Hausmann L, Schumann G, Kaffarnik H
Arzneimittelforschung. 1978;28(1):83-6.
12 metabolically healthy subjects were i.v. administered equipotent doses (ED30) of tolbutamide (7.5 mg/kg), glisoxepide (0.02 mg/kg) and glibenclamide (0.006 mg/kg). Prior to and 2, 5, 8, 10, 20, 40, 60 and 120 min after the injection the following serum parameters were determined: blood glucose, immunologically measurable insulin (IMI) with the double-antibody method (Hales and Randle) and proinsulin (IMP) enzymatically (ISP-method). The maximum level of insulin follows the injection of tolbutamide with a value of 70.5 micronU/ml after 2 min, of glisoxepide after 5 min (67.0 micronU/ml) and of glibenclamide after 20 min (32.3 micronU/ml). The proinsulin fraction of the total insulin shows a level of 12.5 micronU/ml before the test. After the administration of the three compounds proinsulin increases, too, but reaches only 20-40% of the total immunoreactive insulin. The amount of secreted insulin and proinsulin during the 120-min test is rather the same for the three substances. The average increase of insulin is nearly identical for tolbutamide and glisoxepide, whereas it is less for glibenclamide. Both the mean blood sugar depression and the highest mean increase of proinsulin is reached after glisoxepide. The significance of the one-chain precursor of insulin as a part of the sulfonylurea stimulated total insulin for glucose depression is discussed.
对12名代谢健康的受试者静脉注射等效应剂量（ED30）的甲苯磺丁脲（7.5毫克/千克）、格列波脲（0.02毫克/千克）和格列本脲（0.006毫克/千克）。在注射前以及注射后2、5、8、10、20、40、60和120分钟，测定以下血清参数：血糖、采用双抗体法（黑尔斯和兰德尔法）免疫测定的胰岛素（IMI）以及采用酶法（ISP法）测定的胰岛素原（IMP）。胰岛素的最高水平在注射甲苯磺丁脲后2分钟达到，值为70.5微单位/毫升；注射格列波脲后5分钟达到（67.0微单位/毫升）；注射格列本脲后20分钟达到（32.3微单位/毫升）。胰岛素原占总胰岛素的比例在试验前为12.5微单位/毫升。给予这三种化合物后，胰岛素原也增加，但仅达到总免疫反应性胰岛素的20 - 40%。在120分钟的试验期间，这三种物质分泌的胰岛素和胰岛素原的量相当。甲苯磺丁脲和格列波脲胰岛素的平均增加量几乎相同，而格列本脲的增加量较少。格列波脲注射后血糖平均降低幅度和胰岛素原平均增加幅度均达到最高。文中讨论了胰岛素单链前体作为磺酰脲类刺激的总胰岛素的一部分对血糖降低的意义。
