[Distribution of 14C-pethidine in the blood of certain species]

Binding of 14C-pethidine to erythrocytes of some species, particularly human, rat and rabbit, was examined in two different concentrations. This binding was investigated by direct measurement of the relative representation in erythrocytes, plasma proteins and the free fraction in blood. In the case of human erythrocytes the relative representation was 33%, in the rat ones 44%, and in the rabbit ones 54%. The fraction bound to plasma proteins was 45% in man, 29% in rats, and 27% in rabbits. The portion of the free fraction was 22% in man, 27% in rats, and 19% in rabbits. The ratio of the concentrations of the fraction bound to erythrocytes and the fraction free in the blood was 1.72 in man, 2.09 in rats, and 3.92 in rabbits. On the basis of these results it can be concluded that binding of pethidine to erythrocytes does not play an insignificant part in total pharmacokinetics of pethidine.