尼群地平包合物的制备与性质.docVIP

尼群地平-β-环糊精包合物的制备与性质 李星，王建华* 重庆大学生物工程学院，重庆 400044 摘要：目的 研究尼群地平-β-环糊精包合物最佳制备工艺，并研究其包合物性质。方法 采用研磨法、饱和水溶液法、超声波法，通过正交实验设计，确定最佳制备方法及工艺。采用显微观察、X-衍射法、紫外分光光度法来鉴定及研究包合物性质。结果 超声波法制备的包合收率大于其余两法，其最佳包合工艺为超声功率为40KW；β-CD：尼群地平为4:1（摩尔比）；超声温度为20℃；超声时间为70min。经鉴定形成了尼群地平-β-环糊精包合物。结论 使用超声波法包合后，包合物比原料药的溶解性增强了10.5倍，光稳定性增强3.7倍。其包合产物性质的改善，有助于其制剂生物利用度的提高。 关键词：尼群地平；超声波法；包合制备；正交分析 Study on Characterization of the Inclusion Complexes of Nitrendipine with β-Cyclodextrin LI Xing, WANG Jian-hua Bioengineering College of Chongqing University, Chongqing 400044 ABSTRACT: OBJECTIVE To select the optimum preparation process of the inclusion complex of nitrendipine-β-cyclodextrin and study the property of the complex. METHODS The nitrendipine-β-cyclodextrin inclusion complexes were prepared through solid method, saturation solution method and ultrasonic method and the function of inclusion complexes were studied on physical and chemical characterizations. RESULTS The ultrasonic method is the best one in three methods. The optimum entrapment conditions were as follows: The ultrasonic power was 40KW,the ratio ofβ-CD to nitrendipine was 4:1, temperature was 20℃, reaction time was 70 min. The formation of compound nitrendipine -β-CD was confirmed and studied by microscope observation , X-Ray powder diffractometry and UV method. CONCLUSIONS Inclusion complex not only can enhance 3.7 times the stability to light, but also can gain 10.5 times the solubility of guest molecule. Its improvement could increase the value in body use. KEY WORD: nitrendipine; ultrasonic method; preparation of inclusion complex; orthogonal design 尼群地平（nitrendipine, NTD）为二氢吡啶类钙拮抗剂，主要抑制血管平滑肌和心肌的跨膜钙离子内流，降低舒张压，持久扩张冠状血管，降低心肌耗氧量，可用于治疗各种类型的高血压，也可用于充血性心力衰竭。教育部留学回国人员科研启动基金（2006）3312006BB5017 作者简介：李星，（1982-），女，硕士，研究方向：环糊精修饰与应用； TEL E-mail： kinsin1@163.com 王建华，（1962-）男，安徽，博士，教授，研究方向：药物化学，通讯联系人。 腔有疏水性，可把许多大小合适的分子容纳在空腔中形成包合物。β-环糊精作为一种高效、低毒、安全有效的药用辅料，可以促进药物的溶解度和溶出度、提高药物的稳定性、改变药物状态便于制剂、掩盖药物的不良气味和降低刺激性、促进药物的吸收，还具透皮促进作用。因此