共研磨法改善枸橼酸莫沙必利的体外溶出度  

Study on the improvement of dissolution of Mosapride citrate by co-grinding method

作　　者：吕贝贝[1] 王永禄[1] 王栋[1] 顾晓彤[1] 王伊凡[1] 李学明[1] 

机构地区：[1]南京工业大学药学院,江苏南京211816

出　　处：《华西药学杂志》2016年第2期132-134,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81170492);江苏政府留学奖学金(2013)

摘　　要：目的改善枸橼酸莫沙必利的体外溶出度。方法采用共研磨法,分别制备枸橼酸莫沙必利与低取代羟丙基纤维素(L-HPC)、羟丙甲纤维素(HPMC)、聚维酮(PVP)或聚乙二醇6000(PEG 6000)(1∶2)的共研磨物,测定原料药、物理混合物和共研磨物的溶出度;运用X射线衍射法和差示扫描量热法鉴别药物在共研磨物中的存在状态,并考察其稳定性。结果枸橼酸莫沙必利与L-HPC和HPMC共研磨物的溶出度较原料药的显著提高,且稳定性较好。结论共研磨法能够改善枸橼酸莫沙必利的体外溶出度。OBJECTIVE To improve the dissolution rates of Mosapride citrate. METHODS The different co- ground mixtures of mosapride citrate and low- substituted hydroxypropyl cellulose（ L- HPC）,hydroxypropyl methylcellulose（ HPMC）,polyvidone（ PVP）or polyethylene glycol（ PEG） 6000 were prepared by co- grinding method with the ratio of 1 ∶2. The dissolution rates of bulk drug,physical mixtures and co- ground mixtures were determined. The phase of Mosapride citrate in the above mixtures was analyzed by DSC and X- ray diffraction. The stability of the co- ground mixtures were investigated. RESULTS The results showed that the dissolution rates of Mosapride citrate from the co- ground mixtures of L- HPC and HPMC were significantly increased compared with the bulk drug. And these co- ground mixtures had good stability. CONCLUSION The in vitro dissolution rates of Mosapride citrate are improved by Co- grinding method.

关 键 词：枸橼酸莫沙必利 共研磨法 稳定性 溶出度 X射线衍射法 差示扫描量热法 

分 类 号：R917[医药卫生—药物分析学]