The invention provides a compound—ceftiofur acetoxyethyl ester and a preparation method thereof, that is, adding an esterification agent, such as 1-bromoethyl acetate, to an organic solvent from ceftiofur or its sodium salt Steps for obtaining ceftiofur acetoxyethyl ester. The compound, ceftiofur acetoxyethyl ester, has better absorption in the gastrointestinal tract of animals than ceftiofur or its sodium salt, and has the characteristics of high bioavailability, and can be used for the treatment or prevention of pigs, poultry, cattle, The application of drug-resistant Staphylococcus aureus and Gram-negative bacteria in the digestive tract, respiratory tract, and genitourinary tract infection of animals such as sheep and dogs. Bacillus, Pasteurella, etc.