Preparation and Properties of Mesalazine Hydroxypropyl-β-cyclodextrin Inclusion Complexes / 中国药师

ABSTRACT

Objective:To prepare mesalazine hydroxypropyl-β-cyclodextrin ( MSZ-HP-β-CD) inclusion complexes and observe the properties. Methods:The inclusion complexes were prepared by a stirring method and the content of MSZ was determined by HPLC. The preparation technology was optimized by orthogonal test with the inclusion rate and the yield of inclusion complexes as the indices. The inclusion complexes were identified respectively by ultraviolet ( UV) spectrometry, X-ray diffraction ( XRD) and solubility. The dissolution rate was investigated. Results: Using the stirring method, the optimum preparation process was as follows the inclusion temperature was 35 ℃, the ratio of MSZ to HP-β-CD was 1∶ 4 ( mg/g) , and the inclusion time was 3 h. The average inclusion rate of the complexes was 96. 28%, and the yield was 97. 87%. The identification results showed that the freeze-dried powder was inclusion complexes. Compared with that of MSZ, the dissolution of MSZ- HP-β-CD inclusion complexes was notably enhanced. Conclusion:The prepared MSZ-HP-β-CD with optimized technology has good reproducibility and stable technology, which can obviously improve the dissolution of MSZ.