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Studies on Solvency Enhancement of Hesperetin and Andrographolide

Author: ChenMeiLi
Tutor: LiuLongXiao
School: Zhejiang University
Course: Pharmacy
Keywords: Hesperetin Solid dispersion Polyvinylpyrrolidone k30 Tween 80 Andrographolide β-cyclodextrin Hydroxypropyl-β- cyclodextrin Sulfobutyl ether -β-cyclodextrin
CLC: TQ461
Type: Master's thesis
Year: 2010
Downloads: 131
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Abstract


At present, the clinical use of drugs which have more than 1/3 of poorly soluble drugs. Poorly soluble drug dissolution and absorption of slow, low bioavailability, and clinical application. Therefore, how to improve improve the solubility and dissolution rate of poorly soluble drugs is a difficult problem in pharmacy. The solid dispersion for hesperetin, β-cyclodextrin (β-CD) and their derivatives hydroxypropylcellulose of β-CD (HP-beta-CD), sulfo-butyl ether β-CD (SBE-β- The CD) clathrated for andrographolide to study insoluble drug solubilization. The main contents and results are as follows: (1) PVPk30 and Tween80 composite carrier solvent prepared hesperetin ternary solid dispersion, measured dissolution, and the corresponding proportion of hesperetin-PVPk30 made Element solid dispersion comparison, found by the hesperetin and PVPk30 and Tween80 prepared ternary solid dispersions markedly improved the dissolution rate of the hesperetin. By infrared spectroscopy the law (FTIR), differential scanning calorimetry France (DSC), the state of presence of the X-ray powder diffraction (XRD) method identified hesperetin in the ternary solid dispersion. The results show that the hesperetin dispersed in the solid dispersion in amorphous. (2) The effects of β-CD and its two derivatives of HP-β-CD, SBE-β-CD andrographolide phase solubility to determine the type of inclusion and calculation of the stability constants. The study shows that: the β-CD, HP-β-CD and SBE-β-CD can be formed with andrographolide molar ratio of 1:1 clathrate, the clathrate type respectively BS, AL and AL, cyclodextrin hydroxy formed between the former in a high concentration of β-CD solution intermolecular hydrogen bonds andrographolide is difficult to enter the hole, so that the andrographolide solubility decreases; latter two with HP-β-CD or SBE -β-CD concentration of the solution increases, the solubility of the andrographolide also increases. The stability constants show that the use of β-CD, HP-β-CD and SBE-β-CD inclusion after clathrate were stable. Were used grinding method, ultrasonic method and coprecipitation prepared andrographolide β-CD and its derivatives clathrate measured dissolution andrographolide original drug, as well as andrographolide with various cyclodextrin The physical mixture of dissolution performance comparison and found that the dissolution rate of clathrate andrographolide significantly increased. Using differential scanning calorimetry, X-ray diffraction and infrared spectra andrographolide phase identification. The results show that, indeed form inclusion complexes with the grinding method, ultrasonic method and coprecipitation method andrographolide-p-CD system.

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