[关键词]
[摘要]
目的 建立丹皮酚β-环糊精包合物的制备工艺。方法 以包合物收得率和包合率为指标,采用正交试验优选β-环糊精包合丹皮酚的条件,在此条件下,采用3种不同的包合工艺制备丹皮酚环糊精包合物,并对pH和HPMC对包合的影响进行了研究。结果 1份丹皮酚用6份量的乙醇溶解后,以每小时1/30V的速度加入45℃10份量β-环糊精的饱和溶液中,搅拌包合至包合物形成,包合率可达80%,包合物收率可达75%以上;不同pH、HPMC下,丹皮酚相溶解曲线呈AL型,不同的pH和HPMC条件下包合稳定常数差异较大。结论 采用优化的饱和溶液法及工艺条件制备包合物,包合率与收率高、工艺简单、设备要求不高,适用于工业化生产。pH2.5、0.5%HPMC条件可进一步增强药物与环糊精的包合作用。
[Key word]
[Abstract]
Objective To set up the preparing technology of paeonol-β-cyclodextrin (β-CD) inclusion compound. Methods The inclusion conditions were optimized by using the orthogonal test for the compound formation of paeonol-β-CD, taking the rate of recovery and inclusion as the criteria. Three different including methods or equipments were adopted and compared with the documentary method. The effect of pH and HPMC on the inclusion of paeonol with β-CD was investigated. Results The inclusion rate and recovery rate were more than 80% and 75%, respectively following the optimized saturated solution method, i.e. resolving 1 part of paeonol in 6 parts of absolute alcohol, then slowly adding the solution into the saturated solution containing 10 parts of β-CD in 1/30 V/h at 45 ℃, keeping stirring until the inclusion compound formation. An A_L-type phase solubility curve was obtained. The difference of apparent stability constant is significant under different pH values and different HPMC contents. Conclusion The technology and procedure are relative simple and high efficient, which are applied for the industrialization. HPMC (0.05%) in pH 2.5 is shown to increase the inclusion of paeonol with β-CD.
[中图分类号]
[基金项目]
国家高技术产业发展项目计划(计高技[2001]2170号)