Preparation And Pharmacokinetics Of Cefquinome Sulfate Injections

A new veterinary drug, cefquinome sulfate injection(CSI), was studied of prescription and production technique in the GMP workshop, and also valued the middle scale-production, stability, quality control and pharmacokinetics. The results as follow:1. Through studying the prescription and magnifying technology,the production technique of CSI was confirmed. Firstly,2500mL oil for injection was added in a clean steel barrel, after warmed to78～84℃,5g hydrogenated castor oil was added in and stirred to dissolve., then5g antioxidant1was joined to melt. Secondly, anthoer1000mL oil and250ml benzyl alcohol were added in the barrel. Thirdly, a big flask was put through2000mL oil and1.25Kg cefquinome sulfate, after stirred, the solution was made into quartering symmetrically, and gone into the cases of the ball. mill. The ball mill run30mintes, and the solution through granulation detdction was added in the barrel. The oil was added to50000ml. The whole solution was added into the cases of the ball mill and stirred10-20mintes. When the granulation detdction was finished, the stir procedure wa.s stop. The production was tested, loaded, examined by light, covered and packed.2. The CSI prodution from pilot-scale was tested of the constant temperature and constant humidity, light acceleration and long-term stability test. The results showed that CSI prodution was steady in the long-termed test at25℃, keeping from light.3. Pharmacokinetics of CSI was studied on pigs. The kinetic disposition followed a2-compartmental open model after a single intramuscle or intravenous. Intramuscle administration at2mg/kg b.w, the drug was absorbed rapidly, and obtained the peak value (3.86μg/L) after0.57h. The pharmacokinetic parameters of intramuscle and intravenous administration were as follows:the half time of distribution(t1/2)were0.93h and0.07h, the volume of distribution were0.16L/mL and0.17L/mL. After a single intramuscle administration, the plasma drug concentration remained above0.15ug/mL within6h and remained0.01μg/mL-0.02μg/mL within12h-16h. Because the MIC of cefquinome against susceptive bacillus is0.01μg/mL, the CSI intramuscle administration to treat the disease of pig respiratory was2mg/kg b.w..daily.To sum up. the priscription and technology of CSI was safe, effective, quality control, and adapted to pruduct in a GMP workshop and to use in market.