Screening And Inclusion Studies Of Carbohydrate Polymer Anti-tuberculosis Drugs

Isoniazid,ethambutol and acetylsalicylic acid,which have certain killing or inhibiting effects on microorganisms,are joined by suitable chemical bonds to form new acetylsali cylic acid-isoniazid and acetylsalicylic acid-ethylamine butanol hybrids molecules.It is a new drug which are expected to improve single targets of isoniazid,ethambutol and ace tylsalicylic acid resistance of drug molecules with multiple targets.The conditions of hy brid synthesis reaction are mild,simple process,easy availability of raw materials and en vironmental friendliness.Preliminary activity data showed that the bioactivity of the het erozygous product was stronger than original drug.Packages for the convenience of clinical medicine,the prepared acetylsalicylic aid-isoniazid and isocyanic acid-ethylamine butanol drugs are encapsulated with inclusion technology of freeze-drying method and saturated aqueous solution method to obtain ace tylsalicylic acid-isoniazid-?-cyclodextrin inclusion compound,acetylsalicylic aid-isoniazid-chitosan inclusion compound,acetylsalicylic acid-ethylamine buta nol-?-cyclodextrin inclusion compound,acetylsalicylic acid-ethylamine butanol inclusion.Coplex70% of inclusion rate and 30% of yield as comprehensive evaluation indexes,the efects of molar ratio or mass ratio,reaction temperature and time on the inclusion efficicy of heterozygous compounds were investigated by using the 3 factor 5 horizontal homogeni zation experiment method.The structure of the hybrid was characterized by UV,IR,LCMS and HNMR.The structure of the inclusion complex was characterized by UV,IR and DSC.The anti-tuberculosis activity of the inclusion complex was preliminarily obtained.The results showed that the molar ratio of acetylsalicylic acid-isoniazid to ?-cyclodextrin was0.5,the inclusion temperature was 70 °C,and the inclusion time was 2.5 h,calculate the comprehensive evaluation for 90.9%;acetylsalicylic acid-isoniasid and chitosan mass ratio was 1,the inclusion temperature was 70 °C,and the inclusion time was 2 h,calculate the comprehensive evaluation for 81.6%;the molar ratio of acetylsalicylic acid-ethylamine butanol to ?-cyclodextrin was 1.5,the inclusion temperature was 70 °C,the inclusion time was 2.5 h,calculate the comprehensive evaluation for 91.9%;the mass ratio of acetylsali cylic acid-ethylamine butanol to chitosan was 1,the inclusion temperature was 70 °C,the combined time was 2.5 h,calculate the comprehensive evaluation for 88.7%.