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

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.