饱和水溶液法制备葛根素的β环糊精包合物研究-.doc

饱和水溶液法制备葛根素的β环糊精包合物研究*
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作者:尤思路,高秀蓉,廖昌军
【摘要】目的探讨用饱和水溶液法制备葛根素的β环糊精包合物的最佳工艺。方法运用饱和水溶液法制备葛根素β环糊精包合物,并采用紫外分光光度法测定葛根素含量,紫外光谱、红外光谱验证包合物。结果通过正交试验得到最佳制备工艺为葛根素与β环糊精投料比为 1∶1,包合时间为3h,包合温度为60℃,包合率可达94%。结论饱和水溶液法制备葛根素β环糊精包合物工艺简单可行,适用于葛根素口服制剂的改进。
【关键词】葛根素;β环糊精包合物;正交试验
ABSTRACT Objective To discuss the optimum technology of saturated water solution in preparing β-cyclodextrin pound of puerarin. Methods Ultraviolet spectrophotometry was applied to detect the content of puerarin, and ultraviolet spectrum and infrared spectrum were applied to verify the plex. Results Orthogonal test worked out the optimum preparation process: the feed ratio (mol ratio) of puerarin and
β-cyclodextrin was 1:1, the inclusion time was 3 hours and the inclusion temperature was 60, then the inclusion rate reached 94%. Conclusions Satureated solution is of simple application in the preparation of β-cyclodextrin pound of puerarin, and it is suitable for the improvement of puerarin oral preparation
KEYWORDS puerarin β-cyclodextrin pound orthogonal test
葛根素(puerarin ,PU)是从豆科植物野葛、甘葛藤根中提取的一种黄酮甙, mol/L。具有扩张冠脉血管、降低血压和心肌耗氧,抗心律失常和明显限制心肌梗死范围等药理作用,临床上对高血压、心绞痛、急性心肌梗死和视网膜静脉阻塞、突发性耳聋等疾病有较好的疗效[1]。本品静注,在动物体内分布广,消除快,不易积蓄,无代谢饱和现象[2]。大鼠灌胃后,24 % 。正常成人口服葛根素后36 %从尿排出,72 %[3]。表明葛根素由于溶解度低,口服吸收程度较差。为提高PU生物利用度,考虑制备β环糊精(βCD)包合