河南省专业学位研究生精品教学案例项目-药物制剂工艺与技术
入库时间：2025-12-26 23:55:05 浏览：2 收藏：0 评价：0 推荐：0
案例简介
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专业学位类别：
药学 -
专业领域/方向：
药学/药剂学 -
第一作者：
阎玺庆 -
单位：
河南医药大学 -
关键词：
漂浮片；工业生产；法莫替丁 -
摘要（中文）：
法莫替丁（famotidine） 是第三代H2 受体拮抗剂，能够抑制胃酸分泌，适用于胃及十二指肠溃疡、反流性食管炎、上消化道出血、卓－艾综合征等症。由于有较强极性，且膜透过性差，所以其口服吸收不完全，生物利用度仅为45%~50%。法莫替丁属于米噻唑衍生物，分子具有硫酰胺端，因此其在胃中易溶，在碱性条件下不易溶解，因此该药具有具有pH 依赖性，在小肠中溶解度大大下降。目前上市的剂型主要为普通片剂、注射剂、胶囊、颗粒剂、咀嚼片及口服混悬剂等剂型，法莫替丁普通片剂剂量为20mg，普通剂型的缺点为在胃中崩解迅速崩解，并随胃动力进入进入小肠，所以药物在主要吸收部位胃部的吸收时间较短，部分药物经过肠道被排出。为了提高法莫替丁的生物利用度，需使之在胃部保留足够时间和药物缓慢释放量，比较理想的方法可以通过设计胃漂浮片解决。 -
摘要（英文）：
As a third-generation H2 receptor antagonist, Famotidine is an imidazole derivative used in the treatment of gastric and duodenal ulcers and acute gastrointestinal diseases. It belongs to the class III drug in the biopharmaceutical classification system (BCS). Owing to its strong polarity and poor membrane permeability, its absorption through oral administration is incomplete and so its bioavailability is only 45%-50%. As a pH dependent medicine, its absorption sites are mainly in the stomach and the upper part of the small intestine. Although It is easy to dissolve in the stomach, the solubility in the small intestine environment is difficult. Its main formulations include ordinary tablets, injection, capsules, granules, chewable tablets and oral suspension agent. The dosage of commercial tablets is 20 mg. The ordinary tablets can be disintegrated quickly after oral in the stomach, so the drug molecules cannot be fully absorbed and reduce its curative effect. In order to improve the bioavailability of famotidine, it is necessary to keep it in the stomach for a long time and release the drug slowly, which can be solved by designing a gastric floater. In this case, the production process of the floating tablet is detailed described through the Famotidine manufacturing process. -
适用课程：
药物制剂工艺与技术 -
教学目的与用途：
通过法莫替丁漂浮片的制备生产，掌握制剂从实验室到生产过程详细过程 -
准备工作：
实验室 -
启发思考问题：
实验室的宝贝，如何成为现实的药物？ -
案例知识点：
组方优化，中试，质检过程 -
案例正文：