Studies On Berberine Hydrochloride Particles And Its Relevant Pharmacology

Berberine hydrochloride is a traditional antibiotics.It is restricted in their application in pig production because of its bitter taste.Objective of this study is to prepare berberine hydrochloride coated particles.The particles was prepared by the Fluidized Bed Spray using polyacrylic resin IV as coating material,and its standard for quality control was establish.Finally,the MIC of Berberine hydrochloride on common pathogens and the palatability of the particles were studied.1.Study on the effect of different adhesive,different material ratio and different coating gain on the appearance,hardness,particle size and dissolution of particles.The experimental results were that:best prescription was 5% polyvinylpyrrolidone as adhesive,microcrystalline cellulose(MCC) do excipients,starch do diluent,the rate of berberine hydrochloride:MCC:starch was 1:0.75:3.25.2.Study on the effect of atomization pressure,spouting velocity,inlet air temperature,air output and inlet wind humidity on the quality of coated particles,optimal process parameters.The experimental results were that: operating parameters of Fluidized Bed Spray were that throwing pill speed and air volume were:14.5 r/min and 27.5 m~3/h;coating liquid,cited wind frequency, rotating frequency,temperature and atomization pressure were 10 mL/min,20 HZ,4 HZ,55℃and 0.15 Mpa.The preparation process of the coated particles was simple,even particle size and easy for industrialization.It has a good application prospect.3.The standard for quality control was established by studying on the appearance,drug content,drug dissolution of the particles.The results showed that:Coated particles were yellow colour,strong hardness,good appearance and fluidity.Encapsulation efficiency was 90%-95%.At 37℃,coated particles were quickly released in pH2.0 solution with a total dissolution more than 80% in one hour,but they were sparely soluble in water.More than 80%particle size was in the range of 150-42 urn.4.According to the antibiotic susceptibility test in NCCLS,the mimimum inhibitory concentrations(MIC) of berberine hydrochloride on several strains were detected by micro-dilution.The experimental results were that:MIC of berberine hydrochloride on escherichia coli ranged in 512-1024μg/mL,MIC of berberine hydrochloride on salmonella ranged in 512-1024μg/mL; staphylococcus and pasteurellosis bacillus were more sensitive to berberine hydrochloride.MIC of berberine hydrochloride on staphylococcus, pasteurellosis bacillus and streptococcus were 256μg/mL,256μg/mL and 512μgmL respectively.5.HPLC determination of berberine hydrochloride in swine plasma had been developed.Average recoveries,recovery,detection limit and calibration curve were studied.The results showed that:this method is easy operation,and has well stability,high sensitivity and recovery,short detection time.The minimum detectable concentration of this method was 0.5μg/L.It can be used in pharmacokinetic research of berberine hydrochloride.6.Three health piglets were used in this test,were divided into 3 groups. The control group fed basic diet,groupⅠfed mixture of diet and berberine hydrochloride raw,groupⅡfed mixture of diet and berberine hydrochloride coated particles respectively,feeding 3 days.The palatability of the particles was investigated by this feeding trial.The results showed that:compared with the control group,when addition of berberine hydrochloride was 0.5 g/kg,intake of groupⅠdecreased 28.74%,while groupⅡdecreased 1.15%;when addition of berberine hydrochloride was 1.0 g/kg,intake of groupⅠdecreased 42.53%,while intake of groupⅡparticles decreased 12.64%.Coating technique cover up the bitterness in berberine hydrochloride efficiently which improved the compliance of oral administration.