Razavi Mahboubeh, Nyamathulla Shaik, Karimian Hamed, Noordin Mohamed Ibrahim
Department of Pharmacy, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia.
Department of Pharmacy, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia ; Center for Natural Products and Drug Discovery, Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur, Malaysia.
Drug Des Devel Ther. 2014 Sep 9;8:1315-29. doi: 10.2147/DDDT.S68517. eCollection 2014.
This study aimed to develop hydrophilic, gastroretentive matrix tablets of famotidine with good floating and swelling properties. A novel gastroretentive drug delivery formulation was designed using salep, also known as salepi, a flour obtained from grinding dried palmate tubers of Orchis morio var mascula (Orchidaceae family). The main polysaccharide content of salep is glucomannan, highly soluble in cold and hot water, which forms a viscous solution. Salep was characterized for physicochemical properties, thermal stability, chemical interaction, and surface morphology using X-ray diffraction analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy. Ten different formulations (S1-S10) were prepared using famotidine to salep ratios from 1:0.5 to 1:5. Results demonstrated that all formulations were able to sustain the drug release for more than 24 hours. The S5 formulation, with a famotidine to salep ratio of 1:2.5, had the shortest floating lag time of 35 seconds and 100% drug release within 24 hours. The dissolution data were fitted into popular mathematical models to assess the mechanism of drug release. S5 showed Zero order release (R=0.9746) with Higuchi diffusion (R=0.9428). We conclude that salep, a novel polymer, can be used in controlled release formulations to sustain release for 24 hours, due to inherent swelling and gelling properties.
本研究旨在开发具有良好漂浮和溶胀性能的法莫替丁亲水胃滞留型基质片。使用角豆粉（也称为salepi）设计了一种新型胃滞留药物递送制剂，角豆粉是由磨碎的雄性长距玉凤花（兰科）干燥掌状块茎获得的一种粉末。角豆粉的主要多糖成分为葡甘露聚糖，在冷水和热水中均高度可溶，可形成粘性溶液 采用X射线衍射分析、差示扫描量热法、傅里叶变换红外光谱法及扫描电子显微镜对角豆粉的理化性质、热稳定性、化学相互作用及表面形态进行了表征。使用法莫替丁与角豆粉的比例从1:0.5至1:5制备了10种不同的制剂（S1 - S10）。结果表明，所有制剂均能够使药物释放持续超过24小时。法莫替丁与角豆粉比例为1:2.5的S5制剂具有最短的漂浮滞后时间35秒，且在24小时内药物释放率达100%。将溶出数据拟合到常用数学模型中以评估药物释放机制。S5呈现零级释放（R = 0.9746）和 Higuchi 扩散（R = 0.9428）。我们得出结论，角豆粉作为一种新型聚合物，由于其固有的溶胀和胶凝特性，可用于控释制剂中以实现24小时持续释放。
