中间作用胰岛素类似物des(64,65)-人胰岛素原的时间作用谱。

Diabete & metabolisme Pub Date : 1995-12-01
L Heinemann, T Heise, A Klepper, J Ampudia, R Bender, A A Starke
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引用次数: 0

摘要

Des(64,65)-胰岛素原(DPRO)是胰岛素原转化为胰岛素过程中产生的几种内源性中间体之一。在药物制剂中,它是一种不含其他蛋白质的透明溶液。动物实验和初步的人体研究表明,DPRO应该具有与nph -胰岛素相似的持久的时间作用谱。因此,我们在9名健康男性志愿者中使用血糖钳技术比较了这两种制剂的时间作用谱。腹腔皮下注射不同剂量的DPRO(0.1、0.15、0.2 U/kg)或等效剂量的NPH(0.2、0.3、0.4 U/kg)。DPRO的最大代谢效应(GIRmax)大于nph -胰岛素(p < 0.05)。随着剂量的增加,DPRO的GIRmax差异显著,而nph -胰岛素的GIRmax差异不显著。达到最大代谢效应的时间(tmax)对于任何一种制剂的三个剂量是相似的。DPRO组tmax比nph -胰岛素组早30 min达到(p < 0.01)。与nph -胰岛素组相比,DPRO组在最大活动后降至半最大活动的速度明显快于nph -胰岛素组(p < 0.0001)。因此,皮下注射DPRO产生了介于普通胰岛素和nph -胰岛素之间的时间作用谱。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Time-action profiles of the intermediate-acting insulin analogue des(64,65)-human proinsulin.

Des(64,65)-proinsulin (DPRO) is one of several endogenous intermediates arising during the conversion of proinsulin to insulin. In pharmaceutic preparations it is a clear solution containing no other proteins. Animal experiments and preliminary human studies indicated that DPRO should have a protracted time-action profile similar to that of NPH-insulin. Accordingly, we compared the time-action profiles of these two preparations, using the euglycaemic glucose clamp-technique in 9 healthy male volunteers. Different doses of DPRO (0.1, 0.15, 0.2 U/kg) or equipotent doses of NPH ( 0.2, 0.3, 0.4 U/kg) were injected subcutaneously into the abdominal wall. The maximal metabolic effect (GIRmax) of DPRO was greater than that of NPH-insulin (p < 0.05). With increasing doses, GIRmax differed significantly for DPRO but not for NPH-insulin. The time to maximal metabolic effect (tmax) was similar for the three doses of either preparation. However, tmax was reached 30 min earlier with DPRO than with NPH-insulin (p < 0.01). the decline to half-maximal after maximal activity was significantly faster with DPRO than with NPH-insulin (p < 0.0001). Subcutaneous injection of DPRO thus produced a time-action profile between that of regular insulin and NPH-insulin.

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