Enhancement of dissolution rate and oral bioavailability of poorly soluble drug florfenicol by using solid dispersion and effervescent disintegration technology

被引:1
|
作者
Li, Chao [1 ]
Li, Nanxin [1 ]
Chen, Xingyu [1 ]
Li, Xiaojuan [1 ]
Liu, Chang [1 ]
Abbas, Awn [1 ]
Wang, Yueli [1 ]
Qi, Shuangcai [1 ]
Zhang, Yifan [1 ]
Li, Dongbo [1 ]
Zhang, Wei [1 ]
Shu, Gang [1 ]
Lin, Juchun [1 ]
Li, Haohuan [1 ]
Xu, Funeng [1 ]
Peng, Guangneng [1 ]
Fu, Hualin [1 ]
机构
[1] Sichuan Agr Univ, Coll Vet Med, Dept Pharm, Chengdu, Peoples R China
关键词
Florfenicol; Solid dispersions; Effervescent tablets; Fast disintegrating tablets; Pharmacokinetics; DIRECT COMPRESSION; CASSIA-FISTULA; IN-VITRO; SOLUBILITY; RELEASE; TABLETS; MECHANISM; IMPROVE; POLYMER; AGENT;
D O I
10.1080/03639045.2023.2295488
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Objective Florfenicol(FF) is an excellent veterinary antibiotic, limited by poor solubility and poor bioavailability.Significance Here in, we aimed to explore the applicability of fast disintegrating tablets compressed from Florfenicol-loaded solid dispersions (FF-SD-FDTs) to improve the dissolution rate and oral bioavailability of Florfenicol.Methods Utilizing selecting appropriate preparation methods and carriers, the solid dispersions of Florfenicol (FF-SDs) were prepared by solvent evaporation and the fast disintegrating tablets (FF-SD-FDTs) were prepared by the direct compression (DC) method.Results The tablet properties including hardness, friability, disintegration time, weight variation, etc. all met the specifications of Chinese Veterinary Pharmacopeia(CVP). FF-SD-FDTs significantly improved drug dissolution and dispersion of FF in vitro compared to florfenicol conventional tablets (FF-CTs). A pharmacokinetics study in German shepherd dogs proved the AUC(0-infinity) and C-max values of FF-SD-FDTs are 1.38 and 1.38 times more than FF-CTs, respectively.Conclusions Overall, it can be concluded that FF-SD-FDTs with excellent disintegration and dissolution properties were successfully produced, which greatly improved the oral bioavailability of the poorly soluble drug FF, and the study provided a new idea for a broader role of FF in pet clinics.
引用
收藏
页码:45 / 54
页数:10
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