微晶纤维素联用硬脂酸制备阿司匹林缓释微丸影响研究

Preparation of Aspirin Sustained Release Pellets Using Stearic Acid and Microcrystalline Cellulose

目的研究微晶纤维素(MCC)与硬脂酸(SA)联用对制备遇水敏感药物阿司匹林(ASP)缓释微丸工艺影响。方法以非水润湿剂挤出滚圆(E-S)成丸为工艺基础,与含水E-S微丸对比,以微丸特性、药物稳定性以及体外释放度为指标,考察SA/MCC/ASP不同丸芯比例的影响。结果当SA/MCC在处方中大于35%时,挤出较容易;当SA/MCC比例约为1时,滚圆效果最好;载药量以65%为最佳。与含水处方相比,非水制备微丸粒径小且均一,表观特性较好,制备过程ASP稳定性好。两者体外释放度无显著差异;实验表明,3个月加速稳定性非水处方水解程度低于含水处方。结论 SA能有效改善ASP非水E-S法制备微丸特性。

OBJECTIVE To evaluate mieroerystalline eellulose（MCC） and stearic acid（SA） on extrusion-spheronisation（E-S） for aspirin sustained release pellets. METHODS Mixtures with varying drug concentration and SA/MCC ratios were processed via non-aqueous E-S. Multi-index evaluation method were assessed by rheological behavious, drug stability and release in vitro compared with aqueous E-S. RESULTS The extrusion was easier when 5A/MCC was 〉 35%. When the ratio of SA/MCC was about 1, the roll effect was the best. The drug content was 65%. Compared with aqueous E-S, non-aqueous E-S was small and homogeneous pel- lets, better apparent characteristics, stability. There were no obvious different in drug release in vitro. CONCLUSION These prove to be superior aids for water sensitive aspirin when exposed to non-aqueous solvent by E-S.