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Protocyanidin slow release capsule

A technology of proanthocyanidin and anthocyanin content, applied in the directions of antidote, drug delivery, organic active ingredients, etc., can solve the problems of short action time, short half-life, no sustained release effect, etc., to increase stability, improve stability, Simple preparation process

Inactive Publication Date: 2002-12-11
天津市园艺工程研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This proanthocyanidin capsule preparation has no sustained-release effect, and the proanthocyanidin is released rapidly after oral administration, with short half-life and short action time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1, prepare 500ml of 0.8% chitosan solution with 1.0% acetic acid, add 15 grams of CaCl 2 , made of chitosan-CaCl 2 solution. Take 1 gram of grape seed proanthocyanidin extract and add it to 50ml, 5% sodium alginate aqueous solution, mix well to make proanthocyanidin-sodium alginate solution, drop proanthocyanidin-sodium alginate solution into chitosan-CaCl with a needle 2 solution, stirred for 10-60 minutes, filtered or centrifuged, and the obtained spheres were washed with water and then dried to obtain proanthocyanidin sustained-release microcapsules. The particle size of the proanthocyanidin slow-release microcapsule is less than 1 mm, and the average content of proanthocyanidin in the microcapsule is 9% (percentage by weight). The dissolution test shows that the dissolution rate of proanthocyanidin in the phosphate buffer solution of pH 7.4 is 82% in 24 hours. .

Embodiment 2

[0023] Embodiment 2, prepare 1.0% chitosan solution 500ml with 2.0% acetic acid, add 15 grams of CaCl 2 , made of chitosan-CaCl 2 solution. Get 0.5 gram of grape seed oligomeric proanthocyanidin preparation (OPC) and join in 50ml, 5% sodium alginate aqueous solution, make proanthocyanidin-sodium alginate solution, drop proanthocyanidin-sodium alginate solution into chitosan- CaCl 2 solution, stirred for 10-60 minutes, filtered or centrifuged, and the obtained spheres were washed with water and then dried to obtain proanthocyanidin sustained-release microcapsules. The particle diameter of the proanthocyanidin slow-release microcapsule is less than 1mm, and the average proanthocyanidin content in the microcapsule is 6% (percentage by weight). The dissolution test shows that the dissolution rate of the proanthocyanidin in the phosphate buffer solution with pH 7.4 is 85% within 12 hours.

Embodiment 3

[0024] Example 3, take 0.5 g of pine bark proanthocyanidin extract and add it to 50 ml of 3% sodium alginate aqueous solution to make proanthocyanidin-sodium alginate solution, add proanthocyanidin-sodium alginate solution to 500 ml with a high-pressure spray gun, 0.5-5.0% (W / V)CaCl 2 In the solution, stir gently for 10-60 minutes, filter or centrifuge, wash the obtained spheres with water, add 500ml of 0.5% chitosan solution prepared with 1.0% acetic acid, stir for 10-60 minutes, filter or centrifuge, and wash the obtained spheres with water After drying, proanthocyanidin sustained-release microcapsules are obtained. The particle size of the proanthocyanidin slow-release microcapsule is less than 0.6mm, and the proanthocyanidin content in the microcapsule is 8% (percentage by weight). The dissolution test shows that the dissolution rate of the proanthocyanidin in the phosphate buffer solution of pH 7.4 is 67% in 12 hours. .

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PUM

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Abstract

A protocyanidin sloow release microcapsule has microcapsule size smaller than 3 mm, protocyanidin content of 0.25-25 wt% and sustained release period of 12-48 hr in buffering phosphoric acid solutionof pH 7.4. The wall of the microcapsule is one three layer structure including agglomerate calcium alginate layer, chitosan and alginate complex layer and deposited chitosan layer. The microcapsule is prepared through compounding water solution of calcium alginate containing protocyanidin, preparing chitosan-CaCl2 solution, adding miniature liquid drop of water solution of calcium alginate containing protocyanidin into chitosan-CaCl2, solution and subsequent processing. The release rate of the coated protocyanidin is adjustable.

Description

technical field [0001] The invention relates to a slow-release microcapsule of proanthocyanidins, which belongs to the improvement of oral proanthocyanidin formulations. Background technique [0002] Proanthocyanidins are a class of polyphenolic compounds formed by hydroxyflavan compounds connected by carbon-carbon bonds. Because anthocyanins can be produced by heating in an acidic medium, this type of polyphenolic compounds is named proanthocyanidins. The structural units of procyanidins are flavan-3-ols, such as catechin, epicatechin, etc. According to the degree of polymerization, di-tetramers are usually called oligomeric proanthocyanidins, or OPC for short. Proanthocyanidins widely exist in nature, such as grapes, blueberries, cherries, plums, hawthorn, cocoa beans, peanuts, ginkgo, rhubarb, cinnamon bark and pine bark, among which grape seeds and pine bark are the best sources of proanthocyanidins. [0003] Proanthocyanidins have a strong antioxidant and free radical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/352A61P39/06
Inventor 张峻吉伟之蔡国增齐欣陈晓云
Owner 天津市园艺工程研究所
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