Ritzl F, Feinendegen L E, Lintz W, Tisljar U
Arzneimittelforschung. 1978;28(7):1184-6.
Seven patients suffering from maturity on-set diabetes mellitus were given orally 100 mg of 14C-labelled butylbiguanide, specific activity 1.40 or 1.23 muCi/mg, resp. Three days before oral administration, two of the patients had received an i.v. injection of 50 mg butylbiguanide labelled with 120 muCi 14C. The radioactivity in the blood of the patients was followed up during the first 12-h period after administration of the drug. For determination of the radioactivity in the urine aliquots of three 24-h portions were measured. Furthermore, the radioactivity was checked of each individual sample of faeces for the first 72 h after administration. The radioactivity in the exhaled air was also measured. By comparison of the excretion after i.v. and oral application an absorption efficiency of 90% to 92% was calculated. Butylbiguanide is almost exclusively and fast excreted via the kidney. 86.5% of the i.v. administered material was eliminated within 24 h and 88.1% within 3 d in the urine of a person without kidney disease. Elimination through faeces was negligible, 0.2% in a person without kidney disease and 0.7% in a patient with renal insufficiency. The data obtained from the exhaled air show that there is only a negligible break-down of butylbiguanide, if any, to CO2 in man.
七名成年发病型糖尿病患者口服了100毫克14C标记的丁双胍，比活度分别为1.40或1.23微居里/毫克。在口服给药前三天，其中两名患者静脉注射了50毫克用120微居里14C标记的丁双胍。在给药后的头12小时内对患者血液中的放射性进行了跟踪。为测定尿液中的放射性，测量了三个24小时时段的等分试样。此外，在给药后的头72小时内对每份粪便样本的放射性进行了检查。还测量了呼出空气中的放射性。通过比较静脉注射和口服给药后的排泄情况，计算出吸收效率为90%至92%。丁双胍几乎完全通过肾脏快速排泄。在无肾脏疾病的人的尿液中，静脉注射给药物质的86.5%在24小时内被清除，88.1%在3天内被清除。通过粪便的排泄可忽略不计，在无肾脏疾病的人中为0.2%，在肾功能不全患者中为0.7%。从呼出空气中获得的数据表明，在人体中丁双胍分解为二氧化碳的情况（如果有的话）极少。
