Chen Hong-Yan, Jin Zhen, Chen Shan-Quan
Department of Chemical Engineering, Huizhou University, Huizhou 516007, China.
Zhong Yao Cai. 2012 Jan;35(1):138-41.
To optimize the preparation of Coptisine hydrochloride/beta-cyclodextrin (beta-CD) inclusion complex and analyze the structure of the inclusion complex.
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.
The optimum process was as follows: coptisine hydrochloride: beta-CD (mol/mol) = 1: 2, 40 degrees 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 x 10(6) M(-1) at 298K, the benzene ring of coptisine hydrochloride was included into the cavity of beta-CD, furthermore, the thermal stability and water-solubility of coptisine hydrochloride was improved when it was included with beta-CD.
The 2:1 (molar ratio) complexes between beta-CD and coptisine hydrochloride is formed, which improves the bioavailability of coptisine hydrochloride.
优化盐酸黄连碱/β-环糊精（β-CD）包合物的制备工艺，并分析包合物的结构。
以包封率为评价指标，考察温度、包合时间、冷却时间等影响包合物形成的因素；采用紫外-可见光谱（UV-vis）、差示扫描量热法（DSC）、核磁共振氢谱（1H-NMR）及增溶实验对包合物进行分析。
最佳工艺为：盐酸黄连碱与β-CD摩尔比为1∶2，于40℃搅拌2 h后冷却3 d，包封率为90.64%。各项表征结果表明，在298 K时包合平衡常数Ka为3.11×10(6) M(-1)，盐酸黄连碱的苯环被包入β-CD的空腔内，且盐酸黄连碱与β-CD包合后其热稳定性和水溶性均有所提高。
形成了β-CD与盐酸黄连碱摩尔比为2∶1的包合物，提高了盐酸黄连碱的生物利用度。
