摘要
目的 研制单硝酸异山梨酯 (5 ISMN)定时脉冲释放片 ,并考察体外溶出的影响因素。方法 采用压制包衣技术制备 5 ISMN定时脉冲释放片 ,以崩解时间和膨胀率为指标 ,筛选了崩解剂类型和用量 ;采用反相高效液相色谱法测定体外溶出度 ,以释药时滞为指标 ,经均匀设计实验 ,筛选优化外包衣层处方组成。结果 片芯选用羧甲基淀粉钠为崩解剂 ,用量 2 0 %即能达到设计要求。固定硬度 ,调整亲疏水性成分的比例 ,确定了时滞为 3,4 ,5h的 3个基本处方。硬度、亲疏水性物质比、溶出介质黏度对时滞影响显著。结论 单硝酸异山梨酯压制包衣片能实现体外定时脉冲释药 ,并可通过调整处方和工艺因素实现不同时滞的控释效果。
OBJECTIVE: To prepare the time-controlled tablets of isosorbide mononitrate and study the influence factors on the release of it in vitro. METHODS: The pulsatile tablets of isosorbide-5-mononitrate was prepared with the press-coated technics. The types and amount of disintegrants were chosen according to the disintegrate time and the expanding rate. The uniform design method was used to optimize the formulation of coating layer. RESULTS: 20% CMS-Na was selected as the disintegrant. The three basic formulations were determined by changing the ratio of hydrophilic and hydrophobic materials at a certain hardness. Hardness, the ratio of hydrophilic and hydrophobic materials and viscosity had notable effects on the lag time. CONCLUSION: The press-coated tablets of isosorbide mononitrate can release at the predetermined time and the controlled-release purpose can be reached by adjusting formulation and technic factors.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2003年第8期604-608,共5页
Chinese Pharmaceutical Journal
基金
全军医药卫生"十五"科研基金重点资助课题 (No.0 1Z0 0 4)
关键词
单硝酸异山梨酯
定时脉冲释放片
制备
体外溶出度
二硝酸异山梨酯
Coating techniques
Disintegration
Dissolution
Hardness
Hydrophilicity
Hydrophobicity
Nitrates
Optimization
Viscosity
