Preparative Technique And In Vitro Evaluation Of Nano Cefquinome Sulfate Transdermal Delivery System

Cefquinome sulfate as the fourth generation cephalosporins, with a broad-spectrum antimicrobial, antibacterial activity is suitable for parenteral administration advantages. However, because of the fat-soluble compounds, the development of suspension injection is low bioavailability and onset slowly. Because of its larger particle size, transdermal topical formulations and efficacy difference is low. Transdermal delivery system (TTS) is the way of administration of transdermal drug that absorbed through the skin into the systemic circulation for achiving the effective blood concentration and achiving to treat and prevent disseases cows suffering from mastitis is rich in blood vessels, so it is suitable for transdermal drug delivery, and the smaller size of fat-soluble drugs is likely to improve the transdermal efficiency. Based on the above ideas, this issue using anti-solvent recrystallization of cefquinome sulfate to prepare nano cefquinome sulfate, prepared the cream that is easy to use and stability. Then we evaluate the transdermal and curative effect of nano cefquinome sulfate cream.The main research topics and findings are as follows:1 Designed negative pressure in the anti-solvent recrystallization test equipment that has a negative pressure system, injection system and response system system..2 Optimized by orthogonal design, we get the optimum conditions of nano-quinoline sulfate oxime cephalosporin anti-solvent recrystallization.that is the concentration of cefquinome sulfate is 200 mg·mL-1, the volume ratio is 5, the reaction time is 45 min and concentration dropping is 15 ml·min-1. Analysis showed that the process parameters influcing the quality of cefquinome sulfate is concentration, reaction time, volume ratio and dropping.3 We get the size of 394.5 nm through negative pressure anti-solvent recrystallization of the pilot study under the best conditions, and the yield was 72% that is consistent with the small test results.4 We conduct the Scanning electron microscopy, Laser particle size, Differential thermal analysis, X-ray diffraction and Fourier transform infrared spectroscopy analysis of the nanostructured cefquinome sulfate and conclusive evidence of anti-solvent recrystallization treatment reduced the particle size of cefquinome sulfate, made the amorphous powder component to increase, the crystallinity decreased and while the chemical structure has not changed.5 Nano cefquinome sulfate as raw materials, the cream formulation was prepared and conducted in vitro penetration test. The results showed that:the original cefquinome sulfate powder in the 0-12 h were not through the cortex, while the nano- cefquinome sulfate solution 0.5 h start to cross the leather, cream from 1 h begin to cross. Total volume of through the leather per unit basically consistent with the linear relationship.6 Nano cefquinome sulfate was carried the clinicall test of milk and the residue in milk. The results showed that:cow diseases are significantly improved for using nanometer cefquinome sulfate cream of 3.5 days. The residual cefquinome sulfate is essentially undetectable after metabolism of 2 days.Above the experimental study, nano cefquinome sulfate was testified having good efficacy. While shorter in the body's metabolic cycle, and easy to use, stable performance. We provide the experimental basis for further explore the form of the preparation in vivo pharmacokinetics, bioavailability and early treatment.