Shanghai Clinical Center for Endocrine and Metabolic Diseases, Rui-Jin Hospital affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, People's Republic of China.
Endocrine. 2010 Aug;38(1):48-52. doi: 10.1007/s12020-010-9326-4. Epub 2010 May 1.
Intensive insulin therapy for diabetic patients has been demonstrated as an appropriate treatment. Regular fast-acting insulin can hardly mimic the efficiency of endogenous meal-activated insulin secretion. Glulisine is a new rapid-acting insulin analog for mealtime insulin supplementation. We compared the pharmacokinetics and pharmacodynamics end points between the two rapid-acting insulin analogs Glulisine and Lispro. Twenty healthy adult males age ranging from 22 to 32 years were included in a randomized, open-label, cross contrast research. Two long duration hyperinsulinemic euglycemic clamp tests, one with Glulisine and the other with Lispro, were conducted on two separate days for all the participants. The two rapid-acting insulin analogs were administrated randomly to each participant. Glucose infusion rate (GIR) began to increase 20 min after injection in both Glulisine and Lispro groups. GIR increased sharply during the first 150 min and reached a peak at 6.23 ± 1.35 mg/(kg min) in the Glulisine group and 6.02 ± 1.27 mg/(kg min) in the Lispro group. It returned to the initial level at hour 5. The Area Under Curve (AUC(0-clamp end)) in Glulisine and Lispro groups were 1455.04 ± 381.88 mg/kg and 1356.25 ± 287.30 mg/kg (P > 0.05), respectively. However, AUC(0-1h) between the two groups showed significant difference, with Glulisine showed greater AUC(0-1h) in the first hour after injection. Other parameters showed no significant difference between the two groups. Insulin analogs Glulisine and Lispro were proved to have equivalent pharmacokinetic and pharmacodynamic parameters when administered to healthy Chinese adults, but with Glulisine showing greater AUC(0-1h) after injection.
强化胰岛素治疗已被证明是糖尿病患者的一种合适的治疗方法。常规速效胰岛素几乎无法模拟内源性餐时胰岛素分泌的效率。赖脯胰岛素是一种新型速效胰岛素类似物，可用于餐时胰岛素补充。我们比较了两种速效胰岛素类似物赖脯胰岛素和谷赖胰岛素的药代动力学和药效学终点。20 名年龄在 22 岁至 32 岁之间的健康成年男性被纳入一项随机、开放标签、交叉对照研究。所有参与者在两天内分别进行了两次长时间的高胰岛素-正常血糖钳夹试验，一次使用谷赖胰岛素，另一次使用赖脯胰岛素。两种速效胰岛素类似物随机分配给每个参与者。谷赖胰岛素和赖脯胰岛素组分别在注射后 20 分钟开始增加葡萄糖输注率（GIR）。GIR 在最初 150 分钟内急剧增加，在谷赖胰岛素组达到 6.23±1.35mg/（kg·min）的峰值，在赖脯胰岛素组达到 6.02±1.27mg/（kg·min）的峰值。在 5 小时时恢复到初始水平。谷赖胰岛素和赖脯胰岛素组的 AUC（0-钳夹结束）分别为 1455.04±381.88mg/kg 和 1356.25±287.30mg/kg（P>0.05）。然而，两组之间的 AUC（0-1h）差异显著，谷赖胰岛素在注射后 1 小时内显示出更大的 AUC（0-1h）。其他参数在两组之间没有显著差异。当给予健康中国成年人时，胰岛素类似物谷赖胰岛素和赖脯胰岛素被证明具有等效的药代动力学和药效学参数，但谷赖胰岛素在注射后显示出更大的 AUC（0-1h）。
