羟丙基-β-环糊精包合对盐酸哌唑嗪的增溶作用研究  

Effect of Hydropropyl-β-Cyclodextrin on Solubility of Prazosin Hydrochloride

作　　者：刘龙孝[1] 朱素燕[1] 

机构地区：[1]浙江大学药物信息学研究所,杭州310027

出　　处：《中国药学杂志》2006年第2期122-125,共4页Chinese Pharmaceutical Journal

基　　金：教育部科学技术研究重点项目资助(104093)

摘　　要：目的研究羟丙基-β-环糊精(HP-β-CD)包合对几乎不溶于水的药物盐酸哌唑嗪溶解度和溶出度的增强作用。方法分别采用研磨法、超声波法和共沉淀法制备盐酸哌唑嗪的HP-β-CD包合物,测定其溶出度,并与盐酸哌唑嗪原药,以及盐酸哌唑嗪与HP-β-CD的物理混合物的溶出性能进行比较。用差示扫描量热法,X-射线衍射和红外光谱对包合物进行物相鉴别。结果 HP-β-CD与盐酸哌唑嗪形成包合物并使其溶解度增加(226．4±3．0)％。结论 HP-β-CD能大幅度地提高盐酸哌唑嗪的溶解度和溶出度。OBJECTIVE To investigate the enhancement of dissolution and solubility of prazosin hydrochloride by its complexation with hydropropyl-β-cyclodextrin（HP-β-CD）. METHODS The inclusion complexes of prazosin hydrochloride were prepared by grinding, ultrasonic method and co-precipitation. The dissolution of inclusion complexes was determined and compared with free prazosin hydrochloride and its physical mixture. The binary systems of prazosin hydrochloride and HP-β-CD were characterized by differential Manning calorimetry, X-ray diffractometry and Fourier transformation-infrared spectroscopy. RESULTS HP-β-CD and prazosin hydrochloride formed inclusion complex with the molar ratio of 1 and the solubility of prazosin hydrochloride was enhanced by （226.4±3.0）%. CONCLUSION The solubility and dissolution rate of prazosin hydrochloride are increased by HP-β-CD inclusion complexation evidently.

关 键 词：盐酸哌唑嗪 羟丙基-Β-环糊精 包合物 相溶解度 溶出度 

分 类 号：R943.4[医药卫生—药剂学]