| Using Chitosan and beta cyclodextrin as a inclusion material,HYD made in the laboratory,Levofloxacin,pyrazinamide,isoniazid and thymopentin anti-tuberculosis small molecule were as the main research objects,we obtained the HYD-β-cyclodextrin inclusion complex inclusion complex,Levofloxacin-CHitosan inclusion complex,pyrazinamide-β-cyclodextrin inclusion complex,isoniazid-β-cyclodextrin inclusion complex and thymopentin-β-cyclodextrin;the inclusion rate and yield of the inclusion complexes were taken as the comprehensive evaluation index after weighted summation(the weighting coefficients are 70 % and 30 %).The effects of mass ratio/molar ratio of host to guest,inclusion temperature and inclusion time on the inclusion efficiency were studied by uniform design test;by Fourier transform infrared spectroscopy(FTIR)、DSC and UV spectrophotometry,we studied the characterization of the five inclusion complexes of Levofloxacin,pyrazinamide,isoniazid,thymopentin and HYD and studied the antituberculous activities of five kinds of inclusion complexes.The results showed: the mass ratio of levofloxacin to chitosan 69.9,inclusion temperature 60.6 ℃,inclusion time 0.5 h,and the compre hensive evaluation was 100 %;the molar ratio of pyrazinamide to β-cyclodextrin 1.5,inclusion temperature 70 ℃,inclusion time 1.03 h,and the comprehensive evaluation was 96.18 %;the molar ratio of isoniazid to β-cyclodextrin 1.5,inclusion temperature 30 ℃,inclusion time 0.5 h,and the comprehensive evaluation was 87.80 %;the molar ratio of HYD to β-cyclodextrin 1.5,inclusion temperature 70 ℃,inclusion time 1.08 h,and the comprehensive evaluation was 90.83 %;the molar ratio of thymopentin to β-cyclodextrin 1.5,inclusion temperature 70 ℃,inclusion time 1.15 h,and the comprehensive evaluation was 90.03 %.And the five inclusion complexes all showed good antituberculous activity. |