nonlinear and to mostly show up in the lipophilicility parameter LogP of ligands. During the multiple regression analysis, a number of regression equations were derived, which described the relationship of the perfluorane affinity Kaf to the physicochemical properties of drugs and could predict this interaction for both existing and newly synthesized compounds.
Objective: to estimate the perfluorane adsorption capacity of the drugs belonging to different pharmacological groups. Materials and methods. The binding of perfluorane to 50 drugs at concentrations of 12.5 to 100 ^M was studied in vitro using equilibrium dialysis. Results. Interactions of ligands with the particles of perfluorane emulsion were found to be of three types. Type 1 substances were characterized by negative affinity to perfluorane; type 2 ligands acted indifferently with the emulsion; type 3 compounds were reversibly adsorbed with the particles of the blood substitute by the affinity constants ( Kaff) of 104 M-1. Conclusion. The perfluorane adsorption capacity is ambiguous and seems to depend on the properties of ligands. Type 3 interactions, which may lead to an increase in blood adsorption capacity and change in the pharmacokinet-ics of drugs used in combination with perfluorane, appear to be the most important. Key words: perfluorane, binding, drugs, drug interactions.