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用于口腔给药的聚合物薄膜的评估。

Evaluation of polymeric films for buccal drug delivery.

作者信息

Skulason S, Asgeirsdottir M S, Magnusson J P, Kristmundsdottir T

机构信息

Faculty of Pharmaceutical Sciences, University of Iceland, Hagi, Hofsvallagata 53, 107 Reykjavik, Iceland.

出版信息

Pharmazie. 2009 Mar;64(3):197-201.

Abstract

The objective of this study was to evaluate the suitability of the bioadhesive polymers Carbopol 981 NF, Carbopol 1382 and sodium alginate as possible carriers for films for buccal drug delivery. Films were prepared by casting and solvent evaporation method, using propylene glycol as plasticizer and hydoxypropylmethyl cellulose to modify the properties of the films. The bioadhesive and mechanical properties of the films were evaluated with a TA-XT2i Texture Analyser. The alginate films exhibited greater bioadhesion and showed higher tensile strength and elasticity than the Carbopol films. There was a marked difference in the way the polymeric films hydrated in simulated saliva solution. Upon swelling the diameter of the alginate films did not increase but their thickness increases slightly, however the surface area of the Carbopol films increased significantly which points to them being unsuitable for drug delivery to the buccal mucosa. Excessive hydration of a polymeric film for buccal delivery could lead to decreasing adhesive strength and possibly loss of adhesion and hence shorter duration of retention. HPMC appeared to improve the properties of the films, affecting the bioadhesiveness and increasing tensile strength. For the alginate films an increase in HPMC leads to an increase in elasticity but for the Carbopol polymers this was not the case. The release profile of a model drug, sumatriptan succinate, showed that drug release was by diffusion rather than due to disintegration of the films. The results indicate that sodium alginate may be a suitable carrier for polymeric films for use in the buccal cavity.

摘要

本研究的目的是评估生物黏附聚合物卡波姆981 NF、卡波姆1382和海藻酸钠作为口腔给药薄膜可能载体的适用性。采用流延和溶剂蒸发法制备薄膜,使用丙二醇作为增塑剂,羟丙基甲基纤维素来改善薄膜的性能。用TA-XT2i质构分析仪评估薄膜的生物黏附性和机械性能。海藻酸钠薄膜表现出更大的生物黏附性,并且比卡波姆薄膜具有更高的拉伸强度和弹性。聚合物薄膜在模拟唾液溶液中的水化方式存在显著差异。海藻酸钠薄膜溶胀时直径没有增加,但厚度略有增加,然而卡波姆薄膜的表面积显著增加,这表明它们不适用于口腔黏膜给药。用于口腔给药的聚合物薄膜过度水化可能导致黏附强度降低,甚至可能失去黏附性,从而缩短滞留时间。羟丙基甲基纤维素似乎改善了薄膜的性能,影响了生物黏附性并提高了拉伸强度。对于海藻酸钠薄膜,羟丙基甲基纤维素的增加会导致弹性增加,但对于卡波姆聚合物则并非如此。模型药物琥珀酸舒马曲坦的释放曲线表明,药物释放是通过扩散而不是由于薄膜的崩解。结果表明,海藻酸钠可能是用于口腔的聚合物薄膜的合适载体。

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