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Folate receptor-mediated colon-localized release of curcumin from microemulsions

A technology for folic acid receptors and colon localization, which is applied in antipyretics, antivirals, anti-inflammatory agents, etc., and achieves the effects of simple preparation method, improved solubility, and low cost

Inactive Publication Date: 2011-12-07
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, through oral administration, the use of folic acid receptor-mediated effects to promote drug absorption or targeted drug delivery has not been reported in domestic and foreign literature.

Method used

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  • Folate receptor-mediated colon-localized release of curcumin from microemulsions
  • Folate receptor-mediated colon-localized release of curcumin from microemulsions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Weigh 1.5g of Labrafil M19944 CS, 4.455g of Cremophor EL, 45mg of FA-PEG-CHEMS, and 4g of TranscutolHP. After stirring evenly, add 500mg of curcumin. After stirring evenly, curcumin self-microemulsion concentrate is obtained. Finally, add the concentrated solution into the colon-soluble capsules to obtain the product.

Embodiment 2

[0020] Weigh 1.5g of Capryol 90, 7.4625g of Cremophor EL, 37.5mg of FA-PEG-Chol, and 1g of PEG400, stir evenly with electromagnetic force, add 480mg of curcumin, and stir evenly to obtain curcumin self-microemulsion concentrate. Finally, add the concentrated solution into the colon-soluble capsules to obtain the product.

Embodiment 3

[0022] Weigh 3 g of Capryol 90, 2.91 g of Cremophor EL, 90 mg of FA-PEG-DSPE, and 4 g of absolute ethanol, and stir evenly with electromagnetic waves, then add 600 mg of curcumin, and stir evenly to obtain curcumin self-microemulsion concentrate. Finally, add the concentrated solution into the colon-soluble capsules to obtain the product.

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Abstract

The invention discloses a folate-receptor-mediated curcumin self-microemulsion colon-specific delivery preparation, which is composed of the following components in parts by weight: 0.05-7.5 parts of curcumin, 10-40 parts of oil phase, 30-60 parts of surfactant, 30-60 parts of cosurfactant and a folic acid lipid material the amount of which accounts for 0.01-3% the weight of the surfactant. In the invention, curcumin is processed into a self-microemulsion preparation, which is composed of a pharmaceutically common oil phase, a surfactant and a cosurfactant, and the solubility of curcumin can be increased by the oil phase, surfactant and cosurfactant; when the oil phase, surfactant and cosurfactant are mixed in an appropriate ratio, an O / W microemulsion can be formed in water by self-microemulsification, so that the solubility of curcumin is up to 30-70 mg / mL and the solubility is increased by more than 40000 times; and the solubility of turmeric is effectively improved, the oral absorption availability of the preparation is improved, and the preparation has the advantages of strong targeting, simple preparation method, low cost, etc.

Description

technical field [0001] The invention relates to a folic acid receptor-mediated curcumin self-localized drug release preparation of microemulsion colon. Background technique [0002] Curcumin (Curcumin, Cur) is a natural active ingredient, which has anti-inflammatory, anti-oxidation, anti-human immunodeficiency virus, liver and kidney protection, anti-cancer and anti-cancer effects. The National Cancer Institute of the United States has listed it as the first The third generation of cancer chemoprevention drugs, and listed in the US Pharmacopoeia in 2000. Cur is a poorly soluble drug with low oral absorption and an oral absolute bioavailability of about 1%. Clinical trials have shown that it has a good therapeutic effect on human colon cancer, but its daily oral dosage is 3600-8000 mg. Therefore, it is an urgent problem to seek a new drug dosage form that can effectively improve the solubility of curcumin, promote the oral absorption of curcumin, and improve the curative eff...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/12A61K47/42A61P1/16A61P13/12A61P29/00A61P31/14A61P39/06
Inventor 翟光喜张林
Owner SHANDONG UNIV
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