トルブタマイドの生体内分布に関するオートラジオグラフィーによる研究

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タイトル別名
  • Studies on the Distribution of <SUP>14</SUP>C-tolbutamide in Rat after Oral Administration of the Drug.
  • トルブタマイド ノ セイタイナイ ブンプ ニ カンスル オートラジオグラフィー

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抄録

Although tolbutamide, a typical oral hypoglycemic drug, is widely used for the treatment of diabetes mellitus, the mechanism of the hypoglycemic effect and the side effects of the drug have not yet been entirely clarified. The author attempted to clarify the distribution of 14C-tolbutamide in rats after oral administration of the drug by using a whole-body autoradiographic procedure.<BR>Male Wister rats weighing about 100 g were subjected to autoradiography and following results were obtained.<BR>1) 14C-radioactivity in the duodenum and the colon reached the highest value after three hours and thereafter decreased gradually. In contrast, radioactivity in the cecum and in the rectum increased again after five hours. The radioactivity in the bile duct was very high. Judging from the fact that the concentration in the rectum was far lower than that in the cecum, the major portion of14C-radioactivity must be reabsorbed between the cecum and the rectum. A small portion of the14C must be excreted in the feces.<BR>2) The highest concentration of 14C in the whole body throughout the eight hour observation was in the bone marrow and in the lymph vessels.<BR>3) Radioactivity in the lungs, liver, kidney and thyroid gland was high. Radioactivity in the heart, pancreas, adrenal glands and spleen was also high, but not as high as that in the former group. The radioactivity in adipose tissue and in muscle tissue was very low. The radioactivity in urine bladder was very high, suggesting that the major portion of the 14C was excreated via the urine.<BR>Judging from above data, the extra-pancreatic effect of tolbutamide may be located in the bone marrow, lymph vessels, lung, kidney, liver and thyroid gland. The effect of tolbutamide o these tissues remains to be elucidated. It is also possible that tolbutamide may have some effect on the heart, spleen and abrenal glands. As the concentration of tolbutamide is very low in adipose tissue and in muscle tissue, the effect of the drug on these tissues may not be present in vivo.

収録刊行物

  • 糖尿病

    糖尿病 20 (5), 645-651, 1977

    一般社団法人 日本糖尿病学会

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