Preparation And Physical Property And Safety Evaluation Of Ceftiofur Sodium Liposomes

Liposomes as a drug carrier were encapsulating the ceftiofur sodium in the body lipid, with a view to improve the targeting of drugs to extend the effective plasma concentration time, to reduce the drug dosage and improve the therapeutic index. In this study, ceftiofur sodium liposomes were made up with the drug-containing of 1% by the reverse-phase evaporation method. Its physical and chemical properties were studied and irritated through intramuscular injection, intravenous injection of ceftiofur sodium liposomes to test its excitation to animals and vitro haemolyticus. A preliminary evaluation of clinical application for the ceftiofur sodium liposomes were introduced in this paper.In this study, the method of sephadex column chromatography-high-performance liquid chromatography (HPLC) to determinate the ceftiofur sodium liposome encapsulation efficiency was established, this method could accurately determinate the content of the ceftiofur sodium, and avoid interference, simple and feasible. Regression equation: Y=40598X-1085 (r=0.9999) . The average RSD of accuracy and recovery about the method was less than 1.0%.Taking the entrapment efficiency as the evaluation index,selecting reverse phase evaporation to prepare the ceftiofur sodium, and research the factors has a bearings on the encapsulation efficiency and stability of ceftiofur sodium liposome, such as the ratio of lipit, drug to lipid and organic phase to water phase. The best technology and prescription that the ceftiofur sodium liposome was preferred by orthogonal design.The mass ratio between yolk lecithin and cholesterin was 2: 1; the mass ratio between ceftiofur sodium and lipid were 1:8 and volume ratio between inorganic phase and organic phase were 1:3. when the pH was 6.5 and the temperature was 25℃, its encapsulation efficiency could reach up to 57.16±0.67% and the technology was steady.The quality assessment about ceftiofur sodium liposome were as follows: the color was jasmine by visual study and had no precipitate and impurity. The liposome was rounding and regular under the light microscope. Non-recovery of liposome could be destroyed in a high temperature and soon turned yellow and took on opacity as well as precipitate. Lamination phenomenon were taken place during 90d at 4℃. But it could be able to recover its original conditions when pendulating lightly.The result of safety evaluation were carrying out. using ceftiofur sodium liposome was safe, and no hemolysis happened. The results about musle irritation test and vascular irritation test were showed that ceftiofur sodium liposome was not clearly exitation and could be used intramuscular injection and intravenous drip.