Guzmán A, García R
School of Pharmacy, Medical Sciences Campus, San Juan, PR 00936.
P R Health Sci J. 1990 Aug;9(2):155-9.
Insulin degradation and inactivation occurs when the protein is given to an animal through oral route. The following compounds were assessed to determine their potential effect in increasing insulin absorption: polyoxyethylene (20) oleyl ether (Brij 99), polyoxyethylene lauryl ether and polyoxyethylene (20) cetyl ether (Brij 58). In this study the above compounds, along with stearic acid, were used to prepare granules with or without addition of insulin and were given orally to rabbits. Both glucose and insulin levels in blood were measured at different time intervals, the former with a glucometer and the latter using radioimmunoassay (RIA). To determine if there was a relationship between the glucose and the insulin levels in blood, a highly sensitive radioimmunoassay method was used to detect any small changes in the level of insulin in blood. A significant decrease in glucose blood levels (P less than 0.05) was obtained after oral administration of each of granules containing insulin. The greatest reduction was observed after half an hour of the oral administration of the granules. A similar response was obtained with the hypodermal injection of 1/5 of the oral insulin dose. Granules prepared with Brij 58 and containing insulin was the only formula that showed increase of insulin level in the blood. This was equivalent to 1/10 of the change produced after hypodermal injection of the hormone. In these experiments the changes in blood insulin levels were not directly proportional to the corresponding changes in blood glucose.
当通过口服途径将胰岛素给予动物时,会发生胰岛素降解和失活。评估了以下化合物以确定它们在增加胰岛素吸收方面的潜在作用:聚氧乙烯(20)油基醚(Brij 99)、聚氧乙烯月桂醚和聚氧乙烯(20)十六烷基醚(Brij 58)。在本研究中,上述化合物与硬脂酸一起用于制备添加或不添加胰岛素的颗粒,并口服给予兔子。在不同时间间隔测量血液中的葡萄糖和胰岛素水平,前者使用血糖仪测量,后者使用放射免疫测定法(RIA)。为了确定血液中葡萄糖和胰岛素水平之间是否存在关系,使用高度敏感的放射免疫测定法检测血液中胰岛素水平的任何微小变化。口服每种含胰岛素的颗粒后,血糖水平显著降低(P小于0.05)。口服颗粒半小时后观察到最大降幅。皮下注射口服胰岛素剂量的1/5也获得了类似的反应。用Brij 58制备并含有胰岛素的颗粒是唯一显示血液中胰岛素水平升高的配方。这相当于皮下注射该激素后产生变化的1/10。在这些实验中,血液胰岛素水平的变化与血糖的相应变化并不直接成比例。