Prrparation And Characterization Of Inclusion Complex Of β-CD And Its Derivative With Baicalein

In this paper,four kinds of β-cyclodextrin derivatives were prepa-red:hydroxypropyl-β-cyclodextrin,carboxymethyl-β-cyclodextrin,hydr-oxythyl-β-cyclodextrin and randomly methylated-β-cyclodextrin.Andthey were identified by IR and NMR.The solubilization and stableconstants of β-cyclodextrin and its derivatives with baicalein weremeasured.The best inclusion reaction technologies of β-cyclodextrinand four derivatives with baicalein,using inclusion ration as theevaluation index,were selected.And then the inclusions werecharacterized.The experimental results were as follows:(1)Four kinds of β-cyclodextrin derivatives were prepared:hydrox-ypropyl-β-cyclodextrin,carboxymethyl-β-cyclodextrin,hydroxythyl-β-cyclodextrin and randomly methylated-β-cyclodextrin.And they wereidentified by IR and NMR.(2)In the same conditions,the Kaof methylated-β-cyclodextrincomplex with baicalein was bigger than other complexes.The solubiliza-tion effect was:methylated-β-cyclodextrin>hydroxypropyl-β-cyclodex-trin>hydroxythyl-β-cyclodextrin>carboxymethyl-β-cyclodextrin>β-cyc-lodextrin.As their density become bigger,the solubilization effectbecome stronger and the derivatives were more suitable for inclusionthan β-cyclodextrin.(3)The inclusions were characterized by IR,TG and SEM.Theresult showed that the complexes are prepared.The best inclusionreaction technologies of β-cyclodextrin and four derivatives withbaicalein, inclusion ration as the evaluation index,were selected.The best inclusion reaction technology of β-cyclodextrin and baic-alein:inclusion temperature:50℃;time for inclusion:90min;β-cyclodex-trin:baicalein=3:1;stirring speed:1500r/min;the max inclusion ration of baicalein:70.37%.The best inclusion reaction technology of hydroxypr-opyl-β-cyclodextrin and baicalein:hydroxypropyl-β-cyclodextrin:baica-lein=3:1;time for inclusion:60min;the density of hydroxypropyl-β-cycl-odextrin:15%; inclusion temperature:50℃;the max inclusion ration ofbaicalein:78.30%.The best inclusion reaction technology of carboxym-ethyl-β-cyclodextrin and baicalein: inclusion temperature:40℃;time forinclusion:90min;carboxymethyl-β-cyclodextrin:baicalein=3:1;the densi-ty of carboxymethyl-β-cyclodextrin:25%; the max inclusion ration ofbaicalein:72.84%. The best inclusion reaction technology of hydroxythy-β-cyclodextrin and baicalein:hydroxythyl-β-cyclodextrin:baicalein=3:1;stirring speed:1500r/min;inclusion temperature:40℃; the density ofhydroxythyl-β-cyclodextrin:20%;the max inclusion ration of baicalein:77.53%.The best inclusion reaction technology of randomly methylated-β-cyclodextrin and baicalein:time for inclusion:90min; the density ofrandomly methylated-β-cyclodextrin:20%;inclusion temperature:45℃randomly methylated-β-cyclodextrin:baicalein=4:1;the max inclusionration of baicalein:81.43%.The five inclusion reaction technologieswere reasonable and stable.The research of solubilization,technology of inclusion reaction andinvestigation of physical and chemical properties of β-cyclodextrin andits derivatives with baicalein have an important meaning to broaden theapplication scope of baicalein,and can provide some help for thetraditional Chinese medicine research.