Insititut d'Investigacions Biomèdiques August Pi i Sunyer, Calle Mallorca 183, Piso P01, 08036 Barcelona, Spain.
Expert Opin Pharmacother. 2012 Feb;13(2):255-81. doi: 10.1517/14656566.2012.650862. Epub 2012 Jan 13.
Insulin lispro protamine suspension (ILPS) is a protamine-based insulin lispro formulation that allows 24-h coverage while limiting the number of daily injections. ILPS was developed to be the basal insulin component of premixed biphasic formulations with insulin lispro, i.e., the lispro/ILPS 25/75 and 50/50 mixed compounds, but has recently also been marketed as a basal insulin analog formulation, with an indication for the therapy of diabetic patients.
This article reviews the available literature on pharmacokinetics/pharmacodynamics (PK/PD), efficacy and safety of ILPS administered as basal insulin, or in premixed biphasic formulations, in patients with type 1 and type 2 diabetes mellitus.
The results of this review suggest that ILPS may be associated with a favorable time-action profile, basal and postprandial glycemic control, and efficacy in terms of rates of patients reaching glycosylated hemoglobin targets; an increased risk of hypoglycemic episodes, compared to other basal insulins, seems to be related to the percentage of patients upgrading from once- to twice-daily injections. This increased risk might be linked with the concomitant use of insulin secretagogues in patients on higher daily dosages and is generally not observed in patients using one injection of ILPS a day. Thus, ILPS can be considered a valid option both as basal insulin and as basal component of the actual premixed formulations of lispro for the therapy of diabetic patients.
胰岛素赖脯氨酸鱼精蛋白混悬液(ILPS)是一种基于鱼精蛋白的胰岛素赖脯氨酸制剂,可提供 24 小时覆盖,同时限制每日注射次数。ILPS 的开发目的是作为含有胰岛素赖脯氨酸的预混双相制剂(即赖脯肽/ILPS 25/75 和 50/50 混合化合物)的基础胰岛素成分,但最近也被作为基础胰岛素类似物制剂上市,用于治疗糖尿病患者。
本文综述了关于作为基础胰岛素或在预混双相制剂中给药的 ILPS 的药代动力学/药效学(PK/PD)、疗效和安全性的现有文献,适用于 1 型和 2 型糖尿病患者。
这篇综述的结果表明,与其他基础胰岛素相比,ILPS 可能与有利的时间作用曲线、基础和餐后血糖控制以及达到糖化血红蛋白目标的患者比例有关;与其他基础胰岛素相比,低血糖发作的风险似乎增加,这与从每日一次注射升级为每日两次注射的患者比例有关。这种风险增加可能与同时使用胰岛素促分泌剂有关,在使用更高每日剂量的患者中更为常见,而在每天使用一次 ILPS 的患者中通常不会观察到。因此,ILPS 可被视为治疗糖尿病患者的基础胰岛素和实际赖脯肽预混制剂的基础成分的有效选择。