Profil Institut für Stoffwechselforschung GmbH, Neuss, Germany.
Diabetes Care. 2010 Jun;33(6):1288-90. doi: 10.2337/dc09-1807. Epub 2010 Feb 25.
To determine the pharmacokinetic and pharmacodynamic properties of an oral insulin (OI) formulation compared with subcutaneously injected regular human insulin (RHI).
Ten male patients with type 2 diabetes (means +/- SD; A1C 7.0 +/- 1.1%; BMI 28.3 +/- 2.7 kg/m(2)) received either 300 units of insulin combined with 400 mg of delivery agent orally or 15 units RHI subcutaneously under isoglycemic clamp conditions.
Maximum insulin concentration was greater and onset of action was faster with OI (C(max) 93 +/- 71 vs. 33 +/- 11 microU/ml; AUC(GIR)((0-1h)) 173 +/- 86 vs. 27 +/- 32 mg/kg; P < 0.05). Mean insulin concentration and glucose infusion rate returned to baseline within 3 h after OI administration. Relative bioavailability of OI was 7 +/- 4% (1st 2 h).
This proof-of-concept study demonstrated that absorption of OI is feasible under fasting conditions. OI has a fast onset and a short duration of action but also shows a rather high between-subject variability in absorption.
比较口服胰岛素（OI）制剂与皮下注射常规人胰岛素（RHI）的药代动力学和药效学特性。
10 名 2 型糖尿病男性患者（平均值 +/- 标准差；A1C 7.0 +/- 1.1%；BMI 28.3 +/- 2.7 kg/m2）分别接受 300 单位胰岛素和 400 毫克递送剂口服或 15 单位 RHI 皮下注射，在等血糖钳夹条件下进行。
OI 的最大胰岛素浓度更高，作用更快（C(max) 93 +/- 71 与 33 +/- 11 microU/ml；AUC(GIR)((0-1h)) 173 +/- 86 与 27 +/- 32 mg/kg；P < 0.05）。OI 给药后 3 小时内，平均胰岛素浓度和葡萄糖输注率恢复至基线。OI 的相对生物利用度为 7 +/- 4%（前 2 小时）。
这项概念验证研究表明，在禁食条件下 OI 的吸收是可行的。OI 具有快速的作用开始和短的作用持续时间，但在吸收方面也表现出相当高的个体间变异性。
Zotero 插件