Preparation Of Liposome-based Polymer Drugs And Screening Of Anti-tuberculosis Activity

The single-target drug pyrazinamide,sulfacetamide,ofloxacin and acetylsalicylic acid with certain antimicrobial activity are joined by appropriate chemical bonds to form new acetylsalicylic acid-pyrazine amide and sulfonamide The acyl-oxafloxacin hybrid molecule is a new drug with multiple targets,and it is expected to improve the drug resistance of pyrazinamide,sulfacetamide,ofloxacin and acetylsalicylic acid drug molecules in a single target.The designed heterozygous preparation reaction process is simple,the raw materials are easy to obtain,and the structure characterization confirms the structure of the hybrid molecules.Preliminary activity data showed that the biological activity of the resulting hybrid product was enhanced relative to the original drug.The acetylsalicylic acid-pyrazine amide liposome and the sulfacetamide-oxafloxacin liposome were prepared by using liposome as the inclusion material.The dialysis method,filtration method and organic solvent extraction method were compared.The separation method between plastid and free drug,considering the effect and operability,finally determines the filtration method as the separation method between liposome and free drug.The Tween-80 ethanol solution(w/w: 10%)was selected as the demulsifier.The most suitable ratio of the demulsifier to the liposome was investigated.The recovery rate was evaluated.The final ratio was demulsifier: liposome.=2:1.The single factor experiment method was used to investigate the effects of water bath temperature,bath time and phospholipid ratio on the liposome properties of the two compounds.The comprehensive factors of the encapsulation efficiency and recovery rate were used to find out the better experiment.The test results of the liposome anti-tuberculosis activity of the prepared liposome showed that the liposome could better protect the hybrid drug molecule and lay a good foundation for the design of the new dosage form.