胰岛素类似物——Aspart30

Insulin analogous——Aspart 30

未修饰的人胰岛素分子之间由于自我联合形成六聚体,导致胰岛素从皮下注射部位吸收进入血循环的时间延迟。速效胰岛素类似物Aspart,因其β链的28位上的氨基酸被天门冬氨酸所取代,至使胰岛素分子彼此排斥,而降低了胰岛素分子的耦联生成6聚体,从而使之经皮快速吸收。Aspart30是由30%可溶性门冬氨酸胰岛素和70%鱼精蛋白结晶体门冬氨酸胰岛素组成。因此本文对Aspart30药代动力学及临床研究做一综述。

The major factor that determines the onset and duration of insulin action is the absorption rate from the subcutaneous insulin depot. At high concentrations, human insulin exists mainly in the hexameric form. The dissociation from hexamers to dimers and monomers is required before absorption into the blood occurs. Thus, the absorption rate is inversely correlated to the selfassociation of insulin molecules to hexamers . The human insulin analog insulin aspart, produced by substituting the aspartic acid for the prolin amino acid sequence at the 28 position of the human insulin β-chain, dissociates more rapidly to monomers and dimers at physiological concentration . Thus, insulin aspart exhibits more rapid absorption in both healthy and diabetic subjects. Biphasic insulin aspart 30 is a premixed formulation containing 30% free insulin aspart(IAsp) and 70% protamine - bound IAsp.In this paper, the pharmacokinetics and clinical trial of the Aspart 30 were summarized.