摘要
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。
Objective：To optimize the preparation of Coptisine hydrochlorideβ-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 in- clusion complex e.g. temperature, inclusion time and cooling time were investigated; UV-vis, DSC, ^-1H-NMR, and solubilization ex- periment were utilized to analyze the inclusion complex. Results： The optimum process was as follows： coptisine hydrochloride： fl-CD （mol/mol） = 1： 2, 40℃, 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 x 106 M-1 at 298K, the benzene ring of coptisine hydrochloride was in- cluded 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 im- proves the bioavailability of coptisine hydrochloride.
出处
《中药材》
CAS
CSCD
北大核心
2012年第1期138-141,共4页
Journal of Chinese Medicinal Materials
基金
惠州学院博士科研启动基金(C510.0209)
关键词
Β-环糊精
黄连碱
包合
增溶性
β-cyclodextrin
Coptisine hydrochloride
Inclusion
Solubility enhancement
