OBJECTIVE To optimize β-cyclodextrin (β-CD) inclusion process of Cinnamomi Ramulus Formula Granules volatile constituents by orthogonal test, based on standard relation and information entropy method.
METHODS On the basis of single factor experiments, the ratio of β-CD to aromatic aqueous solution, the inclusion temperature, and the inclusion time were selected as the investigating factors; the inclusion rate, drug loading, and standard relation of cinnamic aldehyde in inclusion complex were used as the evaluation index. The information entropy method was used to determine the weight coefficient of each index, then the comprehensive score was calculated, the inclusion process conditions were optimized by orthogonal experiment. The inclusion complex was characterized by thin layer chromatography, ultraviolet absorption spectroscopy, Fourier infrared spectroscopy, and X-ray diffraction.
RESULTS The best inclusion process was that the ratio of β-CD to aromatic aqueous solution was 3∶100 (g·mL-1), the inclusion temperature was 50 ℃, and the inclusion time was 1 h. The average inclusion rate of the obtained inclusion compound was 80.84%, the drug loading was 8.63%, and the standard relation was 0.91. The results of thin-layer chromatography, ultraviolet, infrared spectroscopy and other characterization experiments showed that the volatile components in the aromatic aqueous solution successfully entered the β-CD cavity, and the inclusion complex was successfully prepared.
CONCLUSION The optimum inclusion process is stable and feasible, which can provide references for the preparation process of Cinnamomi Ramulus Formula Granules.