betadex and coptisine

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.

Topics: Berberine; beta-Cyclodextrins; Drug Compounding; Drug Stability; Plant Extracts; Solubility; Spectrophotometry, Ultraviolet; Temperature; Time Factors