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Eudragit S100 coated curcumin pectin microsphere and preparation method thereof

A technology of curcumin fruit and curcumin, applied in the field of curcumin pectin calcium microspheres and preparation thereof, can solve problems such as limitation, and achieve the effects of improving drug concentration and effectively treating colon cancer

Inactive Publication Date: 2011-02-16
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pectin (pectin) is a group of galacturonic acids that can be specifically degraded by polysaccharidases in the colon, but natural pectin has certain solubility in water, acid and alkali, making it useful in the application of colon-targeted carriers restricted

Method used

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  • Eudragit S100 coated curcumin pectin microsphere and preparation method thereof
  • Eudragit S100 coated curcumin pectin microsphere and preparation method thereof
  • Eudragit S100 coated curcumin pectin microsphere and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0031] Embodiment 1: Preparation of the curcumin pectin calcium microspheres coated with Eudragit S100

[0032] Liquid paraffin as oil phase, Span 80 as emulsifier, CaCl 2 2H 2 O solution is a cross-linking agent, and the specific steps are as follows: dissolve 0.16 g of pectin in 4 g of hot water solution, place at room temperature, add 0.064 g of curcumin, and stir overnight on an electromagnetic stirrer to obtain an aqueous phase. At room temperature, the uniformly mixed aqueous phase was slowly added to 16 g of liquid paraffin containing 1.5% Span 80 under electromagnetic stirring at 800 r / min, and stirred for 8 min to form a W / O emulsion. Then, 0.4 g of calcium chloride dihydrate solution with a mass fraction of 30% was added to the formed emulsion, and crosslinked for 10 min. Finally, the obtained suspension was suction-filtered, and alternately washed three times with petroleum ether and isopropanol to obtain calcium pectin microsphere powder, which was dried under re...

Embodiment 2

[0038] Embodiment 2: Preparation of the curcumin pectin calcium microspheres coated with Eudragit S100

[0039] Liquid paraffin as oil phase, Span 80 as emulsifier, CaCl 2 2H 2 O solution is a cross-linking agent, and the specific steps are as follows: dissolve 0.13g of pectin in 4g of hot water solution, place at room temperature, add 0.043g of curcumin, and stir overnight on an electromagnetic stirrer to obtain an aqueous phase. At room temperature, slowly add the uniformly mixed water phase into 10 g of liquid paraffin containing 2.0% Span 80 under 800 r / min electromagnetic stirring, and stir for 30 min to form a W / O emulsion. Then, 0.6 g of calcium chloride dihydrate solution with a mass fraction of 20% was added to the formed emulsion, and crosslinked for 15 min. Finally, the obtained suspension was suction-filtered, and alternately washed three times with petroleum ether and isopropanol to obtain calcium pectin microsphere powder, which was dried under reduced pressure...

Embodiment 3

[0045] Embodiment 3: the preparation of the curcumin pectin calcium microsphere of Eudragit S100 coating

[0046] Liquid paraffin as oil phase, Span 80 as emulsifier, CaCl 2 2H 2 O solution is a cross-linking agent, and the specific steps are as follows: dissolve 0.16 g of pectin in 4 g of hot water solution, place at room temperature, add 0.107 g of curcumin, and stir overnight on an electromagnetic stirrer to obtain an aqueous phase. At room temperature, slowly add the uniformly mixed water phase into 12 g of liquid paraffin containing 1.5% Span 80 under electromagnetic stirring at 1000 r / min, and stir for 20 min to form a W / O emulsion. Then, 1.2 g of calcium chloride dihydrate solution with a mass fraction of 30% was added to the formed emulsion, and crosslinked for 20 min. Finally, the obtained suspension was suction filtered, and washed three times alternately with petroleum ether and isopropanol to obtain calcium pectin microsphere powder, such as figure 1 (left); dri...

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Abstract

The invention discloses an eudragit S100 coated curcumin pectin microsphere. The microsphere is prepared by the following steps: preparing the curcumin pectin microsphere, and coating, wherein the curcumin pectin microsphere is prepared from curcumin and pectin, the mass ratio of the curcumin to the pectin is 1:(1-6), the grain size of the pectin microsphere is between 50 and 80 mu m, the loading rate is between 10 and 31 percent, and the entrapment rate is between 40 and 60 percent; and the coating material is Eudragit S100, the mass ratio of the Eudragit S100 to the curcumin pectin microsphere is (5-10):1, the grain diameter of the coated microsphere is between 150 and 210mu m, and the loading rate is between 0.8 and 1.5 percent. The colon targeting pectin coated microsphere prepared from the curcumin can specifically release the curcumin under a colon physiological condition, the medicament is concentrated in the colon region, and the local medicament concentration is improved, so the function of effectively treating colon cancer can be achieved.

Description

technical field [0001] The invention relates to Eudragit S100-coated curcumin pectin calcium microspheres and a preparation method thereof. Background technique [0002] Curcumin (Cur) is a natural phenolic compound extracted from the plant Curcuma longa L. in the family Zingiberaceae. It has various pharmacological effects such as anti-inflammatory, antibacterial, anti-tumor, and antioxidant. The results of phase II clinical trials of curcumin in the treatment of colon cancer abroad have been reported. Due to the low oral bioavailability of curcumin, in order to achieve the therapeutic concentration of the target site, it is necessary to increase the dosage (up to 12g / day). However, the increase of the dosage will inevitably bring a lot of inconvenience to the patient's medication and preparation process. [0003] Oral colon-targeted drug delivery system (OCDDS) is a new drug delivery method developed in the late 1990s. Pectin (pectin) is a group of galacturonic acids tha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/00A61K47/36A61K31/12A61K47/32A61K9/16
Inventor 翟光喜张林曹丰亮
Owner SHANDONG UNIV
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