Kelly H M, Deasy P B, Busquet M, Torrance A A
School of Pharmacy, Trinity College, University of Dublin, Ireland.
Int J Pharm. 2004 Jul 8;278(2):391-406. doi: 10.1016/j.ijpharm.2004.03.022.
Xerostomia is commonly known as 'dry mouth' and is characterised by a reduction or loss in salivary production. A bioadhesive gel for its localised treatment was formulated to help enhance the residence time of the product, based on the polymer Carbopol 974P. The bioadhesion of various formulations was evaluated on different mucosal substrates, as simulations of the oral mucosa of xerostomic patients. Depending on the type of model substrate used, the mechanism of bioadhesion could alter. When the rheology of various formulations was examined, changes in bioadhesion were more easily interpreted, as the presence of other excipients caused an alteration in the rheological profile, with a change from a fully expanded and partially cross-linked system to an entangled system. Improving the lubricity of the product was considered important, with optimum incorporation of vegetable oil causing a desirable lowering of the observed friction of the product. The final complex formulation developed also contained salivary levels of electrolytes to help remineralisation of teeth, fluoride to prevent caries, zinc to enhance taste sensation, triclosan as the main anti-microbial/anti-inflammatory agent and non-cariogenic sweeteners with lemon flavour to increase the palatability of the product while stimulating any residual salivary function.
口干症通常被称为“口腔干燥”，其特征是唾液分泌减少或丧失。基于卡波姆974P聚合物，制备了一种用于局部治疗的生物粘附凝胶，以帮助延长产品的停留时间。在不同的粘膜底物上评估了各种制剂的生物粘附性，作为口干症患者口腔粘膜的模拟。根据所用模型底物的类型，生物粘附机制可能会改变。当检查各种制剂的流变学时，生物粘附的变化更容易解释，因为其他辅料的存在导致流变学特征发生改变，从完全膨胀和部分交联的系统转变为缠结系统。提高产品的润滑性被认为很重要，植物油的最佳掺入导致产品观察到的摩擦力降低。最终开发的复合制剂还含有唾液水平的电解质以帮助牙齿再矿化、氟化物以预防龋齿、锌以增强味觉、三氯生作为主要的抗菌/抗炎剂以及柠檬味的非致龋甜味剂，以增加产品的适口性，同时刺激任何残留的唾液功能。
