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含硫酸庆大霉素的鼻腔给药黏膜黏附微球:制备与体外特性研究

Mucoadhesive microspheres containing gentamicin sulfate for nasal administration: preparation and in vitro characterization.

作者信息

Hasçiçek Canan, Gönül Nurşin, Erk Nevin

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ankara, Turkey.

出版信息

Farmaco. 2003 Jan;58(1):11-6. doi: 10.1016/S0014-827X(02)00004-6.

Abstract

In this study, suitable microsphere formulations were designed in order to provide the absorption of a high polar drug through nasal mucosa. For this purpose, gentamicin sulfate (GS) was chosen as a model drug and used at different drug/polymer ratios in the microsphere formulations. The microspheres were prepared by spray drying technique. Hydroxypropyl methylcellulose was used as a mucoadhesive polymer in the formulations to increase the residence time of the microspheres on the mucosa. Sodium cholate was added into the formulations for increasing the absorption of GS through nasal mucosa. The in vitro characteristics of the microspheres were determined. The microspheres were evaluated with respect to the particle size, production yield, encapsulation efficiency, shape and surface properties, drug-polymer interaction, mucoadhesive property, in vitro drug release and suitability for nasal drug delivery.

摘要

在本研究中,设计了合适的微球制剂,以便通过鼻黏膜实现高极性药物的吸收。为此,选择硫酸庆大霉素(GS)作为模型药物,并在微球制剂中以不同的药物/聚合物比例使用。微球通过喷雾干燥技术制备。羟丙基甲基纤维素用作制剂中的黏膜黏附聚合物,以增加微球在黏膜上的停留时间。向制剂中加入胆酸钠以增加GS通过鼻黏膜的吸收。测定了微球的体外特性。对微球进行了粒径、产率、包封率、形状和表面性质、药物-聚合物相互作用、黏膜黏附性、体外药物释放以及鼻用药物递送适用性等方面的评估。

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