Preparation and Properties Study of Inclusion Complex of Triptonide with 2,6-Dimethyl-β-cyclodextrin

Abstract

The inclusion complex of Triptonide (TN) and 2,6-dimethyl- β -cyclodextrin (DM- β -CD) was prepared by saturated aqueous solution method. The TN/DM- β -CD inclusion complex was characterized by Fourier transform infrared spectrometry (FTIR), X-ray powder diffraction (XRD), scanning electron microscopy (SEM) and thermogravimetric analysis (TGA), and the possible inclusion mode was inferred by 1 H nuclear magnetic rosonace (NMR) and 2D ROESY. The Job's plot showed that the inclusion ratio of host and guest was 1:1. The stability constant of 2891 M −1 was determined by UV absorbance spectra. The result showed that the DM- β -CD was able to solubilize TN to level as high as 2.7 mg mL −1 . The water solubility of inclusion complex was increased by 150 times. In vitro release experiments showed that the cumulative release rate of the inclusion complex reached 70% in 12 h, while the cumulative release rate of TN reached 70% in 120 h. The inclusion complex had important applications in medical field with higher activity, higher solubility and lower toxicity. A novel Tri/DM-β-CD inclusion complex was prepared and characterized. The inclusion ratio of host and guest was 1:1, and the stability constant of inclusion was 2891 M −1 . The result showed that the DM-β-CD was able to solubilize Tri to level as high as 2.7 mg mL −1 . The water solubility of inclusion complex increases 150 times. At 12 h, the cumulative release rate of Tri in the inclusion complex was higher than the individual guest.