文献类型：期刊文献

中文题名：盐酸小檗碱-羟丙基-β-环糊精包合物的制备、表征及溶出度研究

英文题名：Study on Preparation,Characterization and Dissolution of Berberine Hydrochloride-hydroxypropyl-β-cyclodextrin Inclusion Compound

作者：张锴[1];陈小慧[2];杨群[1,2]

机构：[1]太极集团浙江东方制药有限公司;[2]绍兴文理学院元培学院

年份：2014

卷号：25

期号：25

起止页码：2349

中文期刊名：中国药房

外文期刊名：China Pharmacy

收录：CSTPCD、、CSCD_E2013_2014、CSCD

语种：中文

中文关键词：盐酸小檗碱;羟丙基-β-环糊精;包合物;表征;溶出度

外文关键词：Berberine hydrochloride; Hydroxypropyl-β-cyclodextrin.; Inclusion compound; Characterization; Dissolution

中文摘要：目的:制备盐酸小檗碱-羟丙基-β-环糊精(盐酸小檗碱-HP-β-CD)包合物,以提高其溶出度,并对其进行表征。方法:以HP-β-CD为包合材料,采用喷雾干燥法制备盐酸小檗碱-HP-β-CD包合物。通过相溶解度法考察包合物中盐酸小檗碱与HP-β-CD的包合摩尔比及包合过程的热力学常数;以桨法测定盐酸小檗碱原料药、盐酸小檗碱-HP-β-CD包合物及其物理混合物的溶出度;以X射线衍射法和扫描电子显微镜法对包合物进行物相鉴定。结果:30、40、50℃下盐酸小檗碱和HP-β-CD均形成1∶1摩尔比的包合物,相溶解度图呈AL型,50℃时表观稳定常数KC为647.17,吉布斯自由能变化ΔG<0,包合反应的热焓值ΔH为6.11 kJ/mol,熵值ΔS为72.73 J/(mol·K),包合过程为吸热过程,包合反应是一个熵驱动的反应;与盐酸小檗碱原料药和物理混合物比较,包合物的溶出度明显增加;物相鉴定结果表明包合物中盐酸小檗碱的晶体衍射峰均消失。结论:制得的盐酸小檗碱-HP-β-CD包合物能显著提高盐酸小檗碱的溶出度。

外文摘要：OBJECTIVE： To prepare and characterize the Berberine hydrochloride-hydroxypropyl-β-cyclodextrin （berberine hydrochloride-HP-β-CD） inclusion compound so as to improve its dissolution. METHODS： Using HP-β-CD as inclusion material, Berberine hydrochloride-HP-β-CD inclusion compound was prepared by spray-drying method. Meanwhile, the mol ratio between host and guest molecular and the thermodynamic constants during the inclusion process were researched by phase solubility method. The inclusion compound was also identified by X-ray diffraction and scanning electron microscope, respectively. The dissolution of raw material, Berberine hydrochloride-HP-β-CD inclusion compound and physical mixture were determined by paddle method. RESULTS ： An 1 ： 1 molar ratio inclusion compound of berberine hydrochloride with HP-β-CD was formed at 30, 40, and 50 ℃. The phase diagram was AL type. The apparent stability constant of KC was 647.17 at 50 ℃ [△G〈0, △H=6.11 kJ/mol,△S=72.73 J/（mol·K）], and the procedure of inclusion was an endothermic process. The inclusion reaction was an entropy driven reaction. The XRD and SEM results showed that the crystal diffraction peaks of berberine hydrochloride were disappeared. Compared with raw material and physical mixture of berberine hydrochloride, the dissolution of inclusion compound was increased significantly. CONCLUSIONS： The dissolution of Berberine hydrochloride-HP-β-CD inclusion compound can significantly improve the dissolution of berberine hydrochloride.