左乙拉西坦单向释药控释片的制备与释放度评价
Preparation and release evaluation of levetiracetam unidirectional release controlled-release tablets
席雨梦 1何函星 2王晓晖 1郝俊红 1何朝星 1杜青1
作者信息
- 1. 河北医科大学药学院,石家庄 050017
- 2. 石家庄市人民医院,石家庄 050011
- 折叠
摘要
目的:拟研制一种新型左乙拉西坦(levetiracetam,LEV)单向释药控释片.方法:将处方量LEV与载体材料通过溶剂-熔融法制备固体分散体颗粒,干法制粒压片制备药物层,压制保护层后得双层片芯,保护层顶面粘贴保护膜,浸渍法将片芯包衣后,撕掉保护膜即得底面和侧面包衣的LEV单向释药控释片.以体外累积释放度等为评价指标,考察其处方工艺,并进行体外释药模型拟合.结果:最终处方为药物层:LEV原料药250 mg,十八醇62.5 mg,硬脂酸镁6.25 mg;压片硬度为6 kg;保护层:乳糖用量200 mg;包衣层:包衣液为10%EC M70 乙醇溶液;包衣增重百分比为10%.LEV单向释药控释片12h体外累积释放达90%以上,释药行为符合零级释放模型.结论:自制的LEV单向释药控释片处方工艺简单可行、体外释放缓慢平稳,符合控释制剂理想特征.
Abstract
Objective:To develop a novel type of levetiracetam(LEV)unidirectional release controlled-release tablet.Methods:Solid dispersion particles were prepared by solvent-melting layer method,and a double layer core was obtained.The top surface of the protective layer was pasted with a protective film,the core was coated using impregnation method,and the protective film was torn off to obtain the bottom and side-coated LEV unidirectional drug release controlled release tablets.Taking the cumulative release rate in vitro as the evaluation index,the prescription technology was investigated,and the in vitro drug release model was fitted.Results:The final formulation was as follows:Drug layer:LEV 250 mg,octadecanol 62.5 mg,magnesium stearate 6.25 mg,tablet hardness 6 kg;Protective layer:lactose 200 mg;Coating layer:the coating solution was 10%EC M70 ethanol solution,and the weight gain percentage of the coating is 10%.The cumulative release rate of LEV controlled-release tablets was more than 90%after 12 h in vitro,and the release behavior was in accordance with zero-order release model.Conclusion:The formulation and preparation process of LEV controlled-release tablets is simple and feasible,and the in vitro drug release is slow and stable,which accords with the ideal characteristics of controlled-release tablets.
关键词
左乙拉西坦/控释片/浸渍法包衣/体外释放Key words
levetiracetam/controlled-release tablets/impregnation coating/in vitro release引用本文复制引用
基金项目
河北省自然科学基金资助项目(H2020206451)
河北省2021年度医学科学研究课题资助项目(20211108)
出版年
2024
NETL
NSTL
维普
万方数据