氟苯尼考-β-环糊精包合物的制备、表征与大鼠药代动力学研究  

Preparation,characterization,and pharmacokinetic study of the inclusion complex of florfenicol-β-cyclodextrinsin rats

作　　者：嵇欣雨 魏霞丽 练婷婷 金庆日 JI Xinyu;WEI Xiali;LIAN Tingting;JIN Qingri(School of Pharmacy,Hangzhou Medical College,Linan Zhejiang 311399,China)

机构地区：[1]杭州医学院,浙江临安311399

出　　处：《延边大学农学学报》2024年第2期45-52,共8页Journal of Agricultural Science Yanbian University

基　　金：杭州医学院“求真人才工程”(00004F1RCYJ2202)。

摘　　要：氟苯尼考(Florfenicol,FF)是一种动物专用的酰胺醇广谱抗生素。室温下,氟苯尼考在水中的溶解度很低,严重限制了其广泛应用。为提高氟苯尼考的溶解度,该试验采用饱和水溶液法制备氟苯尼考-β-环糊精包合物,以包封率和产率作为评价指标,通过正交试验筛选出最佳处方。该试验采用X射线衍射(X-ray diffraction,XRD)、扫描电子显微镜(Scanning electron microscope,SEM)和傅里叶变换红外光谱(Fourier transform infrared spectroscopy,FT-IR)对处方进行表征。结果表明:最佳处方为氟苯尼考与β-环糊精的比例为1:3、温度70℃、搅拌时间1.5 h;氟苯尼考-β-环糊精包合物的包封率和产率分别为91.30%和90.48%;通过XRD、SEM和FT-IR表征,证明该包合物成功制备;在溶出度实验中,氟苯尼考-β-环糊精包合物的累积溶出率高于氟苯尼考原料药和物理混合物;与原料药相比,氟苯尼考-β-环糊精包合物的达峰浓度(Maximum drug concentration,Cmax)、达峰时间(Maximum time,tmax)和药时曲线下面积(Area under the concentration-time curve,AUCall)均显著增加(P<0.05)。综上说明β-环糊精提高了氟苯尼考的体内吸收率和生物利用度。该试验将为开发氟苯尼考-β-环糊精包合物在家畜灌服给药方面提供新的方法。Florfenicol(FF)is an animal-specific amphenicol broad-spectrum antibiotic.At room temperature,the solubility of florfenicol in water is very low,which severely limits its wide application.In order to improve the solubility of florfenicol,the saturated aqueous solution method was used to prepare the inclusion complex of florfenicol-β-cyclodextrin,and the inclusion rate and yield were used as evaluation indices to screen the best prescription through orthogonal testing.The prescriptions were characterized by X-ray diffraction(XRD),scanning electron microscopy(SEM)and Fourier transform infrared spectroscopy(FT-IR).The results indicated that the optimal formulation was florfenicol withβ-cyclodextrin at a ratio 1:3,with a temperature of 70℃and stirring time of 1.5 h.The inclusion rate and yield of florfenicol-β-cyclodextrin inclusion complex were 91.30%and 90.48%,respectively.XRD,SEM and FT-IR characterization proved that the inclusion complex was successfully prepared.In the dissolution experiment,the cumulative dissolution rate of florfenicol-β-cyclodextrin inclusion complex was higher than that of florfenicol raw drug and physical mixture.Compared with the API,the maximum drug concentration(C_(max)),maximum time(t_(max))and area under the concentration-time curve(AUC_(all))of the florfenicol-β-cyclodextrin inclusion complex were significantly increased(P<0.05).In summary,β-cyclodextrin can improve the absorptivity and bioavailability of florfenicol in vivo.This trial will provide a new method for development of florfenicol-β-cyclodextrin inclusion complex in livestock oral administration.

关 键 词：氟苯尼考 Β-环糊精 包合物 生物利用度 药代动力学 

分 类 号：R961[医药卫生—药理学]