Study on Inclusion Complex of Poorly Water-Soluble Drug with β-Cyclodextrin :The feasibility of form

来源 :第七届国际分离科学与技术会议(Proceedings of the 7th International Conferen | 被引量 : 0次 | 上传用户:jim_666cn
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  In this study,the feasibility of formation,physical properties and the bitterness change of drug/β-CD complex for poorly water-soluble drug (Diphenhydramine hydrochloride,DPH,Cetirizine dihydrochloride,CTZ,dl-chlorpheniramine maleate,CPA,Loperamide hydrochloride,LPM,Valsartan,VAL,Tetracycline hydrochloride,TTC) were studied.The effect of β-CD on drugs was studied by introducing NMR tools for figuring out one to one binding between drugs and β-CD except for VAL.The equation modified by Hanna-Ashbaugh was plotted to calculate the value of association constant for 5 drugs: CTZ=38.2,DPH=28.2,TTC=83.5,CPA=65.8,LPM=45.6.VAL didnt form drug/β-CD complex.Also,drug/β-CD complex was manufactured by physical mixing,freeze-drying and using supercritical carbon dioxide as anti-solvent (ASES process) to assess physical properties and the change of bitterness.Physical characteristics change of Drug/β-CD complex was studied by XRD and DSC.Drug/β-CD complex except for VAL caused indistinct thermal properties and crystallizability different from original drugs.The change of bitterness was studied by taste perception test.Taste perception test showed that the bitterness of CTZ,DPH,TTC,CPA was masked and decreased but the bitterness of LPM,VAL was not masked even though β-CD covered the phenyl ring of LPM.
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