伏立康唑磺丁基醚-β-环糊精包合物滴眼液的制备及质量考察  

Preparation and Quality Evaluation of Eye Drop Containing Voriconazole Sulfonated Butyl Ether-β-Cyclodextrin Inclusion Compound

作　　者：宋玲[1] 胡拥军[1] 张霁霁 

机构地区：[1]湖北省妇幼保健院药剂科,武汉430070 [2]荆州市第一人民医院

出　　处：《中国药师》2017年第10期1753-1755,共3页China Pharmacist

摘　　要：目的:制备1%伏立康唑(VCZ)磺丁基醚-β-环糊精(SBE-β-CD)包合物滴眼液,并对其质量进行考察。方法:按摩尔比1∶1制备VCZ SBE-β-CD包合物,以氯化钠为渗透压调节剂,苯扎溴铵为防腐剂制备VCZ SBE-β-CD包合物滴眼液,并对其性状、pH、含量、稳定性及刺激性进行考察。结果:本品为无色透明液体,3批样品的pH为6.44±0.20,6.50±0.15,6.48±0.22,渗透压为(320±4.62),(316±2.88),(322±2.60)MOsm,VCZ平均含量为1.02%(g·ml^(-1)),加速试验及长期试验中本品各项指标均无明显变化,对家兔眼无明显刺激。结论:VCZ SBE-β-CD包合物滴眼液具有主药含量高、质量稳定、眼用安全等特点,值得进一步研究。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 1 ：1. 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 ＆#183;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.

关 键 词：伏立康唑 磺丁基醚-Β-环糊精 包合物 滴眼液 制备 质量评价 

分 类 号：R944.9[医药卫生—药剂学]