Insoluble drug delivery system based on water-soluble cyclodextrin
A cyclodextrin polymer, insoluble drug technology, applied in the directions of inactive components of polymer compounds, pill delivery, capsule delivery, etc., can solve problems such as general application of non-ionic water-soluble cyclodextrin polymers that have not yet been suggested , to achieve the effect of high yield, mild reaction conditions, and improved solubility
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Embodiment 1
[0023] Example 1 Synthesis of water-soluble β-cyclodextrin polymer
[0024] 22.7 g (0.02 moles) of β-cyclodextrin were dissolved in 80 g (56 ml, 0.6 moles) of 30% NaOH at room temperature and stirred for 24 hours. The reaction solution was heated to 30° C., and 29.38 ml (34.84 g, 0.2 moles) of ethylene glycol diglycidyl ether was slowly added under stirring for 1 hour, and reacted at 30° C. for 4 hours, and a small amount of acetone was added to terminate the reaction. The reactant was cooled to room temperature, and the reaction solution was neutralized with 6 mol / l hydrochloric acid until the pH value was neutral, then the reaction solution was dialyzed to remove salt and unreacted components, concentrated under reduced pressure, finally precipitated with absolute ethanol, and vacuum-dried. 17.5 g of product are obtained. The cyclodextrin content was determined to be 26.4% by the iodine titration method (Acta Chim. Hung., 100, 265 (1979)).
Embodiment 2
[0025] Example 2 Synthesis of water-soluble γ-cyclodextrin polymer
[0026] 27.1 g (0.02 moles) of γ-cyclodextrin were dissolved in 60 g (40 ml, 0.5 moles) of 33% NaOH at room temperature and stirred for 24 hours. The reaction solution was heated to 30° C., and 44.1 ml (52.26 g, 0.3 moles) of ethylene glycol diglycidyl ether was slowly added for 1 hour under stirring, and reacted at 30° C. for 6 hours, and a small amount of acetone was added to terminate the reaction. The reactant was cooled to room temperature, and the reaction solution was neutralized with 6 mol / l hydrochloric acid until the pH value was neutral, then the reaction solution was dialyzed to remove salt and unreacted components, concentrated under reduced pressure, finally precipitated with absolute ethanol, and vacuum-dried. 14.2 g of product are obtained. The content of cyclodextrin was determined to be 22.3% by titration iodine method.
Embodiment 3
[0027] Example 3 Synthesis of water-soluble γ-cyclodextrin polymer
[0028]27.1 g (0.02 moles) of γ-cyclodextrin were dissolved in 112 g (56 ml, 1.4 moles) of 50% NaOH at room temperature and stirred for 24 hours. The reaction solution was heated to 65° C., and then 23.52 ml (27.76 g, 0.3 moles) of epichlorohydrin was added rapidly, and reacted at 65° C. for 4 hours, and a small amount of acetone was added to terminate the reaction. The reactant was cooled to room temperature, and the reaction solution was neutralized with 6 mol / l hydrochloric acid until the pH value was neutral, then the reaction solution was dialyzed to remove salt and unreacted components, concentrated under reduced pressure, finally precipitated with absolute ethanol, and vacuum-dried. 10.5 g of product are obtained. The content of cyclodextrin was determined to be 33.4% by titration iodine method.
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