共研磨法提高兰索拉唑的溶出度

Improvement of Dissolution of Lansoprazole by Co-grinding Method

采用共研磨法分别制备兰索拉唑与β-环糊精(β-CD)、低取代羟丙纤维素(L-HPC)、羟丙甲纤维素(HPMC)、聚乙烯吡咯烷酮(PVP)、交联聚维酮(PVPP)、聚乙二醇(PEG)6000或壳聚糖(1:1)的共研磨物,测定了原药、物理混合物和共研磨物的溶出度,并用差示扫描量热法和X-射线衍射法鉴别药物在共研磨物中的存在状态。测定了兰索拉唑原药、物理混合物和共研磨物于室温放置6个月后的含量和溶出度,考察共研磨样品的稳定性。结果表明,兰索拉唑与β-CD、L-HPC、HPMC、PVP和壳聚糖的共研磨物的溶出度较兰索拉唑原药有显著提高,且稳定性较好。

The different co-ground mixtures of lansoprazole and β-cyclodextrin （β-CD）, low-substituted hydroxypropyl cellulose （L-HPC）, hyprornellose （HPMC）, polyvinylpyrrolidone （PVP）, polyvinylpolypyrrolidone （PVPP）, polyethylene glycol （PEG） 6000 or chitosan were prepared by co-grinding method with the ratio of 1 ： 1. The dissolution rates of bulk drug, physical mixtures and co-ground mixtures were determined. The phase of lansoprazole in the above mixtures was analyzed by DSC and X-ray diffraction. The drug content and dissolution of the samples stored at room temperature for six months were also investigated to evaluate the stability of the co-ground mixtures. The results showed that the dissolution rates of lansoprazole from the co-grotmd mixtures of β-CD, L-HPC, HPMC, PVP or chitosan were significantly increased compared with the bulk drug. And these co-ground mixtures had good stability.