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目的:制备伏立康唑(VCZ)磺丁基醚-β-环糊精(SBE-β-CD)包合物,并对其性质进行考察。方法:分别采用搅拌法、超声法及研磨法制备VCZ SBE-β-CD包合物,以包合率及包合物收率为考察指标筛选出最佳的方法,采用正交试验进一步优化其处方及制备工艺,差示扫描量热技术及溶解度法进行性质验证,并考察其体外溶出特性。结果:搅拌法的包合率及包合物收率最高,优化的最佳工艺及处方条件为:包合温度为25℃,搅拌时间为4 h,VCZ与SBE-β-CD的质量比为1∶1。优化后的包合物包合率为(86.14±0.69)%,包合物收率为(97.11±0.31)%;包合后,VCZ的特征峰消失,溶解度显著增加,与VCZ相比,包合物中的药物溶出度速度及溶出量显著增加。结论:用搅拌法成功制备了VCZ SBE-β-CD包合物,为VCZ滴眼剂的研究奠定了试验基础。
OBJECTIVE: To prepare the inclusion compound of voriconazole (VCZ) sulfobutyl ether-β-cyclodextrin (SBE-β-CD) and investigate its properties. Methods: VCZ SBE-β-CD inclusion complex was prepared by stirring method, ultrasonic method and grinding method respectively. The best method was selected by using the inclusion rate and the inclusion compound yield as the investigation index. The orthogonal test was used to further optimize Prescription and preparation process, differential scanning calorimetry and solubility method to verify the nature, and investigate its in vitro dissolution characteristics. Results: The inclusion rate and the yield of inclusion compound were the highest. The optimum conditions were as follows: the inclusion temperature was 25 ℃, the stirring time was 4 h, the mass ratio of VCZ to SBE-β-CD was 1: 1. The inclusion rate of inclusion complex was (86.14 ± 0.69)% and the yield of inclusion complex was (97.11 ± 0.31)%. After inclusion, the characteristic peak disappeared and the solubility of VCZ disappeared significantly. Compared with VCZ, The drug dissolution rate and dissolution in the compound increased significantly. CONCLUSION: VCZ SBE-β-CD inclusion compound was successfully prepared by stirring method, which laid the foundation for the study of VCZ eye drops.