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用于胰岛素口腔给药的生物粘附性聚合物纳米粒:制备与表征

Pelleted bioadhesive polymeric nanoparticles for buccal delivery of insulin: preparation and characterization.

作者信息

Venugopalan P, Sapre A, Venkatesan N, Vyas S P

机构信息

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Doctor Harisingh Gour Vishwavidyalaya, Sagar, India.

出版信息

Pharmazie. 2001 Mar;56(3):217-9.

Abstract

The study was an attempt to develop an alternative buccal delivery system for insulin. Insulin bearing nanoparticles were prepared by the emulsion internal phase evaporation method. The effect of some formulation variables viz., polymer/drug ratio and emulsifier concentration was studied on particle size and entrapment efficiency. Nanoparticles were pelleted to impart three-dimensional structural conformity and coherence thereby facilitating buccal application. Solid lateral and horizontal sedimentaton in the pellet can be avoided by nanoparticulation and ensuring uniform drug distribution throughout the pellet. The in vitro studies of the pellets included bioadhesion and drug release profile. In vivo studies were performed on diabetic rats. A significant hypoglycemic response was observed after 7 h, without any detectable fluctuation in blood glucose profile and risk of hypoglycemia.

摘要

该研究旨在开发一种用于胰岛素的替代性口腔给药系统。通过乳液内相蒸发法制备了载胰岛素纳米颗粒。研究了一些制剂变量,即聚合物/药物比例和乳化剂浓度对粒径和包封率的影响。将纳米颗粒制成丸剂以赋予三维结构的一致性和连贯性,从而便于口腔给药。通过纳米粒化并确保药物在整个丸剂中均匀分布,可以避免丸剂中出现固体横向和水平沉降。丸剂的体外研究包括生物黏附性和药物释放曲线。在糖尿病大鼠上进行了体内研究。7小时后观察到显著的降血糖反应,血糖曲线无任何可检测到的波动,也无低血糖风险。

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