美沙拉嗪-β-环糊精包合物的制备及其性质研究  

Preparation and Properties of Mesalazine β-Cyclodextrin Inclusion Compound

作　　者：江春玲 刘丛海 张成贵[2] 谢恒元 蔡广亚 周娅 陈实 Jiang Chunling Liu Conghai Zhang Chenggui Xie Hengyuan Cai Guangya Zhou Ya Chen Shi(Department of Clin- ical Pharmacy, Daehuan Area People＇ s Hospital, Siehuan Dazhou 635000, China Department of Clinical Pharmacy, Dazhou Cen- tral Hospital)

机构地区：[1]达川区人民医院临床药学室,四川达州635000 [2]达州市中心医院临床药学室

出　　处：《中国药师》2017年第2期266-270,共5页China Pharmacist

摘　　要：目的:制备美沙拉嗪-β-环糊精包合物并对其性质进行考察。方法:采用沉淀法制备包合物,并通过紫外光谱(UV)、红外光谱(IR)、差示扫描量热分析(DSC)对其结构进行表征,采用分子对接技术进一步对美沙拉嗪和β-环糊精的包合过程进行模拟。测定包合物的溶解度和溶出度。结果:UV、IR和DSC确定了包合物的形成,美沙拉嗪与β-环糊精包合物的包合比为1∶1,相溶解度图呈A_L型,包合物在去离子水中(25℃,pH 7.0)溶解度为7.8 mg·ml^(-1),美沙拉嗪与β-环糊精形成包合物后能显著提高美沙拉嗪的溶出速度和溶解度。结论:β-环糊精对美沙拉嗪的包合作用能够显著改善美沙拉嗪较差的水溶性及其溶出性质。Objective： To prepare mesalazine 13-cyclodextrin inclusion compound and observe its properties. Methods： The struc- ture was characterized by UV, IR and DSC. The inclusion process of mesalazine and ^-cyclodextrin was simulated using molecular doc- king technique. The solubility and dissolution of inclusion compound were determined. Results： UV, IR and DSC were used to deter- mine the formation of inclusion complex. The inclusion ratio was 1： 1 and the phase solubility diagram was Al. type. The solubility of inclusion compound in deionized water （25 ℃, pH 7.0） was 7.8 mg ml - i. The preparation of mesalazine β-cyclodextrin inclusion compound could significantly increase the dissolution rate and solubility of mesalazine. Conclusion： The prepared mesalazine β-cyclo- dextrin inclusion compound can obviously improve the poor water solubility and dissolution of mesalazine.

关 键 词：美沙拉嗪 Β-环糊精 包合物 热力学 生物利用度 

分 类 号：R945[医药卫生—微生物与生化药学]