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Polymethoxylated flavones and its preparation method

A polymethoxyflavonoid injection and the technology of polymethoxyflavonoids are applied in the directions of anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., and can solve the problems of poor stability, non-compliance with medicinal standards, and unsuitable for industrial production, etc. problem, to achieve the effect of good solubility and good safety

Inactive Publication Date: 2006-09-27
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although polymethoxylated flavones can be dissolved in propylene glycol, they will precipitate in a short period of time after dilution with water and cannot be injected, and the solution completely using alcohol as a solvent should not be directly used for injection, so this technical scheme, because Poor stability, does not meet pharmaceutical standards, not suitable for industrial production

Method used

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  • Polymethoxylated flavones and its preparation method
  • Polymethoxylated flavones and its preparation method
  • Polymethoxylated flavones and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Weigh 180 grams of polyoxyethylene hydrogenated castor oil (RH60) in an airtight container, add 400 ml of absolute ethanol, mix well at room temperature into a liquid state, then add nobiletin, tangeretin, sweet orange element, heptalysin 30 grams of the mixture of oxyflavone and isotangerine, after the container is sealed, make it completely dissolve in a water bath at 50°C. Remove and let stand at room temperature for 45 minutes. Then add activated carbon for needles with a total liquid weight of 0.1%, stir at room temperature for 20 minutes, filter with a No. 4 sand core filter rod, and filter with a 0.22μф300mm sterile membrane under pressure. After the predicted content and pyrogen are qualified, aseptically pack 1000 bottle. It can be used for intramuscular injection after diluting with 5ml of water for injection before use.

Embodiment 2

[0026] Weigh 600 grams of Tween-80 into a sealable container, add 1000 ml of absolute ethanol, mix well at room temperature into a liquid state, then add 100 grams of a mixture of nobiletin, tangeretin and sweet orange, and seal the container , 70 ℃ water bath to make it completely dissolved. Take it out and let it stand at room temperature for 60 minutes. Then add activated carbon for needles with 0.5% of the total weight of the liquid, stir at room temperature for 15 minutes, filter with a No. 4 sand core filter rod, and filter with a 0.22μф300mm sterile membrane under pressure. After the predicted content and pyrogen are qualified, aseptically pack 1000 bottle. Diluted with 100ml 0.9% sodium chloride injection or 5% glucose injection before use, it can be used for intravenous injection.

Embodiment 3

[0028] Take by weighing 400 grams of polyoxyethylene hydrogenated castor oil (RH40) in an airtight container, add 1,2-propanediol 1500 milliliters, mix into a liquid state at room temperature, then add the mixture of sweet orange element, heptamethoxyflavone 50 grams, after the container is sealed, dissolve it completely in a 35°C water bath. Take it out and let it stand at room temperature for 70 minutes. Then add activated carbon for needles with a total liquid weight of 0.3%, stir at room temperature for 30 minutes, filter with a No. 4 sand core filter rod, and filter with a 0.22μф300mm sterile membrane under pressure. After the predicted content and pyrogen are qualified, aseptically pack 1000 bottle. Diluted with 100ml 0.9% sodium chloride injection or 5% glucose injection before use, it can be used for intravenous injection.

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Abstract

The polymethoxyl flavone injection includes polymethoxyl flavone, alcohol and surfactant, and the polymethoxyl flavone is mixture of two or more of nobiletin, tangeretin, sinensetin, heptamethoxyl flavone and isotangeretin. The present invention solves the solubility and stability problem of polymethoxyl flavone injection, and the polymethoxyl flavone injection has high safety, coincides with medicine standard and suitable for intramuscular injection and intravenous injection. The present invention also discloses the preparation process of the polymethoxyl flavone injection.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to polymethoxylated flavone injections and a preparation method thereof. Background technique [0002] Polymethoxylated flavones are a mixture extracted from the fruits of Rutaceae plants. Its main components are nobiletin (Nobiletin, 5,6,7,8,3', 4'-hexamethoxyflavone) and tangeretin (tangeretin, 5,6,7,8,4'-pentamethoxyflavone) In addition, there are sweet orange element (senensetin, 5, 6, 7, 3', 4'-pentamethoxyflavone), heptamethoxyflavone (heptamethoxyflavone, 3, 5, 6, 7, 8 , 3', 4'-heptamethoxyflavone), isosenensetin (isosenensetin, 5, 7, 8, 3', 4'-pentamethoxyflavone) etc. (structural formula is as follows). According to relevant literature reports, polymethoxylated flavones have various medicinal functions such as antifungal infection, treatment of hypertension and diabetes, prevention and treatment of chronic rheumatism, anticancer, treatment of senile dementia, an...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61K31/352A61P9/12A61P3/10A61P3/04A61P29/00A61P35/00
Inventor 潘福生胡凯叶杉
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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