昂丹司琼口腔黏附片的制备及评价  

Preparation and evaluation of ondansetron oral mucosal adhesive tablets

作　　者：张友智[1] 王力[1] 

机构地区：[1]武汉科技大学附属天佑医院,武汉430064

出　　处：《中南药学》2012年第6期437-440,共4页Central South Pharmacy

摘　　要：目的制备及评价盐酸昂丹司琼口腔黏附片。方法采用相关的黏膜黏着剂卡波姆(CP934)、海藻酸钠、低黏度羧甲基纤维素钠(SCMCLV),用直接压片法压片,对黏附片的不同参数如药物含量、体外溶胀百分率、药物体外释放度和黏附力进行评价。结果筛选出最佳配方:昂丹司琼5mg、CP934 30mg、SCMC 165mg、聚乙二醇-6000 40mg、乳糖10mg、硬脂酸镁1.5mg和阿斯巴甜2mg。结论与昂丹司琼的普通片剂进行比较,昂丹司琼口腔黏附片体外药物释放和渗透都很好,既避免了肝脏首过效应,提高了昂丹司琼的生物利用度;又避免了昂丹司琼的苦味,更易于为患者所接受。Objective To develop and evaluate an oral mucosal adhesive tablet containing ondansetron hydrochloride. Methods The tablets were prepared with carbopol （CP 934）, sodium alginate, and sodium carboxymethylcelluiose low viscosity （SCMC LV）. Special punches and dies were fabricated and used in preparing oral mucosal adhesive tablets. The study was appraised by different parameters such as drug content, swelling index, in vitro drug release studies, and mucoadhesive strength. Results The optimized formulation was composed of ondansetron （5 mg）, CP 934 （30 rag）, SCMC LV （165 mg）, PEG-6000 （40 mg）, lactose （10 rag）, magnesium stearate （1.5 mg）, and aspartame （2 mg）. Conclusion Compared with ondansetron ordinary tablets, buccal adhesive ondansetron tablets have good dosage form, maximum release and permeation. Ondansetron oral mucosal adhesive tablets are an alternative route to bypass the hepatic first-pass metabolism and to improve the bioavailability of ondansetron.

关 键 词：口腔黏附片 颊吸收 黏膜黏着剂 昂丹司琼 合理配方 

分 类 号：R944.9[医药卫生—药剂学]