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用于尼古丁缓释的口腔黏附片中所选多糖辅料的评价。

Evaluation of selected polysaccharide excipients in buccoadhesive tablets for sustained release of nicotine.

作者信息

Park Calum R, Munday Dale L

机构信息

School of Pharmacy, The Robert Gordon University, Aberdeen, Scotland, UK.

出版信息

Drug Dev Ind Pharm. 2004 Jul;30(6):609-17. doi: 10.1081/ddc-120037492.

Abstract

Some naturally occurring biocompatible materials were evaluated as mucoadhesive controlled release excipients for buccal drug delivery. A range of tablets were prepared containing 0-50% w/w xanthan gum, karaya gum, guar gum, and glycol chitosan and were tested for swelling, drug release, and mucoadhesion. Guar gum was a poor mucoadhesive and lacked sufficient physical integrity for buccal delivery. Karaya gum demonstrated superior adhesion to guar gum and was able to provide zero-order drug release, but concentrations greater than 50% w/w may be required to provide suitable sustained release. Xanthan gum showed strong adhesion to the mucosal membrane and the 50% w/w formulation produced zero-order drug release over 4 hours, about the normal time interval between daily meals. Glycol chitosan produced the strongest adhesion, but concentrations greater than 50% w/w are required to produce a nonerodible matrix that can control drug release for over 4 hours. Swelling properties of the tablets were found to be a valuable indicator of the ability of the material to produce sustained release. Swelling studies also gave an indication of the adhesion values of the gum material where adhesion was solely dependent upon penetration of the polymer chains into the mucus layer.

摘要

一些天然存在的生物相容性材料被评估为用于口腔给药的粘膜粘附控释辅料。制备了一系列含有0-50%(w/w)黄原胶、刺梧桐树胶、瓜尔胶和乙二醇壳聚糖的片剂,并对其溶胀、药物释放和粘膜粘附性能进行了测试。瓜尔胶是一种较差的粘膜粘附剂,缺乏足够的物理完整性用于口腔给药。刺梧桐树胶表现出比瓜尔胶更好的粘附性,并且能够实现零级药物释放,但可能需要大于50%(w/w)的浓度才能提供合适的缓释效果。黄原胶对粘膜膜表现出强烈的粘附性,50%(w/w)的制剂在4小时内实现了零级药物释放,大约是每日进餐之间的正常时间间隔。乙二醇壳聚糖产生了最强的粘附性,但需要大于50%(w/w)的浓度才能产生一种可控制药物释放超过4小时的不可侵蚀基质。片剂的溶胀性能被发现是该材料产生缓释能力的一个有价值的指标。溶胀研究还给出了胶材料粘附值的指示,其中粘附仅取决于聚合物链渗透到粘液层中。

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