药剂学硕士研究学位论文.doc

单位代码： 10369 学 号：2010届硕士研究生学位论文 法莫替丁胃内漂浮型缓释片的研究 Study on the Famotidine Intragastric floating Sustained-release Tables 学科专业 药剂学 研究方向 药物新剂型与新技术 导 师 教授 硕 士 生 2010年4月?合肥 摘 要 胃内漂浮型缓释制剂是根据流体动力学平衡控制系统原理设计的一种新型给药系统法莫替丁第三代一种高效、长效的组胺H2受体拮抗剂。临床研究表明，法莫替丁用于治疗消化性溃疡时的剂量以每天给药1次，每次40mg为宜。在6.82～68.2μg/ml浓度范围内有较好的线性关系，R2 = 0.9995～μg/ml内呈良好的线性关系，R2 = 0.9994；回收率可达99%，该法简便、灵敏、准确。 4、直接目测法观察法莫替丁胃内漂浮型缓释片的漂浮性能，方便、简洁。 5、法莫替丁胃内漂浮型缓释片为双层片，由速释层（mg）和缓释层（3）HPMC为骨架材料，单硬脂酸甘油酯为助漂剂，NaHCO3为发泡剂。在单因素试验的基础上，采用正交设计优化筛选，获得缓释部分的最佳处方与工艺：法莫替丁34mg，HPMC（K15M：E50=2:1）66mgNaHCO3 16.5mg，单硬脂酸甘油酯 16.5mg乳糖 31mg，以95%乙醇3～4Kg～～HPLC方法样品最低检测浓度为ng/ml，在50～1000ng/ml浓度范围内线性关系良好法莫替丁胃内漂浮型缓释片Abstract The objective of the study is to design and prepare oral controlled drug delivery via gastric retention based on principles of hydrodynamically balanced systems, so as to extend the retention time of control the drug release rate, to enhance the drug absorption in stomach, and to improve drug bioavailability. Famotidine is a new H2-receptor antagonist and effective in the treatment peptic ulcer and duodenum ulcer. Clinincal study shows that the dose of famotidine in the treatment is 40mg once in a day. Methods: Famotidine intragastric floating sustained-release tablets in stomach was designed based on principle of hydronamically balanced systems, and hydrophilic gel was chose as matrices. Single factor experiment was conducted to establish the influencing factors experiment was conducted to establish the influencing factors on the drug release. The formulation was optimized by orthogonal design. Famotidine cotent of intragastric floating sustained-release tablets and their in vitro release rate were tested by HPLC and UV assay methods respectively. In vitro release mechanism should be studied. Cross study in rabbits was conducted to study the pharmacokinetics of famotidine intragastric floating sustai