Compositions containing prodrugs of florfenicol and methods of use
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Abstract
The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one embodiment the prodrug is an esterized form of florfenicol. Examples of suitable prodrugs include one or a combination of one or a combination of the following: florfenicol acetate, florfenicol propionate, florfenicol butyrate, florfenicol pentanoate, florfenicol hexanoate, florfenicol heptanoate, florfenicol octanoate, florfenicol nanoate, florfenicol decanoate, florfenicol undecanoate, florfenicol dodecanoate, and florfenicol phthalate. In another embodiment the prodrug is converted into the florfenicol in vivo by the action of one or more endogenous esterases. The invention also provides new compounds, pharmaceutical compositions containing the compounds, and methods for their administration.
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Citations
42 Claims
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1-24. -24. (canceled)
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25. A method of treating a bacterial infection in a bovine comprising administering to the bovine a composition comprising a florfenicol ester and a pharmaceutically acceptable solvent wherein
the florfenicol ester is selected from the group consisting of florfenicol acetate, florfenicol propionate, florfenicol butyrate, florfenicol pentanoate, florfenicol heptanoate, florfenicol octanoate, florfenicol nanoate, florfenicol decanoate, florfenicol undecanoate, and florfenicol dodecanoate; -
the bacterial infection is susceptible to florfenicol; and
the composition is administered as a single injection in an amount sufficient to treat the infection without requiring a second injection. - View Dependent Claims (26, 27, 28, 29, 30, 31, 32, 33, 34, 37, 38, 39, 40)
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41. The method of claim 45, wherein
the florfenicol ester is florfenicol butyrate, the administering is intramuscular injection, the administering provides a serum concentration of florfenicol in the bovine that is higher three days after administration than the serum concentration that would be obtained if the bovine was administered a single injection of a comparative composition at a dose of 20 mg/kg, wherein the comparative composition contains 300 mg of florfenicol, 250 mg N-methyl-2-pyrrolidone, 150 mg propylene glycol, and sufficient polyethylene glycol to provide 1 mL of the comparative composition, and the administering provides a Cmax for the concentration of florfenicol in the bovine that is lower than the Cmax that would be obtained if the bovine was administered the comparative composition at a dose of 20 mg/kg.
Specification