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新型中效胰岛素L-SNC的药代动力学及生物学活性

Pharmacokinetics and biological activity of the new intermediate-acting insulin L-SNC).

作者信息

Schulz B, Menzel R, Ratzmann K P, Heinke P

机构信息

Central Institute of Diabetes Gerhardt Katsch, I. Clinical Department, Karlsburg/GDR.

出版信息

Exp Clin Endocrinol. 1987 Dec;90(3):278-84. doi: 10.1055/s-0029-1210702.

Abstract

To assess pharmacokinetics and biological activity of the new L-SNC insulin (Berlin-Chemie, a low immunogenic pork insulin in neutral solution purified by chromatography) ten healthy male subjects were connected to the BIOSTATOR. After an overnight fast 0.4 U of L-SNC insulin per kg body weight were injected subcutaneously in the thigh of each individual. Plasma insulin concentrations rose gradually reaching their maximum values after 8 hours. According to C-peptide levels there was some inhibition of endogenous insulin secretion. For the evaluation of insulin action we used the closed loop system (BIOSTATOR) which was transformed in its function into a glucose controlled dextrose infusion system. The amount of glucose delivered by the BIOSTATOR in order to maintain blood glucose steady state concentrations at the "basal" level was taken as a measure of biological activity of the injected insulin. The glucose infusion rate increased after insulin administration, reaching statistical significance after 3 hr. The maximum effect of L-SNC insulin was observed between 5 and 12 hours after injection. The overall duration of action of more than 16 hours meets the increasing need for insulin in the early morning in many diabetic patients. Therefore, L-SNC insulin should be recommended for intensified conventional insulin therapy to cover the night and to prevent dawn phenomenon in insulin dependent diabetics.

摘要

为评估新型L-SNC胰岛素(柏林化学公司生产,一种经色谱法纯化的中性溶液中低免疫原性猪胰岛素)的药代动力学和生物活性,将10名健康男性受试者连接至生物人工肝支持系统(BIOSTATOR)。在禁食过夜后,给每位受试者的大腿皮下注射每千克体重0.4单位的L-SNC胰岛素。血浆胰岛素浓度逐渐升高,8小时后达到最大值。根据C肽水平,内源性胰岛素分泌受到一定抑制。为评估胰岛素作用,我们使用了闭环系统(BIOSTATOR),该系统在功能上转变为葡萄糖控制的葡萄糖输注系统。将生物人工肝支持系统为维持血糖稳态浓度在“基础”水平而输送的葡萄糖量作为注射胰岛素生物活性的指标。胰岛素给药后葡萄糖输注速率增加,3小时后达到统计学意义。L-SNC胰岛素的最大作用在注射后5至12小时观察到。超过16小时的总体作用持续时间满足了许多糖尿病患者清晨对胰岛素日益增加的需求。因此,对于胰岛素依赖型糖尿病患者的强化常规胰岛素治疗,应推荐使用L-SNC胰岛素以覆盖夜间并预防黎明现象。

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