Preparation And Efficacy Evaluation Of Amoxicillin&Sulbactam Sodium Nanoemulsion

Objective:The present studied the preparation of amoxicillin (AMX)&sulbactamsodium (SBT) nanoemulsion,evaluated the quality, stability, security, and the antibacterialefficacy in vitro, it was a suggestion to the treatment of dairy cow mastitis withAMX-SBT-NE.Methods:(1) The compositon of amoxicillin&sulbactam sodium nanoemulsion wasthrough pseudo-ternary phase diagram under the stable nanoemulsion, the ratio of amoxicillinto sulbactam sodium was confired by antibacterial test,the constructure dropset was evaluatedby the dyeing method, transmission electron microscopy (TEM) and laser particle sizeanalyzer.it was also comfird the stable and long-term issue of AMX-SBT-NE(2)The drugcontent was resumed by high-performance liquid chromatography (HPLC),the standard curvefor amoxicillin and sulbactan sodium were gained respectively;(3) The drug safety wasevaluation with acute toxicity test and skin irritation test.(4) The antibacterial test in vitroabout AMX-SBT-NE was experience with Escherichia coli,Staphloclccus aureus,Streptococcus agalactiae, as the common pathogenic bacteria of dairy cow mastitis,thestandard for the test were the minimum bacteriostasis concentration (MIC) and minimumbactericidal concentration (MBC) for three kinds of bacteria.Results:(1) The composition of AMX-SBT-NE was1%to amoxicillin,0.5%tosulbactam sodium,2.5%to cinnamaldehyde,6.25%to PEG400,18.75%to RH-40, and71.5%to distilled water (the above components are quality score) as oil-in-watermicroemulsions, cinnamic aldehyde was oil phase, polyoxyethylene hydrogenated castor oilmixed with polyethylene glycol400was surfactant (Km3:1),the nanoemulsion was spherical,the dropset was13.41nm, dispersion coefficient (PDI) was0.188.the nanoemulsion was goodappearance clear uniform and physical stability.And sodium the bacteriostatic effect was bestat amoxicillin and sulbactam sodium2:1.the longterm of AMX-SBT-NE was about20months;(2) The method for the determination of content of AMX-SBT-NE was HPLC,chromatographic column was Diamond C18column (250mm×4.6mm,5microns), mobilephase was acetonitrile-water-phosphate buffer, detection wavelength was220nm.Amoxicillin was good linear relationship (r=0.9990) in rang from40μg/ml to400μg/ml,the recovery rate was99.9%, RSD was0.52%.Sulbactam sodium was good linear relationship (r=0.9998) in rang from20μg/ml to200μg/ml,the recovery rate was99.9%, RSD was0.66%.AMX was good with the precision, RSD of with-in-day precision was1.33%, RSD ofday-to-day precision was2.06%.SBT was good with precision, RSD of with-in-day precisionwas1.28%, RSD of day-to-day precision was2.31%(3) Safety testing of AMX-SBT-NE wastested, the maximum tolerance of mice was0.35ml/10g BW, the maximum tolerance ratiowas654times. skin irritation test was showed that AMX-SBT-NE was free of stimulationintensity and without excitant;(4) The antibacterial effect of AMX-SBT-NE on three kinds ofbacteria, staphylococcus aureus, streptococcus pneumoniae and Escherichia coli was thatMIC was3.12μg/ml,3.12μg/ml and6.25μg/ml respectively and it was differencesignificantly compared to crude drug (P <0.01).the MBC were6.25μg/ml,12.5μg/ml and12.5μg/ml, and the MBC was significantly differences comparaed to crude drug (P <0.01).Conclusion: The AMX-SBT-NE was of physical stability, the content determinationmethod was of high precision repeatability,the AMX-SBT-NE was quaried for drug safetyrequirements, in vitro it was good antibacterial effect on main pathogenic bacteria of dairycow mastitis.