| Florfenicol?FF?,a new broad-spectrum chloramphenicol antibiotics made chemical synthesis,had been specially for veterinary.This medicine was popular with veterinary service at home and abroad for wide antimicrobial spectrum,safe and efficient,widely distributed in the body,without the potential cause of aplastic anemia and so on.Florfenicol had come into the market in many countries to treat the disease of swine,cattle,other livestock and poultry and fish,including injections,premix and powder and so on.Florfenicol was used for preventing bacteria of swine,poultry and fish in our country.To improve the water solubility of florfenicol,water-soluble florfenicol powder was prepared by inclusion technology with?-cyclodextrin.Taking inclusion rate and the yield of inclusion complex as evaluation indexes,the best inclusion process was screened by orthogonal experiments,the inclusion complex was identified by differential scanning calorimetry analysis?DSC?,fourier transform infra-red spectroscopy?FTIR?,scanning electron microscopy?SEM?.The results showed that the optimum preparation conditions were florfenicol:?-cyclodextrin=1:1?mole ratio?,the inclusion temperature was 80?,the inclusion time was 2 hours and the stirring speed was 500r/min;differential scanning calorimetry analysis?DSC?,fourier transform infra-red spectroscopy?FTIR?and scanning electron microscopy?SEM?showed that florfenicol-?-cyclodextrin inclusion complex had formed;The inclusion ratio of florfenicol-?-cyclodextrin inclusion complex was 91.85%and the yield of florfenicol-?-cyclodextrin inclusion complex was 91.26%,the dissolution rate of florfenicol-?-cyclodextrin was 100%in 15 minutes which was five times as much as florfenicol crude drug.In this paper,a method based on high-performance liquid chromatography?HPLC?was developed for detecting florfenicol and inclusion complex in plasma of tilapia.By using this method,the pharmacokinetics studies were carried out in healthy tilapia after single dose oral administration at 20±1?.In this method,ethyl acetate was used as extraction solvent,and the residue is defatted with n-hexane.The HPLC system used was the Island fluid chromatography?LC-15C?series equipment,detection of florfenicol was performed on th variable wavelength detector at 224nm,the column temperature is 25?and the fiow rate was 1.0 mL/min.The mobile phase is acetonitrile-sodium phosphate buffer?33/67,V/V?solution.The results showed that the standard curves were linear at 0.025?g/mL10.00?g/mL of fiorfenicol.The average recovery of florfenicol in plasma was 98.41±0.54%106.08±2.49%.The limit of quantitation for florfenicol were 0.015?g/mL in plasma.The variation coefficients within a day was less than 2%and between days was less than 10%.Consequently,this method can be used to detect simultaneously the concentration of florfenicol in tilapia plasma.By using this method,the pharmacokinetics studies were carried out in tilapia after single dose oral administration at 20±1?.The weight of chosen tilapia was 350±30g and the does of drug was 15 mg/kg.The concentration-time data were analyzed by the winnolin5.2software.The result of single dose oral administration of florfenicol inclusion complex was:the area under the serum concentration-time cuve?AUC?was 1.6546??g/mL?*h.The distribution volume?V/F?of florfenicol was computed as 247485.9057mL/kg.The total clearance of florfenicol?CL/F?was estimated to be 9065.4279mL/h/kg.The time-point of maximum plasma concentration of the drug(Tmax)and the maximum plasma concentration(Cmax)were caluculated as 7h and 0.1401?g/mL.The area under the serum concentration-time curve?AUC?was 1.7906??g/mL?*h.The distribution volume?V/F?of florfenicol was computed as 52425.2072mL/kg.The total clearance of florfenicol?CL/F?was estimated to be 8376.8671mL/h/kg.The time-point of maximum plasma concentration of the drug(Tmax)and the maximum plasma concentration(Cmax)were caluculated as 13h and 0.1858?g/mL.The results showed that florfenicol inclusion complex can quickly be absorbed in the tilapia,can play pharmacological effects faster. |
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