| Flufenicol is a broad-spectrum antibiotic for amidol animals.It is mainly used for respiratory,urinary and digestive tract diseases caused by sensitive bacterial infections.In this study,florfenicol double suspension emulsion oral liquid was prepared by using the combination of emulsion and suspension preparation technology.The quality evaluation,stability evaluation and target animal pharmacokinetic study of the preparation were carried out to provide the basis for the application of the preparation in veterinary clinic.1.Preparation and quality evaluation of florfenicol double suspension emulsion oral liquid:Centrifugation,solubility,sedimentation volume ratio and high temperature were used as evaluation indexes,and the optimum technological conditions were screened by single factor investigation and orthogonal test.Results:The excipients were 40%soybean oil for injection,6.4%emulsifier,0.3%water phase stabilizer,1%oil phase stabilizer,14%oil phase fluorobenicol and 7%water phase fluorobenicol.The technological conditions were as follows:suspended water phase temperature 60?,suspended oil phase temperature 70?,colloid milling emulsification time 20 min.The 20%florfenicol double suspension emulsion oral liquid is milky white and oil emulsion with an average particle size of 5.15±0.7?m and a normal distribution with a pH value of 5.2±0.2 and good stability.2.Study on the stability of florfenicol double suspension emulsion oral liquid:through the influencing factors test,accelerated test,long-term test and water solution stability test,the content,properties,pH value were taken as the evaluation index.The results showed that both light and temperature had certain effects on the oral solution of florfenicol double suspension.The content of the sample decreased slightly,the character changed little,the pH value decreased,the stability and dispersion uniformity of the aqueous solution were good,and the content distribution of the aqueous solution remained unchanged for at least 24 hours at room temperature and 4?at low temperature,while the content distribution of the aqueous solution changed slightly at 50?.3.A method for the determination of florfenicol in chicken plasma by high performance liquid chromatography was established.The pharmacokinetics of florfenicol double suspension emulsion oral solution and florfenicol solution(fluxinkang)in chicken were compared.The results showed that the mobile phase was acetonitrile:water=26:74,florfenicol in the concentration range of 0.01 g/mL~30.0 g/mL,the linear equation was A=25229*C+4495.8,R~2=0.999(n=8),the minimum quantitative limit was 0.01 g/mL,the extraction recovery was between 87.1%and 107.9%,and RSD was less than 7.2.The main pharmacokinetic parameters of florfenicol double suspension emulsion oral solution and florfenicol solution(fluxinkang)after single dose of 3 mg/kg:Cmax were 1.85+0.69 mg/L and 2.43+1.62 mg/L respectively,Tmax were 1.93+1.25 h and 2.14+1.22 h,T1/2 were47.94+5.69 h and 5.69 h,36.54+15.08 h,AUC(0-24)were 22.9254±8.41 mg/L*h and39.54±7.09 mg/L*h,CL/F were 1.06725±0.60 L/h/kg and 0.81±0.18 L/h/kg,MRT were31.20±5.96 h and 30.29±7.36 h,Vd/F were 45.46±12.28 L/Kg and 37.75±17.7 L/Kg,AUC(0-?)were 34.49±8.18 mg/L*h and 34.15±2.66 mg/L*h.The results showed that the half-life of florfenicol double suspension emulsion oral liquid was longer than that of florfenicol solution(fluxinkang)in chicken than that of florfenicol solution(fluxinkang),which had a certain sustained-release and long-term effect,There was no significant difference in bioavailability. |
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