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Uses of puerarin and derivatives thereof in preparing medicament

A derivative, puerarin technology, applied in the field of puerarin and its derivatives, can solve the problems of poor oral bioavailability, difficult preparation, low solubility of puerarin, etc.

Active Publication Date: 2008-11-12
CHONGQING ACAD OF CHINESE MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low solubility of puerarin in water and organic solvents and poor oral bioavailability, it is difficult to make ideal preparations

Method used

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  • Uses of puerarin and derivatives thereof in preparing medicament
  • Uses of puerarin and derivatives thereof in preparing medicament
  • Uses of puerarin and derivatives thereof in preparing medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Preparation of Puerarin Derivatives

[0067] Get puerarin (Beijing Xiehe Pharmaceutical Factory, content 99%, batch number 20060816) 100g in the round bottom flask, add 2000ml glacial acetic acid to dissolve, add the acetic anhydride of 6 times molar number, stir and react at room temperature for 6 hours, place 24 hours, reduce Press to recover glacial acetic acid to 500ml, let cool to room temperature, pour into 5000ml ice water, stir, filter, dissolve the residue with dichloromethane, put it in a separatory funnel, separate dichloromethane, dehydrate with anhydrous sodium sulfate, filter , and recovered dichloromethane to obtain 184 g of puerarin acetylation product.

[0068] Dissolve 100g of acetylated puerarin in 500ml of dichloromethane, add an equivalent amount of 1% sodium bicarbonate aqueous solution, shake fully for 30 minutes, check with TLC (thin-layer plate is silica gel GF 254 Developing agent is sherwood oil and ethyl acetate by volume ratio 1: 2 proporti...

Embodiment 2

[0070] Preparation method of puerarin derivative injection

[0071] Tetraacetyl Puerarin 50g

[0072] Poloxamer 500g

[0073] Polysorbate 80 500g

[0074] Add water for injection to 5000ml

[0075] Made 1000 pieces

[0076] Wherein the poloxamer is the carrier and the scaffolding agent of the dispersion, and the polysorbate 80 is the solubilizing agent.

[0077] Preparation Process

[0078] (1) Dosing: Weigh 50g of tetraacetylpuerarin and 500g of poloxamer in an aseptic operation room, mix well, add 5000ml of absolute ethanol and grind for 5 minutes to fully dissolve. Then weigh 500g polysorbate 80 and add 5000ml sterilized water for injection to slightly heat to dissolve. Mix the two evenly, recover ethanol at low temperature, and add sterile water for injection to 5000ml.

[0079] (2) Filtration, intermediate inspection and packaging: use 1‰ activated carbon to depyrogenate, and then use sterilized 0.22μm (Sartobran-p produced by SARTORIUS, Germany) filter for sucti...

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Abstract

The invention relates to a novel application of puerarin and derivates thereof in the pharmaceutical field. The puerarin and the derivates thereof have a COX-2-selective inhibition effect, are safe in use without toxic side effect, and have notable effectiveness. The puerarin and the derivates thereof can be used to prevent and cure osteoarthritis, rheumatic arthritis, rheumatoid arthritis, urarthritis, hepatitis, conjunctivis, myocarditis, secondary inflammations caused by tumor and diabetes, itai itai diseases caused by cold or trauma, and other difficult and baffling diseases.

Description

technical field [0001] The present invention relates to the use of puerarin and its derivatives, in particular to the use in the field of pharmacy. Background technique [0002] Commonly used non-steroidal anti-inflammatory drugs (NSAIDs) are widely used clinically to treat various inflammatory diseases, including osteoarthritis, rheumatoid arthritis, rheumatoid arthritis, fever caused by colds, trauma, etc. Pain, cardiovascular, cancer, hepatitis and other diseases. These drugs have the same mechanism of action, which is to inhibit the cyclooxygenase (COX) required for the synthesis of prostaglandins. COX can be divided into structural COX-1 and inducible COX-2. Recent studies have shown that there may be variant COX-3 (isomers of COX-1) {Pi Zhibing, Jiang Zongbin. New progress in clinical research of COX-2 inhibitors [J]. Chinese Journal of Pain Medicine, 2006, 12(5): 297.}. COX-1 mainly exists in the gastrointestinal wall, kidney and platelets, and has the function of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P29/00
Inventor 杨大坚钟国跃徐嘉红张毅李恒华黄小平
Owner CHONGQING ACAD OF CHINESE MATERIA MEDICA
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