Farmakologiia i toksikologiia 1988-01-01

[Dependence of the absorption through the human oral mucosa of antihistaminic (H1) preparations on their physicochemical properties].

K I Bender, A N Lutsevich

Index: Farmakol. Toksikol. 51(1) , 75-9, (1988)

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Abstract

Antihistaminic (H1) drugs pipolphen, suprastin and dimedrol are characterized according to absorption through human oral mucosa and distribution between phosphate buffer solution and organic solvents at various medium pH values. Their constants of ionization and coefficients of distribution in the n-octanol--phosphate buffer system, pH 7.4, as well as the bound fraction at the interaction of these drugs with human serum albumin were determined. The relationship between absorption through human oral mucosa of antihistaminic drugs and the hydrophobic character of their molecules and constants of ionization was found. An attempt was made to predict for them on the basis of the authors' own results and literature data possible pharmacokinetic and pharmacodynamic behavior in the organism.