Binder C, Lauritzen T, Faber O, Pramming S
Diabetes Care. 1984 Mar-Apr;7(2):188-99. doi: 10.2337/diacare.7.2.188.
Where adjustments of diet, physical activity, and dosage of insulin are well known to diabetologists and diabetic patients, present-day knowledge of factors of importance to the pharmacokinetics of insulin is frequently ignored. The pharmacokinetics of insulin comprise the absorption process, the distribution including binding to circulating insulin antibodies, if present, and to insulin receptors, and its ultimate degradation and excretion. The distribution and metabolism of absorbed insulin follow that of endogenous insulin. The distribution and metabolism cannot be actively changed, except in the case of circulating insulin antibodies, which in rare cases also may cause insulin resistance. The use of insulin preparation of low immunogeneity will avoid or reduce this course of variation in action. The absorption process, the detailed mechanisms of which are still unknown, is influenced by many variables where some can be controlled, thereby reducing the intrapatient variability in insulin absorption, which may reach 35%, causing a corresponding metabolic lability. Besides the known differences in timing among different preparations, the size of dose, the injected volume, and the insulin concentration are determinants of absorption role. Fortuitous injection technique contributes to variance, as do changes in blood flow of the injected tissue. This may be induced by changes in ambient temperature, exercise of injected limb, or local massage. Regional differences are also due to differences in blood flow. Serum insulin peaks may peak up to 1 h after injection of soluble insulin into the thigh versus into the abdominal wall. Local degradation of insulin seems of less importance but may, in rare cases, be the cause of high insulin "requirements." Available evidence is reviewed and the importance of implementing the consequences in the daily care of the insulin-treated patient is emphasized.
虽然饮食调整、体育活动和胰岛素剂量调整对于糖尿病专家和糖尿病患者来说已是熟知的内容，但如今人们对胰岛素药代动力学重要影响因素的认识却常常被忽视。胰岛素的药代动力学包括吸收过程、分布（包括与循环中的胰岛素抗体结合，若存在的话，以及与胰岛素受体结合）及其最终的降解和排泄。吸收后的胰岛素的分布和代谢与内源性胰岛素相同。除了循环中的胰岛素抗体这种罕见情况（其也可能导致胰岛素抵抗）外，分布和代谢无法主动改变。使用低免疫原性的胰岛素制剂将避免或减少这种作用变化过程。吸收过程的详细机制仍然未知，它受许多变量影响，其中一些变量可以控制，从而减少患者体内胰岛素吸收的变异性，这种变异性可能达到35%，导致相应的代谢不稳定。除了不同制剂在时间上的已知差异外，剂量大小、注射体积和胰岛素浓度是吸收作用的决定因素。偶然的注射技术以及注射组织血流的变化也会导致差异。这可能由环境温度变化、注射肢体运动或局部按摩引起。区域差异也归因于血流差异。将可溶性胰岛素注射到大腿与注射到腹壁相比，血清胰岛素峰值可能在注射后1小时达到高峰。胰岛素的局部降解似乎不太重要，但在罕见情况下可能是胰岛素“需求量”高的原因。本文回顾了现有证据，并强调了将这些结果应用于胰岛素治疗患者日常护理中的重要性。
