目的:制备法莫替丁胃漂浮缓释微丸,并进行体外评价。方法:选取Eudragit L100和Eudragit RLPO作为固体分散体载体材料,以溶剂法制备法莫替丁固体分散体,粉碎过筛后加入海藻酸钠溶液中,再将混悬液滴入氯化钙醋酸溶液中交联10 min,干燥,得法莫替丁固体分散体胃漂浮微丸。以人工胃液为介质,考察微丸的漂浮率和释放度。结果:胃漂浮微丸持续12 h有95%以上的漂浮率;法莫替丁固体分散体胃漂浮微丸体外释放在5 h达到72%~81%。结论:制备的法莫替丁固体分散体胃漂浮微丸可在人工胃液中持续漂浮并缓慢释放药物。
OBJECTIVE To prepare famotidine gastric floating sustained-release beads and evaluate its in vitro release behaviors. METHODS The solid dispersion of famotidine was obtained by the method of solvent. Eudragit L100 and Eudragit RLPO were used as the carrier material. After being crushed and sieved, the solid dispersion of famotidine was added in the al- ginate solution. Then, the suspension was dropped into the calcium chlorine acetic acid solution and stirred for 10 min. After drying, the famotidine solid dispersion gastric floating beads were obtained and its in vitro properties in simulated gastric fluid were investigated. RESULTS More than 95% of the gastric floating beads were kept floating in 12 h. The cumulative release percentage was found to be 72%~81% in 5 h. CONCLUSION The famotidine solid dispersion gastric floating beads could be kept floating in simulated gastric fluid and delay famotidine release from the beads.