| Florfenicol, is a broadspectrum that is effective against many Gram-positive and Gram-negative organisms. Also it does not cause a dose-related, reversible bone marrow suppression or irreversible aplastic anemia. However, it has very low water solubility. Therefore, there is a need for more water-soluble form of florfenicol.Florfenicol sulfonate, which provides a water-soluble form of florfenicol that has substantially greater aqueous solubility than florfenicol itself. Preferably a water soluable form of florfenicol of the present invention is also a prodrug that rapidly and efficiently converts to florfenicol in vivo. A method to detect florfenicol sulfonate in broiler chickens plasma and tissues by high performance liquid chromatographic (HPLC) with ultra violet detector was developed to analysis the pharmacokinetics paremeters and residue of florfenicol sulfonate in this paper.1The pharmacokinetics of florfenicol sulfonate in broiler chickens tissuesSPE-HPLC method to be established to determine of florfenicol sulfonate in broiler chickens plasma and study the pharmacokinetics. Twelve broiler chickens were used to give of florfenicol sulfonate by single intramuscular administration at a dosage of20mg·kg-1. After extracted with ethyl acetate, florfenicol sulfonate concentration of preparation samples were determined by HPLC/UV with solid phase extraction method. C18was used as the reversed column, and water (ultrapure water):acetonitrile (73:27V/V) as the mobile phase.The concentration-time curve were analyzed with3P97computer program. In present studies, the standard curves for florfenicol was linar in a range of0.25～25, r=0.9993, the detect limit was0.05μg·mL-1. Adding0.5,5and25florfenicol into blank plasma, the recovery rate were86.89±0.01%,88.02±0.02%,86.37±0.01%respectively. The coefficient of within variation was2.08%,4.99%,2.39%, the coefficient of between variation was6.28%,7.49%,6.58%respectively. The results suggested that the kinetics of the injection is fit to one compartment model with first order absorption. The main parameters of florfenicol sulfonate were as follows:T1/2kα:(0.28±0.04)h, T1/2Ke: (2.06±0.06)h, Cmax:(4.17±0.12)μg·mL-1, Tpeak:(0.92±0.09)h, AUC:(16.89±0.35)μg· mL-1·h, V/F(c):(3.52±0.13)L·kg-1, CL/F(s):(1.19±0.03)L·kg-1·h-1, Ke:(0.34±0.01)h-1, ka:(2.57±0.37)h-’, A:(6.56±0.38)uμg·L-1. The results showed that the distribution of florfenicol sulfonate was rapid and wide in the broiler chickens, the concentration of plasma was high and elimination was quick.2The residues of florfenicol and florfenicol amine in broiler chickens tissuesThis experiment was conducted to study the residues of florfenicol and florfenicol amine in broiler chickens. Fourty healthy broiler chickens were used to give florfenicol sulfonate by intramuscular administration for three days at the dosage of20mg·kg-1.Tissue samples including muscle, liver, kidney and skin with fat were collected at different intervals after the last administration. The concentration of florfenicol and florfenicol amine were both well lined within20μg·kg-1～500μg·kg-1in all tissues. Three concentration levels (40μg·kg-1,200μg·kg-1,1000μg·kg-1) of florfenicol and florfenicol amine in the blank tissues were analysed. The average recoverys of FF and FFA were85.2%,85.18%,82.46%,83.86%and83.65%,82.34%,83.63%,84.26%in muscle, liver, kidney, skin with fat respectively. The intra-day coefficients of variation was from1.34%to6.57%. The inter-day coefficients of variation was from1.27%to8.30%. The results showed that the concentration of florfenicol and florfenicol amine in muscle, kidney, skin&fat was declined to lower than LOD level at the7th. At the9th the concentration of florfenicol and florfenicol amine in liver were under the limit of detection. According to the MRLs standards and the result, a five-day of withdrawal time was recommended. |
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