Aman Reham Mokhtar, Meshali Mahasen Mohamed, Abdelghani Galal Mahmoud
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University.
Drug Discov Ther. 2014 Dec;8(6):268-75. doi: 10.5582/ddt.2014.01043.
A stable controlled release resinate-complex for the highly bitter taste famotidine (FAM) was developed to allow once-daily administration and improve patient compliance especially in pediatric and geriatric medicine. The drug-resinate complexes were prepared in different drug to resin (Amberlite IRP-69) ratios by weight (1:1, 1:2, 1:3, 1:4, 1:5 and 1:6). The optimized drug-resinate complex resulted from 1:6 drug to resin ratio experienced maximum drug loading and sustained release property. Hence, it was subjected to physicochemical characterizations by differential scanning colorimetry (DSC), x-ray diffractometry (XRD), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). The optimized complex was further dispensed in the prepared syrup and the suspension was subjected to accelerated stability study, as mentioned in the International Conference on Harmonization (ICH) guidelines. Furthermore, the gustatory properties of the complex were evaluated on humans. The syrup complied successfully with ICH guidelines and sufficiently alleviated the bitterness of famotidine.
开发了一种用于高苦味法莫替丁（FAM）的稳定控释树脂复合物，以实现每日一次给药，并提高患者顺应性，尤其是在儿科和老年医学中。通过重量比（1:1、1:2、1:3、1:4、1:5和1:6）制备了不同药物与树脂（Amberlite IRP-69）比例的药物-树脂复合物。药物与树脂比例为1:6时得到的优化药物-树脂复合物具有最大载药量和缓释性能。因此，通过差示扫描量热法（DSC）、X射线衍射法（XRD）、傅里叶变换红外光谱法（FTIR）和扫描电子显微镜（SEM）对其进行了物理化学表征。按照国际协调会议（ICH）指南所述，将优化后的复合物进一步配制成糖浆，并对该混悬液进行加速稳定性研究。此外，还对该复合物在人体上的味觉特性进行了评估。该糖浆成功符合ICH指南要求，并充分减轻了法莫替丁的苦味。
