鼻用原位凝胶给药系统中药物吸收的影响因素与改进措施

Factors affecting drug absorption and improvement measures for nasal in situ gel delivery system

药物的吸收主要是由药物的理化性质、剂型以及给药途径所决定的。原位凝胶是指在生理条件刺激下能发生分散状态或构象的可逆变化、完成溶液与凝胶间相互转变的新剂型。原位凝胶经鼻腔给药,既避免了药物的胃肠首过效应,又因其能延长药物在给药部位滞留时间,从而避免药物被鼻纤毛快速清除。本文通过系统查阅近年国内外鼻用原位凝胶给药系统的相关文献,就鼻腔的生理特点、药物理化性质与原位凝胶的制剂处方等影响其药物吸收的主要因素及改进措施,进行分析、整理和归纳,旨在为鼻用原位凝胶给药系统的设计与质量控制提供参考。

The absorption of drug depends on its physicochemical characterization,dosage forms and the route of administration.In situ gel is a new drug delivery system,in which reversible changes in dispersion or conformation occur under various physiological conditions,and shift of solution and gel with each other is completed.In situ gel for nasal administration avoids both the gastrointestinal first pass effect and the drug quickly clearance because it can prolong the residence time of drug in the administration site.The main influencing factors for physicochemical characterization of drugs,anatomy and physiology characteristics of the nasal cavity and preparation of in situ gel were searched from the literature published in home and abroad in recent years.In this article,we analyzed,arranged and summarized the measures of promoting the drug absorption of intranasal in situ gel to provide references for the preparation of nasal in situ gel delivery system.