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基于果胶的生物黏附性递送卡波氯铵钠治疗口腔阿弗他溃疡。

Pectin-based bioadhesive delivery of carbenoxolone sodium for aphthous ulcers in oral cavity.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand.

出版信息

AAPS PharmSciTech. 2010 Jun;11(2):743-51. doi: 10.1208/s12249-010-9424-x. Epub 2010 May 5.

Abstract

The objective of this study was to prepare and evaluate the pectin-based dosage form for buccal adhesion. Carbenoxolone sodium, which is used for the treatment of aphthous ulcers in oral cavity, was used as a model drug. The pectin buccal discs were prepared by direct compression. The water uptake and erosion of pectin disc increased progressively with the swelling time. The bioadhesion of dried pectin discs decreased when either the discs were hydrated or the buccal tissue was wet with a small volume of medium. The influencing factors such as pectin type, pectin to lactose ratio, and sweetener type on the formulations were investigated. The results demonstrated that buccal discs prepared from pectin with a high degree of esterification (DE) showed a weaker and more friable characteristic than that with low DE. Decreasing pectin to lactose ratio resulted in the high dissolution rate with low bioadhesive properties. Addition of sweetener in the formulations also affected the hardness, friability, and bioadhesive properties of the discs. The pectin discs containing sweetening agent showed a higher drug release than those without sweetener. The results suggested that pectin-based bioadhesive discs could be used to deliver carbenoxolone sodium in oral cavity.

摘要

本研究旨在制备和评价基于果胶的口腔黏附制剂。我们选用卡波氯铵钠作为模型药物,该药物用于治疗口腔阿弗他溃疡。采用直接压缩法制备果胶口腔黏附片。随着溶胀时间的延长,果胶片的吸水率和侵蚀率逐渐增加。当干燥的果胶片水化或用少量介质润湿口腔组织时,其生物黏附性会降低。考察了果胶类型、果胶与乳糖的比例以及甜味剂类型等因素对制剂的影响。结果表明,酯化度(DE)较高的果胶制备的黏附片比 DE 较低的果胶制备的黏附片具有较弱且更易碎的特性。降低果胶与乳糖的比例会导致高溶解速率和低生物黏附性能。制剂中添加甜味剂也会影响黏附片的硬度、脆性和生物黏附性能。含有甜味剂的果胶黏附片的药物释放率高于不含甜味剂的果胶黏附片。结果表明,基于果胶的生物黏附片可用于口腔递送卡波氯铵钠。

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