[Preparation and stuctural behavior of the inclusion complex of beta-cyclodextrin and coptisine hydrochloride].
OBJECTIVE
To optimize the preparation of Coptisine hydrochloride/beta-cyclodextrin (beta-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: 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.


CONCLUSIONS
The 2:1 (molar ratio) complexes between beta-CD and coptisine hydrochloride is formed, which improves the bioavailability of coptisine hydrochloride.
Department of Chemical Engineering, Huizhou University, Huizhou 516007, China. chenhy@hzu.edu.cn
Hong-Yan
HY
Chen
Zhen
Z
Jin
Shan-Quan
SQ
Chen
D001599:Berberine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D010936:Plant Extracts / Q000737:chemistry*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet / Q000379:methods; D013696:Temperature; D013997:Time Factors; D047392:beta-Cyclodextrins / Q000008:administration & dosage / Q000737:chemistry*
D010936:Plant Extracts; D047392:beta-Cyclodextrins; C034384:coptisine; D001599:Berberine