Preparation And Performance Evaluation Of Enrofloxacin Double Masking Microcapsules

Enrofloxacin is an important animal-specific antibacterial drug.Because of its wide range of sterilization,good oral effect and quick effect,it's deeply loved by the breeding industry.In recent years,oral veterinary drugs have been the main means of breeding,but some oral drugs such as enrofloxacin have a bad odor,and animals cannot use their willpower to insist on oral administration,resulting in a reduction in medicinal intake.It is not conducive to the recovery of the disease.Therefore,this paper takes enrofloxacin as the research object,and determines the optimum preparation of solid dispersion of enrofloxacin by changing the different hydrophilic dispersions and analyzing the influence of different factors on the enteric solubility of enrofloxacin solid dispersion.The carrier and the optimal solution for the preparation of a solid dispersion of enrofloxacin.Using sodium alginate and chitosan as raw materials,calcium alginate-chitosan-ennofloxacin double masking microcapsules were prepared to study the characteristics of microcapsules and to investigate the ratio of materials and environmental factors to microcapsule structure and intestine.The influence of solubility provides a research basis for the oral administration of drugs with bad odor.The main work and conclusions of this paper are as follows:(1)In order to increase the enteric solubility of enrofloxacin and obtain a preliminary taste-masking effect,It's frst to studied the preparation of solid dispersion of enrofloxacin.The prepared carrier material was determined to be polyethylene glycol 6000 by changing the influence of different hydrophilic dispersions on the absorbance value of enrofloxacin solid dispersion artificial intestinal juice.The effects of addition ratio,reaction temperature and stirring speed on the enteric solubility of enrofloxacin solid dispersion were analyzed by single factor experiment.After optimization by response surface experiment,the optimum conditions for the preparation of enrofloxacin solid dispersion were as follows:the ratio of enrofloxacin to polyethylene glycol 6000 is 1:10,and the preparation temperature was 90~oC.The stirring speed was 200 r/min.Under these conditions,the solid dispersion of enrofloxacin prepared in artificial intestinal juice has the largest cumulative release and can be better enteric.Process optimization of calcium alginate-ennofloxacin taste masking microcapsules.Firstly,sodium alginate-ennofloxacin taste-masking microcapsules were prepared by using sodium alginate as raw material.The ratio of enrofloxacin solid dispersion to sodium alginate and the ratio of sodium alginate to calcium carbonate were studied by single factor.The influence of four factors on the embedding rate of calcium alginate-ennofloxacin taste-masking microcapsules was optimized by response surface methodology.The optimal process parameters for the preparation of enrofloxacin taste-masking microcapsules were finally determined:The ratio of solid dispersion of norofloxacin to sodium alginate is 1:5,the ratio of sodium alginate to calcium carbonate is1:6,the amount of glacial acetic acid added during the preparation of microcapsules is 460?L,and the preparation time of microcapsules is 20 minutes.At this time,the embedding rate of calcium alginate-ennofloxacin-masked microcapsules reached a maximum of85.12%.(3)In order to prolong the colonization time of enrofloxacin-masked microcapsules in the intestine,and to enhance the potency effect while enhancing the efficacy,this part of the experiment carried out a calcium alginate-chitosan-ennofloxacin double masking microcapsule Preparation studies.Firstly,chitosan was determined as the experimental material of enrofloxacin double masking microcapsules,and the optimal scheme of double masking was determined by single factor experiment and response surface experiment:the pH value of chitosan solution was 5.5,shell The concentration of the glycan solution was0.6%,and the reaction temperature was 40.5?.At this time,the embedding rate of enrofloxacin in the calcium alginate-chitosan-ennofloxacin-masked microcapsules was85.46%.(4)Characterization of calcium alginate-chitosan-ennofloxacin taste masking microcapsules.The particle size distribution,morphology,embedding rate,drug loading amount and cumulative release rate in artificial oral liquid,gastric juice and intestinal juice of calcium alginate-chitosan-enrofloxacin taste-masked microcapsules prepared by the optimal solution The storage stability and other aspects were evaluated.The results showed that the average particle size of the microcapsules prepared by the optimal solution was 250?m,the average embedding rate was 86.1%,and the average drug loading was 21.9%.Enrofloxacin double The average cumulative concentration of taste masking microcapsules in artificial simulated oral fluid is less than 2?g/mL in 5 min,which is less than the bitterness threshold of pigs,which can achieve the expected taste masking effect.Compared with the original drug of enrofloxacin,the cumulative release rate of enrofloxacin artificial gastric juice in double masking microcapsules was 0.63%at5 min,and the cumulative release at 120 min was 8.09%.The cumulative dissolution of the original drug of Enrofloxacin in the original drug was 81.7%within 5 min,and the cumulative dissolution at 15 min was 87.9%,indicating that the prepared microcapsules can better protect the core drug from gastric acid damage.The cumulative release of enrofloxacin double-masked microcapsules in artificial intestinal fluid for 6 h was 59.1%,the cumulative release at 24 h was 80.11%,and the cumulative release at 48 h was 91%.It can be well sustained release in artificial simulated intestinal fluid,achieving the purpose of targeted release of drugs and enhancing drug efficacy.