Mane Krishnappa, Chaluvaraju Kc, Niranjan Ms, Zaranappa Tr, Manjuthej Tr
Department of Pharmaceutical Chemistry, Government College of Pharmacy, Bangalore - 560 027, India.
J Basic Clin Pharm. 2012 Mar;3(2):283-93. doi: 10.4103/0976-0105.103822. Epub 2012 May 15.
Diabetes is a metabolic disorder where in human body does not produce or properly uses insulin, a hormone that is required to convert sugar, starches and other food into energy. Diabetes finally leads to more complications and to prevent these complications insulin and its analogues are used. After more than half a century of treating diabetics with animal insulin's, recombinant DNA technologies and advanced protein chemistry made human insulin preparations available in the early 1980s. As the next step, over the last decade, insulin analogues were constructed by changing the structure of the native protein with the goal of improving the therapeutic properties of it, because the pharmacokinetic characteristics of rapid, intermediate and long-acting preparations of human insulin make it almost impossible to achieve sustained normoglycemia. The first clinically available insulin analogue, lispro, confirmed the hopes by showing that improved glycaemic control can be achieved without an increase in hypoglycaemic events. Two new insulin analogues, insulin glargine and insulin aspart, have recently been approved for clinical use in the United States and several other analogues are being intensively tested.
糖尿病是一种代谢紊乱疾病，人体无法产生或正常使用胰岛素，而胰岛素是一种将糖、淀粉和其他食物转化为能量所需的激素。糖尿病最终会引发更多并发症，为预防这些并发症，人们会使用胰岛素及其类似物。在用动物胰岛素治疗糖尿病患者半个多世纪后，重组DNA技术和先进的蛋白质化学方法使得人类胰岛素制剂在20世纪80年代初问世。接下来，在过去十年中，人们通过改变天然蛋白质的结构构建胰岛素类似物，目的是改善其治疗特性，因为人胰岛素速效、中效和长效制剂的药代动力学特性几乎无法实现持续的血糖正常。首个临床可用的胰岛素类似物赖脯胰岛素证实了人们的期望，即无需增加低血糖事件就能实现更好的血糖控制。两种新的胰岛素类似物，甘精胰岛素和门冬胰岛素，最近已在美国获批临床使用，其他几种类似物也正在进行深入测试。
