Corticosteroid水溶性誘導体の製剤学的研究(第5報) : Corticosteroid 21-Ester類と血清たんぱくとの結合

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Binding of corticosteroid 21-ester derivatives with serum protein was examined by the equilibrium dialysis method. For serum proteins, bovine serum albumin, bovine serum α-globulin, rabbit serum, and human serum were used. Parameters for the binding of 18 kinds of derivatives with bovine serum albumin were examined under the condition of 15° and pH 7.4,and all the derivatives were found to follow the Langmuir-type binding formula. In the case of hemiester derivatives, a correlation was found to exist between the binding constant, K, and apparent pK_a value, suggesting that electrostatic binding is dominant in these cases. In general, binding rate was found to be greater in carboxylic acid derivatives than in amine derivatives. Examinations were also made on the binding rate of these derivatives with bovine serum α-globulin, rabbit serum, and human serum, and the results therefrom suggested that these derivatives were chiefly bound to albumin in these sera. Effect of pH on the binding of some of the derivatives with bovine serum albumin was also examined.
1971-08-25