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Preparation method and use of nanometer targeting preparation of micro-molecular immune drug

An atom and compound technology, which is applied in the preparation field of ingenol diterpene alcohol angelate to prepare water-soluble targeted drugs, can solve the problems of inability to inject administration, high toxicity, etc., and achieves increasing selectivity range and reducing toxicity. Side effects, the effect of improving tolerance

Inactive Publication Date: 2017-12-26
王成
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The inventor has developed a novel freeze-dried powder injection of ingenol derivatives and a preparation method through various attempts, solved the hydrophobicity problem of ingenol derivatives, improved its stability, and solved the problem of ingenol derivatives at the same time. The clinical "bottleneck" of its toxicity is too high and cannot be administered by injection

Method used

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  • Preparation method and use of nanometer targeting preparation of micro-molecular immune drug
  • Preparation method and use of nanometer targeting preparation of micro-molecular immune drug
  • Preparation method and use of nanometer targeting preparation of micro-molecular immune drug

Examples

Experimental program
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Effect test

Embodiment 1

[0065] (1) MPEG-PDLLA and IM were co-dissolved in 100mL of absolute ethanol at a certain mass ratio (90mg: 1mg), ultrasonically dissolved and added to a spray dryer, dried quickly, and the dried powder was collected, and 950ml of 14% (W / V) Aqueous solution of sucrose for injection, after shaking and ultrasonically dissolving, add 14% (W / V) aqueous solution of sucrose for injection to the 1000ml mark, filter under 0.22um pressure, divide the filtrate into 1ml / bottle, put it in a lyophilizer for quick Freeze to -40°C, pre-freeze for 4 hours, and sublimate and dry to obtain IM freeze-dried powder (IM-PM) for future use. When in use, take 1 bottle of IM-PM freeze-dried powder and add 2ml water for injection or 0.9% sodium chloride water for injection or glucose water for injection, shake to dissolve, after the bubbles dissipate, draw out and add 500ml normal saline or glucose water for injection, intravenously Infusion.

Embodiment 2

[0067] (2) MPEG-PDLLA and IM were co-dissolved in 100mL of absolute ethanol according to a certain mass ratio (98mg: 2mg), ultrasonically dissolved and added to a spray dryer, dried quickly, and the dried powder was collected, and 2ml of 14% (W / V) Aqueous solution of sucrose injection, after shaking and ultrasonically dissolving, add 14% (W / V) aqueous solution of sucrose injection to make up to the mark, filter under 0.22um pressure, divide the filtrate, 2ml / bottle, put it in a lyophilizer Quickly freeze to -40°C, prefreeze for 4 hours, and sublimate and dry to obtain IM freeze-dried powder (IM-PM) for future use. When in use, take 1 bottle of IM-PM freeze-dried powder and add 2ml water for injection or 0.9% sodium chloride water for injection or glucose water for injection, shake to dissolve, after the bubbles dissipate, draw out and add 500ml normal saline or glucose water for injection, intravenously Infusion.

Embodiment 3

[0069] (3) MPEG-PCL and IM were co-dissolved in 100mL of absolute ethanol according to a certain mass ratio (9g: 1g), ultrasonically dissolved and added to a spray dryer, dried quickly, and the dried powder was collected, and 950ml of 14% (W / V) Aqueous solution of sucrose for injection, after shaking and ultrasonically dissolving, adjust the pH value to 5.0, add 14% (W / V) aqueous solution of sucrose for injection to the 1000ml mark, pressurize and filter at 0.22um, divide the filtrate into 1ml / bottle, Quickly freeze in a freeze dryer to -40°C, pre-freeze for 4 hours, and sublimate and dry to obtain IM-PM freeze-dried powder for later use. When in use, take 1 bottle of IM-PM freeze-dried powder and add 2ml water for injection or 0.9% sodium chloride water for injection or glucose water for injection, shake to dissolve, after the bubbles dissipate, draw out and add 500ml normal saline or glucose water for injection, intravenously Infusion.

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Abstract

The invention relates to a construction method and a use of a nanometer targeting preparation of a micro-molecular immune drug. Ingenol phorbol angelate which cannot be dissolved in water and only can be administrated in a skin smearing manner as a gel, and its derivatives are loaded to a carrier auxiliary material to form nanometer particles, and then the nanometer particles are lyophilized to form a powder injection, so the water solubility problem is solved, the stability of the active components of the micro-molecular immune drug is improved, the problem of no vein administration or tumor interventional administration due to too high hydrophobicity and toxicity is solved, and the use of the micro-molecular immune drug is expanded.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method and application of preparing ingenol compounds, especially ingenol diterpene angelate, into water-soluble targeted drugs. Background technique [0002] Ingenol methylbutenoate, also known as PEP005, Ingenol-3-angelate, CAS No. 75567-37-2), can be isolated from various Euphorbia species , especially from Euphorbiapeplus and Euphorbia drummondii. [0003] Studies have found that ingenol methacrylate can directly act on mitochondria, making mitochondria swell, mitochondrial membrane permeabilization, and activating protein kinase C as a cell death inducer, which can cause rapid apoptosis of cancer cells, while normal cells are resistant to Ingenol methacrylate is less sensitive, is a potent anticancer drug, and is therapeutically effective at the microgram level. The immune system is an important anti-cancer mechanism of the human body. Once it finds...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/22A61K31/216A61K47/34A61P35/00
CPCA61K9/0019A61K9/1075A61K9/19A61K31/216A61K31/22A61K47/34
Inventor 王成单颖
Owner 王成
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