Betadex Sulfobutyl Ether Sodium promotes the development of new drug voriconazole eye drops

On September 15, the State Drug Administration issued a drug clinical trial approval notice to voriconazole eye drops independently developed by Shenyang Xingqi ophthalmic Co., Ltd., agreeing to carry out clinical research on fungal keratitis.

Voriconazole is a new triazole spectrum antifungal drug developed by Pfizer. In recent years, voriconazole has successfully cured keratitis caused by Aspergillus, Fusarium and Candida. Its oral bioavailability is high, and its penetrating power is strong. It can reach the experimental therapeutic concentration in plasma, aqueous humor and vitreous in vitro. Prospective clinical studies showed that 1% voriconazole eye drops showed strong tissue penetration and high bioavailability, and could reach a high drug concentration in aqueous humor and vitreous body. The concentration of drug substances in aqueous humor exceeded the minimal inhibitory concentration (MIC) 90 of most sensitive fungi.

However, we should pay attention to the stability of voriconazole eye drops while focusing on the clinical efficacy of topical application of voriconazole eye drops. Shandong Binzhou Zhiyuan Biotechnology Co., Ltd. produces a new type of excipient - sodium sulfobutyl betahydrodextrin (SBE β CD). It is a sodium salt alkylated by 1,4-butanesulfonic lactone under alkaline conditions. It is an anionic, high water-soluble beta cyclodextrin derivative. It can form non covalent complexes with drug molecules, so as to improve the stability, water solubility and safety of drugs, reduce the nephrotoxicity, alleviate the hemolysis of drugs, control the drug release rate, and cover up the bad smell. It can be widely used in injection, oral, nasal and eye preparations. The application of SBE β CD in ophthalmic drugs mainly aims to increase the solubility and stability of poorly water-soluble drugs and reduce the irritation to cornea. It not only increases the solubility of voriconazole, but also improves the clinical characteristics of eye drops. Moreover, 5% ~ 15% SBE β CD has been successfully used in ocular administration.