摘要
目的:对伏立康唑磺丁基醚-β-环糊精(VCZ SBE-β-CD)包合物滴眼液在家兔眼内的药动学进行研究。方法:选取54只健康家兔按数字法随机分为3组,分别双眼单次给予0. 5%伏立康唑(VCZ)滴眼液,0. 5%VCZ SBE-β-CD包合物滴眼液,1. 0%VCZ SBE-β-CD包合物滴眼液。在预设的时间点各组取2只家兔处死后检测房水及角膜中的VCZ,绘制药-时曲线,并利用DAS2. 0版软件拟合隔室模型,并得到主要的药动学参数。结果:家兔眼单次给药后,3种制剂在兔眼房水及角膜中的药动学均符合二室模型。与0. 5%VCZ滴眼液相比,VCZ SBE-β-CD包合物滴眼液在房水及角膜中的达峰时间滞后,峰浓度显著增加,并呈现较好的长效性。与0. 5%VCZ SBE-β-CD包合物滴眼液相比,1. 0%VCZ SBE-β-CD包合物滴眼液具有更高的峰浓度。结论:VCZ SBE-β-CD包合物滴眼液可以显著提高VCZ在眼部的吸收,并明显延长作用时间。
Objective： To study the pharmacokinetics of eye drop containing voriconazole sulfonated butyl ether-β-cyclodextrin （VCZ SBE-β-CD） inclusion compound in rabbits. Methods： Totally 54 healthy rabbits were divided into 3 groups randomly and given 0.5% VCZ eye drop, 0.5% VCZ SBE-β-CD inclusion compound eye drop and 1.0% VCZ SBE-β-CD inclusion compound eye drop, respectively. At the predetermined time, 2 rabbits from each group were sacrificed and the VCZ contents in aqueous humor and cornea were detected. The curves of drug concentration-time were drawn, and the main pharmacokinetic parameters were calculated by DAS2.0 software. Results： After the single dose, the changes of VCZ concentration for the three eye drops in aqueous humor and cor- nea fitted two-compartment models. The Tmax of two VCZ SBE-β-CD inclusion compound eye drops was delayed significantly and the Cmax increased notably when compared with that of 0.5% VCZ eye drop. Meanwhile, two VCZ SBE-β-CD inclusion compound eye drops showed obvious prolonged-release property. The Cmax of 1. 0% VCZ SBE-β-CD inclusion compound eye drop was high than that of 0.5% VCZ SBE-β-CD inclusion compound eye drop. Conclusion： VCZ SBE-β-CD inclusion compound eye drops can enhance the eye absorption of VCZ and prolong the effect significantly.
作者
宋玲
胡拥军
Song Ling;Hu Yongjun(Department of Pharmacy,Hubei Maternal and Child Health Hospital,Wuhan 430070,China)
出处
《中国药师》
CAS
2018年第11期1946-1949,共4页
China Pharmacist
关键词
伏立康唑
磺丁基醚-Β-环糊精
包合物
药动学
家兔
Voriconazole
Sulfonated butyl ether-β-cyclodextrin
Inclusion compound
Pharmacokinetics
Rabbits
