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Studies on Effect of β-cyclodextrin and Its Derivatives Complexation on Physicochemical Properties of Isoquercitrin

Author: LiWenChao
Tutor: ShuangShaoMin
School: Shanxi University
Course: Pharmaceutical Analysis
Keywords: Cyclodextrins Isoquercitrin Inclusion complex Solubility Dissolution rate
CLC: TQ461
Type: Master's thesis
Year: 2009
Downloads: 65
Quote: 1
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Abstract


Chapter 1:The recent development of cyclodextrins inclusion technique has been reviewed and especially focused on the application of cyclodextrins and their derivatives in pharmaceutical industry.The chemical and biological properties of isoquercitrin(IQ) were summarized.Chapter 2:The inclusion complex of IQ withβ-cyclodextrin(β-CD) was prepared and characterized by UV-vis absorption spectroscopy(UV),Fourier transformation-infrared(FTIR) spectroscopy and ~1H Nuclear magnetic resonance(~1H-NMR) spectroscopy.An exact and precise method for UV-vis absorption spectroscopy determination of IQ was developed.The precision experiments within-day and between-day were 1.66%,1.42%,0.28%and 1.99%,1.34%,1.26%,respectively.Results of recovery experiment were 102.60±0.19%,102.61±0.59%and 103.19±0.61%,respectively.The phase solubility diagram of IQ withβ-CD was classified as A_L-type,which suggested IQ was inserted into theβ-CD cavity to form a 1:1 inclusion complex.Further,it is found that the water solubility and dissolution rate of IQ were significantly increased by forming an inclusion complex withβ-CD. The aqueous solubility of IQ-β-CD was 8.22 times higher than that of IQ.The dissolution rate of IQ-β-CD complex was 89.80%within 30 min,while the dissolution rate of IQ was 41.48%which was evidently enhanced by the complex of IQ withβ-CD.Chapter 3:The solid inclusion complex of IQ withβ-CD was prepared by using coprecipitation,ultrasonic and kneading method,respectively.The recovery,inclusion rate,load drug and solubility of IQ were adopted as index to optimize the best method for inclusion preparation.The orthogonal experiment design was applied to optimize the preparation process of inclusion complex.The optimum entrapment conditions were as follows:the reaction time was 6 h,the molar ratio of IQ intoβ-CD was 1:2,the reaction temperature was 55℃.Chapter 4:The inclusion complex of IQ with hydroxypropy-β-cyclodextrin (HP-β-CD) was prepared and characterized by UV,Fourier FTIR and ~1H-NMR.An exact and precise method for UV-vis absorption spectroscopy determination of IQ was developed.The precision experiments within-day and between-day were not more than 2%,respectively.Results of recovery experiment were 100.73±0.82%,101.84±1.12%and 103.11±0.93%, respectively.The phase solubility diagram of IQ with HP-β-CD was classified as A_L-type,which suggested IQ was inserted into the HP-β-CD cavity to form a 1:1 inclusion complex.Further,it is found that the water solubility and dissolution rate of IQ were significantly increased by forming an inclusion complex with HP-β-CD.The solubility of IQ-HP-β-CD was 15.66 times higher than that of IQ.The dissolution rate of IQ-HP-β-CD complex was 98.96%within 15 min,while the dissolution rate of IQ was 41.48%within 30 min which was evidently enhanced by the complex of IQ with HP-β-CD.Chapter 5:The solid inclusion complex of IQ with HP-β-CD was prepared by using stirring,ultrasonic and kneading method,respectively.The recovery, inclusion rate,load drug and solubility of IQ were adopted as index to optimize the best method for inclusion preparation.The orthogonal experiment design was applied to optimize the preparation process of inclusion complex.The optimum entrapment conditions were as follows:the reaction time was 6h,the molar ratio of IQ into HP-β-CD was 1:3,the reaction temperature was 55℃.

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