载葛根素的海藻酸镁胃内滞留释药系统的研究

Preparation and in vitro evaluation of a novel gas and puerarin loaded alginate magnesium gastric retention drug system

采用滴制法制备微丸,选取海藻酸钠为载体材料,氯化镁为交联剂,碳酸氢钠为制泡剂,海藻酸钠与镁离子发生交联反应制得胃漂浮微丸,考察微丸的外观、粒径、微观结构、漂浮性以及释药行为。为延长药物在胃靶向释放时长,在单因素实验的基础上,以Eudragit L100和Eudragit RSALO作为载体材料制备载药固体分散体,粉碎过筛后加入海藻酸钠溶液中,依法制备载药固体分散体胃漂浮微丸,以Eudragit L100、Eudragit RSALO和药物的质量比为考察因素,评价其漂浮性和释放度。结果表明制得的载药固体分散体胃漂浮微丸持续9 h有超过95%的漂浮率,载药固体分散体微丸累积释放在5 h达到76%-83%。本文制备的载药固体分散体胃漂浮微丸可在模拟胃液中持续漂浮并缓慢释放药物,为这类药物的胃漂浮给药系统的发展提供了思路。

To prepare gas loaded gastric floating sustained-release beads, in vitro release behaviors was evaluated. The drug-loaded solid dispersion was prepared by the method of solvent. Puerarin was selected as the model drug. Eudragit L100 and Eudragit RSALO were used as the carrier material. NaHCO3 was chosen as the gas-forming agent. After being crushed and sieved, the drug-loaded solid dispersion was added in the sodium alginate solution. Then, the suspension was dropped into the magnesium chlorine acetic acid solution.After a while and drying, the puerarin solid dispersion gastric floating beads were prepared and its in vitro properties in simulated gastric fluid were investigated. More than 95% of the gastric floating beads kept floating in 9 h. The cumulative release percentage was proved to be 76% ~ 83% in 5 h. The sustained release of puerarin in the sal-magnesium gastric floating beads could be achieved by using the solid dispersion method,which provided some ideas of gastric floating preparations for this kind of drugs.