Preparation And Pharmacokinetic Study Of Florfenicol Disintegrating Tablets

Florfenicol was developed by schering-plough in the United States,which was an antibiotic used to treat respiratory diseases,caused by bacteria and the therapeutic.But there aren't dosage forms for pet in the market;it limits the clinical application of the florfenicol in pets.In order to provide a new florfenicol formulation for pets,this study based on the improvement of the dissolution rate of florfenicol and prepared florfenicol rapidly disintegrating tablets,and studied the prescription,technology,quality and bioavailability of the fluorfenicol,and laid the foundation for the clinical use of florfenicol in pet clinic.In order to improve the solubility of florfenicol,we prepared florfenicol solid dispersion before made into tablets.And dissolution results showed that the solid dispersion is faster than the raw.We got the optimal composition of the florfenicol rapidly disintegrating tablets by single factor and orthogonal experiments,the optimal composition:50g florfenicol,100g PVPk30,56g MCC102,28g T80 lactose,9g micro-silica gel,27g PVPP,20g tartaric acid and10g soda were suppressed 1000 slices.In addition,the research to physical stability of florfenicol rapidly disintegrating tablets showed that appearance and shape,disintegration time,hardness and brittleness were all in accordance with the requirements of pharamacopoly.Influence factor test results showed that rapidly disintegrants tablets were stability in high temperature and strong light conditions but with strong wetting property,it is necessary to consider the packing of materials with stronger moisture resistance.Finally,we compared the pharmacokinetic of rapidly disintegrating tablets and ordinary tablets in dogs.Pharmacokinetic results showed that the florfenicol rapidly disintetrants tablets were absorbed quickly by oral administration with short T_max,and the pharmacokinetic of florfenicol in dogs is consistent with the characteristics of 1st absorption mathematical model.The pharmacokinetic parameters of rapidly disintetrants tablets was AUC_?0-t?=?15.998±5.026?mg/L*h,T_max=?0.917±0.204?h,C_max=?7.942±0.394?mg/L.The pharmacokinetic parameters of conventional tablets was AUC_?0-t?=?10.756±0.967?mg/L*h,T_max=?1.5±0.001?h,C_max=?5.771±0.444?mg/L.This study prepared florfenicol rapidly disintetrants tablets by direct powders compression,and the optimal composition of the florfenicol rapidly disintegrating tablets was got by single factor and orthogonal experiments.The tablets significantly increased the dissolution of florfenicol in water and greatly improved the pharmacokinetic characteristics of florfenicol in dogs.