Groves Emma, Chaw Cheng Shu
a Department of Pharmacy, Health and Well Being , University of Sunderland , Sunderland , UK.
Drug Dev Ind Pharm. 2015;41(10):1608-16. doi: 10.3109/03639045.2014.976573. Epub 2014 Nov 5.
Xanthan gum (XG), a hydrophilic biopolymer with modified release properties, was used to produce directly compressed matrix tablets containing a model drug, sodium p-aminosalicylate. Three formulations were prepared, each containing a different calcium dihydrate salt: calcium chloride, calcium sulfate or dibasic calcium phosphate. The aim of the investigation was to relate the calcium ion content and solubility of the calcium salt to the in vitro drug release profile of the xanthan matrices. Tablet hydration, erosion and drug release were determined in distilled water using the British Pharmacopoeia (BP) paddle method. The data showed that the overall drug release was the greatest with addition of calcium sulfate, followed by calcium chloride and dibasic calcium phosphate. The chloride salt formulation displayed the greatest percentage erosion due to rapid mass loss during the initial phase, followed by those with sulfate or phosphate salts. As xanthan gel viscosity increased and drug release was also found to be lower, it can be concluded that drug release is influenced by the solubility of the salt present in the formulation, since these parameters determine the viscosity and structure of the gel layer.
黄原胶(XG)是一种具有缓释特性的亲水性生物聚合物,被用于制备含有模型药物对氨基水杨酸钠的直接压片基质片剂。制备了三种制剂,每种制剂含有不同的二水合钙盐:氯化钙、硫酸钙或磷酸氢钙。该研究的目的是将钙盐的钙离子含量和溶解度与黄原胶基质的体外药物释放曲线相关联。使用英国药典(BP)桨法在蒸馏水中测定片剂的水化、侵蚀和药物释放。数据表明,添加硫酸钙时总体药物释放最大,其次是氯化钙和磷酸氢钙。由于初始阶段质量快速损失,氯化物盐制剂的侵蚀百分比最大,其次是硫酸盐或磷酸盐盐制剂。随着黄原胶凝胶粘度增加,药物释放也较低,可以得出结论,药物释放受制剂中存在的盐的溶解度影响,因为这些参数决定了凝胶层的粘度和结构。