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口服胰岛素递药系统:障碍、策略及制剂方法:全面综述。

Oral insulin delivery: Barriers, strategies, and formulation approaches: A comprehensive review.

机构信息

Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru 570015, Karnataka, India.

Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru 570015, Karnataka, India.

出版信息

Int J Biol Macromol. 2023 Jul 1;242(Pt 3):125114. doi: 10.1016/j.ijbiomac.2023.125114. Epub 2023 May 31.

DOI:10.1016/j.ijbiomac.2023.125114
PMID:37263330
Abstract

Diabetes Mellitus is characterized by a hyperglycemic condition which can either be caused by the destruction of the beta cells or by the resistance developed against insulin in the cells. Insulin is a peptide hormone that regulates the metabolism of carbohydrates, proteins, and fats. Type 1 Diabetes Mellitus needs the use of Insulin for efficient management. However invasive methods of administration may lead to reduced adherence by the patients. Hence there is a need for a non-invasive method of administration. Oral Insulin has several merits over the conventional method including patient compliance, and reduced cost, and it also mimics endogenous insulin and hence reaches the liver by the portal vein at a higher concentration and thereby showing improved efficiency. However oral Insulin must pass through several barriers in the gastrointestinal tract. Some strategies that could be utilized to bypass these barriers include the use of permeation enhancers, absorption enhancers, use of suitable polymers, use of suitable carriers, and other agents. Several formulation types have been explored for the oral delivery of Insulin like hydrogels, capsules, tablets, and patches which have been described briefly by the article. A lot of attempts have been made for developing oral insulin delivery however none of them have been commercialized due to numerous shortcomings. Currently, there are several formulations from the companies that are still in the clinical phase, the success or failure of some is yet to be seen in the future.

摘要

糖尿病的特征是高血糖状态,这可能是由于β细胞的破坏,也可能是由于细胞对胰岛素的抵抗引起的。胰岛素是一种调节碳水化合物、蛋白质和脂肪代谢的肽类激素。1 型糖尿病需要使用胰岛素进行有效管理。然而,侵入性的给药方法可能会导致患者的依从性降低。因此,需要一种非侵入性的给药方法。口服胰岛素相对于传统方法具有许多优点,包括患者依从性、降低成本,并且它还模拟内源性胰岛素,因此通过门静脉以更高的浓度到达肝脏,从而显示出更高的效率。然而,口服胰岛素必须通过胃肠道中的几个屏障。为了绕过这些屏障,可以使用渗透增强剂、吸收增强剂、合适的聚合物、合适的载体和其他制剂。已经探索了几种用于口服递送胰岛素的制剂类型,如凝胶、胶囊、片剂和贴剂,本文对此进行了简要描述。尽管已经进行了许多尝试来开发口服胰岛素递送,但由于存在许多缺点,目前还没有一种商业化。目前,一些公司的几种制剂仍处于临床阶段,未来的成败仍有待观察。

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