β-环糊精与盐酸黄连碱包合物的制备及其结构研究

目的:优化盐酸黄连碱/β-环糊精(β-CD)包合物的制备工艺,表征包合物结构。方法:以包合温度、包合时间、冷却时间为考察因素,以盐酸黄连碱的包合率为考察指标进行工艺的优选;对包合物结构进行UV-Vis、DSC1、H-NMR表征以及增溶性实验。结果:包合最佳工艺为:β-CD(mol)∶盐酸黄连碱(mol)=2∶1,40℃,包合时间为2 h,冷却时间为3 d,盐酸黄连碱的包合率达到90.64%;UV-Vis表征得到二者的包结常数为3.11×106M-1;DSC表征说明包合物的形成大大提高了盐酸黄连碱的热稳定性;1H-NMR表征说明盐酸黄连碱的苯环进入了β-CD的空腔;而增溶性实验表明包合物的形成促进了盐酸黄连碱在水中的溶解度。结论:β-CD可以与盐酸黄连碱形成2∶1的稳定包合物,并提高了盐酸黄连碱的生物利用度。

Preparation and stuctural behavior of the inclusion complex of beta-cyclodextrin and coptisine hydrochloride

Objective:To optimize the preparation of Coptisine hydrochloride/β-cyclodextrin(β-CD)inclusion complex and analyze the structure of the inclusion complex.Methods: With encapsulation rate as the index of evaluation,different factors influencing the inclusion complex e.g.temperature,inclusion time and cooling time were investigated;UV-vis,DSC,1H-NMR,and solubilization experiment were utilized to analyze the inclusion complex.Results: The optimum process was as follows: coptisine hydrochloride: β-CD(mol/mol)=1∶2,40 °C,agitating for 2h and then cooling for 3d.Inclusion rate was 90.64%.Various characterization results showed that the inclusion equilibrium constant Ka was 3.11 ×106 M-1 at 298K,the benzene ring of coptisine hydrochloride was included into the cavity of β-CD,furthermore,the thermal stability and water-solubility of coptisine hydrochloride was improved when it was included with β-CD.Conclusion: The 2∶1(molar ratio)complexes between β-CD and coptisine hydrochloride is formed,which improves the bioavailability of coptisine hydrochloride.