Preparation and Quality Evaluation of Eye Drop Containing Voriconazole Sulfonated Butyl Ether-β-Cyclo-dextrin Inclusion Compound / 中国药师

ABSTRACT

Objective: To prepare 1% voriconazole ( VCZ) sulfonated butyl ether- β-cyclodextrin ( SBE-β-CD) inclusion com-pound eye drop and study the quality. Methods: VCZ SBE-β-CD inclusion compound was prepared with the molar ratio of VCZ to SBE-β-CD of 11. Sodium chloride was used as the osmotic pressure regulator and benzalkonium bromide was employed as the pre-servative in the preparation of VCZ SBE-β-CD inclusion compound eye drop. The appearance, pH value, content stability and irritation of the eye drop were studied as well. Results:The eye drop was colorless and transparent solution with the pH value of 6. 44 ± 0. 20, 6. 50 ± 0. 15,6. 48 ± 0. 22 the osmotic pressure of (320 ± 4. 62),(316 ± 2. 88),(322 ± 2. 60)MOsm and the VCZ content of 1. 02% g ·ml-1 . The results of accelerated testing and long-term testing showed no notable changes in the quality indices. The eye drop exhibi-ted no significant irritation to the rabbit eyes. Conclusion:VCZ SBE-β-CD inclusion compound eye drop shows the properties of high VCZ content, stable quality and promising safety in eye application, which is worthy of further studies.