塩酸エプラジノンの生体内運命の研究(第1報)塩酸エプラジノンの吸収, 生体内分布および排泄について

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Absorption, distribution, and excretion of an antitussive piperazine derivative, Eprazinone hydrochloride (I), in mice, rats, rabbits, and men were studied by autoradiography, liquid scintillation counting, and colorimetry. In whole-body autoradiogram of mice, the radioactivity was found in a high level in bladder urine, already 15 min and was found only in the large intestine and gall bladder 12 hr after oral administration of ^3H-I. Rapid absorption and excretion, and a little accumulation of this drug in mice were suggested by these findings. Estimation of the drug remaining in the gastrointestinal tract of rats after oral administration of I revealed that absorption of I was rapid. The radioactivity in blood of rats and rabbits reached a maximum 2 and 1 hr, respectively, after oral administration of ^3H-I. The radioactivity in rat tissues was found in the carcase and in the liver in a high level, and in the brain in a trace. The excretion of Eprazinone (Ia) from rat feces was greater than that from urine after both oral and intravenous administration. Excretion of the drug from rat bile was great, and this fact suggested that the large excretion of Eprazinone (Ia) from rat bile played an important role. In the rabbit, excretion of the drug from urine was dominant, but the amount excreted from feces could not be neglected.
社団法人日本薬学会の論文
1975-08-25