尼莫地平固体自微乳化舌下速溶片的制备及质量评价

Preparation and quality evaluation of nimodipine solid self-microemulsifying fast-disintegrating sublingual tablets

目的:制备尼莫地平固体自微乳化舌下速溶片(NM-S-SMFDST)并进行质量评价。方法:以最大饱和量,口感为指标筛选固体吸附载体的种类,考察其对尼莫地平固体自微乳化粉末流动性及溶出度的影响来确定吸附载体的量;以正交设计方法优化自微乳化舌下速溶片处方,并对外观、乳化后粒径及形态、崩解及润湿时间、含量均匀度、含量、溶出度及口感进行了评价。结果:优化最佳处方比例为:尼莫地平∶自乳化辅料混合物∶Aerosil-300∶甘露醇∶MCC∶PVPP∶阿斯巴甜=3.3%∶37.0%∶28.3%∶12.4%∶8%∶8%∶3%。所制备的NM-S-SMFDST外观及口感良好,乳化后粒径为:(34.4±2.62)nm,1 h累积溶出度达90%以上,崩解、湿润时限、含量以及含量均匀度达到要求。结论:所制得的NM-S-SMFDST处方及工艺合理,质量指标均符合舌下片的要求。

OBJECTIVE To prepare nimodipine solid self-microemulsifying fast disintegrating sublingual tablets and evaluate their quality. METHODS The type of adsorbents were screened with the maximum saturation and taste as index, and the capacity of adsorbents were determined by investigating the influence of adsorbents on nimodipine solid self-microemulsifying powder flowability and dissolution. The prescription was optimized by orthogonal test. The appearance, the particle size and morphology after emulsification, the disintegration and wetting time, the content uniformity, the content, the dissolution and the taste were evaluated. RESULTS The obtained best prescription was 3.3% of nimodipine, 37% of SMEDDS, 28.3% of Aerosil-300, 12. 4 % of mannitol, 8 % of MCC, 8 % of PVPP, 3 % of aspartame. NM-S-SMFDSTs were integrated with desira- ble appearance and taste. The particle size was （34. 4± 2. 62） nm, the cumulative dissolution percentage was above 90% within 1 h. The disintegration and wetting time, the content and content uniformity were up to requirement. CONCLUSION The prescription and technology are reasonable and the quality indexes conform to the requirement of NM-S-SMFDST.