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胰岛素给药:非侵入性(可能更符合生理状态)给药的当前策略与未来方向

Insulin administration: present strategies and future directions for a noninvasive (possibly more physiological) delivery.

作者信息

Matteucci Elena, Giampietro Ottavio, Covolan Vera, Giustarini Daniela, Fanti Paolo, Rossi Ranieri

机构信息

Department of Clinical and Experimental Medicine, University of Pisa, Siena, Italy.

Department of Chemistry and Industrial Chemistry, University of Pisa, Siena, Italy.

出版信息

Drug Des Devel Ther. 2015 Jun 17;9:3109-18. doi: 10.2147/DDDT.S79322. eCollection 2015.

Abstract

Insulin is a life-saving medication for people with type 1 diabetes, but traditional insulin replacement therapy is based on multiple daily subcutaneous injections or continuous subcutaneous pump-regulated infusion. Nonphysiologic delivery of subcutaneous insulin implies a rapid and sustained increase in systemic insulin levels due to the loss of concentration gradient between portal and systemic circulations. In fact, the liver degrades about half of the endogenous insulin secreted by the pancreas into the venous portal system. The reverse insulin distribution has short- and long-term effects on glucose metabolism. Thus, researchers have explored less-invasive administration routes based on innovative pharmaceutical formulations, which preserve hormone stability and ensure the therapeutic effectiveness. This review examines some of the recent proposals from clinical and material chemistry point of view, giving particular attention to patients' (and diabetologists') ideal requirements that organic chemistry could meet.

摘要

胰岛素是1型糖尿病患者的救命药物,但传统的胰岛素替代疗法基于每日多次皮下注射或持续皮下泵调节输注。皮下胰岛素的非生理性给药意味着由于门静脉和体循环之间浓度梯度的丧失,全身胰岛素水平会迅速且持续升高。事实上,肝脏会将胰腺分泌到门静脉系统的约一半内源性胰岛素降解。胰岛素逆向分布对葡萄糖代谢有短期和长期影响。因此,研究人员基于创新的药物制剂探索了侵入性较小的给药途径,这些制剂可保持激素稳定性并确保治疗效果。本综述从临床和材料化学的角度审视了一些近期的提议,特别关注有机化学能够满足的患者(以及糖尿病专家)的理想需求。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4f3/4476457/dc5809de9e69/dddt-9-3109Fig1.jpg

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