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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

Inactive Publication Date: 2006-12-20
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As can be seen above, the preparation of non-ionic water-soluble cyclodextrin polymers and their general application in pharmaceutical preparations have not been suggested in the literature, especially the research on drug complexes and preparations based on water-soluble cyclodextrin polymers, has not yet been reported

Method used

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  • Insoluble drug delivery system based on water-soluble cyclodextrin
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  • Insoluble drug delivery system based on water-soluble cyclodextrin

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The invention relates to an insoluble medicine feeding system based on soluble cyclodextrin polymer, with high yield and the application in batch production, wherein said medicine compound is formed by insoluble medicine and cyclodextrin derivant, whose mass ratio is 0.1-100:1; and said insoluble medicine is the one whose solubility is less than 1% in room temperature; the soluble cyclodextrin polymer uses cyclodextrin as crosslink agent to be concentrated with cyclodextrin monomer. The inventive product is not shaped powder, whose average molecular weight can reach 10000.

Description

Technical field: [0001] The present invention relates to the application of a new type of pharmaceutical excipient in pharmaceutical preparations, in particular the application of water-soluble cyclodextrin polymers in pharmaceutical preparations, especially a combination of cyclodextrin polymers and water-insoluble drugs. Drug formulations based on inclusion solubilization. Background technique: [0002] Due to the low dissolution rate of water-insoluble drugs, it is difficult for the drug to reach the effective blood concentration required for treatment, and the bioavailability is poor and highly variable, which affects the efficacy; for new active compounds, it will affect preclinical screening and clinical Therefore, "solubilization" is a major topic in drug research. Inclusion technology is the use of physical or physicochemical methods to introduce drugs into the cavity of cyclodextrin derivatives, so that the drug has many new properties, such as increasing solubilit...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K9/20A61K9/48
Inventor 潘卫三聂淑芳张姝
Owner SHENYANG PHARMA UNIVERSITY
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