左羟丙哌嗪β-环糊精包合物的处方工艺优化及鉴定  

Formulation Process Optimization and Identification of Levodropropizine β-cyclodextrin Inclusion Compound

作　　者：赵珊[1,2] 王慧娟[1,2] 林冰[1,2] 庄学亮 周英[1,2] 

机构地区：[1]贵州大学药学院,贵阳550025 [2]贵州省中药民族药创制工程中心,贵阳550025

出　　处：《中国药房》2014年第37期3496-3499,共4页China Pharmacy

基　　金：贵阳市科技计划项目[No.筑科合同(2012204)47号];贵州大学大学生创新性实验计划项目[No.贵大创字(2011)063号]

摘　　要：目的:优化左羟丙哌嗪β-环糊精包合物的处方工艺,并对包合物进行鉴定。方法:采用饱和水溶液法制备包合物,以左羟丙哌嗪与β-环糊精摩尔比、包合温度、包合时间为考察因素,以收率和包合率为指标,采用正交设计优化处方。比较溶出5 min时所制包合物、左羟丙哌嗪和β-环糊精的物理混合物、左羟丙哌嗪原料药的溶出度,采用差示热分析法(DTA)和X-射线衍射法(XRD)对所制包合物进行鉴定,并比较包合物和物理混合物的口感。结果:最优处方工艺为左羟丙哌嗪与β-环糊精摩尔比为1∶1,包合温度为65℃,包合时间为0.5 h;所得包合物的平均收率为95.3%,平均包合率为82.3%;溶出5 min时包合物、物理混合物、左羟丙哌嗪原料药的溶出度分别为98.37%、61.62%、92.59%;DTA和XRD图谱确证已形成了包合物;包合物较物理混合物苦味明显降低。结论:成功制得左羟丙哌嗪β-环糊精包合物,其可较好掩盖药物的苦味。OBJECTIVE： To optimize the formulation process of Levodropropizine β-cyclodextrin（β-CD） inclusion compound, and to identify it. METHODS： The inclusion compound was prepared by saturated water solution method. The formulation process of the compound was optimized by orthogonal design with yield and inclusion rate as index using mole ratio of levodropropizine to β-CD, inclusion temperature and inclusion time as factors. The dissolution rate of prepared compound, Levodropropizine and β-CD physical mixture and levodropropizine raw material were compared 5 min after dissolving. The inclusion compounds were identified with differential thermal analysis （DTA） and X-ray diffraction （XRD）. The taste of the compound was compared with that of physical mixture. RESULTS： The optimal formulation was as follows： mole ratio of levodropropizine to β-CD was 1 ： 1 ; inclusion temperature was 65 ℃ and inclusion time was 0.5 h. Average yield of inclusion compound was 95.3% and average inclusion rate was 82.3%. 5 min after dissolving, the dissolution rates of prepared compound, physical mixture and levodropropizine raw material were 98.37%, 61.62% and 92.59%, respectively. Inclusion compound was confirmed to be formed by DTA and XRD. The bitter taste of the compound decreased significantly, compared with physical mixture. CONCLUSIONS： Levodropropizine β-CD inclusion compound is prepared successfully and can cover up the bitter taste of drugs.

关 键 词：左羟丙哌嗪β-环糊精包合物 处方工艺优化 鉴定 饱和水溶液法 

分 类 号：R943[医药卫生—药剂学]