奈妥吡坦/β-环糊精包合物的制备、评价与表征.

Preparation of netupitant/茁-cyclodextrin inclusion compound, to improve the water solubility of netupitant. Netupitant/茁-cyclodextrin inclusion compound was prepared by saturated aqueous solution method; taking the drug load as the index, the impacts of mass ratio (core-wall ratio), coating temperature, coating time and stirring speed of netupitant and 茁-cyclodextrin were investigated. The optimal netupitant/茁-cyclodextrin inclusion compound was obtained based on the results of single factor experiment, orthogonal designed experiments were used to optimize the preparation formula and process, and the encapsulation rate, drug loading capacity and stability were evaluated in vitro. Fourier transform infrared spectroscopy (FTIR) and X-ray powder diffraction (XRD) were used to characterize the optimal netupitant/茁-cyclodextrin inclusion compound. The optimal preparation conditions for the netupitant/茁-cyclodextrin inclusion compound are as follows: core-wall ratio 1:20, coating temperature 40℃, coating time 20 min, stirring speed 150 r/min. Under these conditions, the drug loading capacity of the netupitant/茁-cyclodextrin inclusion compound was 4.73 %, the inclusion rate was 94.8%, and the stability in aqueous solution was good. Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis proved the successful preparation of netupitant/茁-cyclodextrin inclusion compound. Netupitant/ 茁-cyclodextrin is successfully prepared, and the water solubility of netupitant increases by more than 1500 times, which provides an experimental basis for the development of new water-soluble pharmaceutics of netupitant. [ABSTRACT FROM AUTHOR]