MKC253 is glucagon-like peptide 1 (GLP-1, 7-36 amide) adsorbed onto Technosphere microparticles for oral inhalation. The pharmacokinetics of inhaled GLP-1 and the pharmacokinetic-pharmacodynamic (PK-PD) relationship between inhaled GLP-1 and insulin were analyzed in two trials, one in healthy normal volunteers and the other in patients with type 2 diabetes. Inhaled GLP-1 was absorbed quickly, with peak concentrations occurring within 5 min, and levels returned to baseline within 30 min. Inhaled GLP-1 appeared to produce plasma levels of GLP-1 comparable to those of parenteral administration and sufficient to induce insulin secretion resulting in attenuation of postmeal glucose excursions in subjects with type 2 diabetes. An E(max) (maximum effect) model described the relationship between GLP-1 concentration and insulin release. The variability in the E(max) may be due to differences in baseline glucose levels, differences resulting from genetic polymorphisms in GLP-1 receptors (GLP-1Rs), or the stage of diabetes of the patient.

译文

:MKC253是胰高血糖素样肽1(GLP-1,7-36酰胺),吸附在Technosphere微粒上,可以口服吸入。在两项试验中分析了吸入GLP-1的药代动力学以及吸入GLP-1和胰岛素之间的药代动力学-药效学(PK-PD)关系,一项是健康正常志愿者,另一项是2型糖尿病患者。吸入的GLP-1很快被吸收,在5分钟内达到峰值浓度,并在30分钟内恢复到基线水平。吸入的GLP-1似乎产生与胃肠外给药相当的GLP-1血浆水平,并且足以诱导胰岛素分泌,从而导致2型糖尿病患者餐后葡萄糖偏移减少。 E(max)(最大作用)模型描述了GLP-1浓度与胰岛素释放之间的关系。 E(max)的可变性可能是由于基线葡萄糖水平的差异,GLP-1受体(GLP-1Rs)的遗传多态性导致的差异或患者的糖尿病分期所致。

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