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A tetrazinedicarboxamide liposome preparation and preparation method thereof

A technology of tetrazine dicarboxamide and liposome preparation, which is applied in the preparation of new tetrazine dicarboxamide formulations, tetrazine dicarboxamide liposome preparation and its preparation field, and can solve problems such as retention and inability to absorb drugs , to achieve the effect of low toxicity, beneficial to disease treatment, and beneficial to removal

Active Publication Date: 2020-11-27
石雷 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to overcome the defect that the medicine existing in the prior art cannot be absorbed and stays in the body

Method used

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  • A tetrazinedicarboxamide liposome preparation and preparation method thereof
  • A tetrazinedicarboxamide liposome preparation and preparation method thereof
  • A tetrazinedicarboxamide liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Tetrazinedicarboxamide liposome preparation, this liposome comprises following composition and quality:

[0034] Tetrazine dicarboxamide: 4mg;

[0035] Cholesterol: 20mg;

[0036] Lecithin (PC content 98%): 100mg;

[0037] Ethanol: 10mL;

[0038] Phosphate buffer solution (pH 6.8): 20 mL.

[0039] Dissolve the prescribed amount of tetrazinedicarboxamide, lecithin, and cholesterol in ethanol, stir and dissolve to prepare solution A; put solution A in a flask, and use a rotary evaporator to remove the organic solvent ethanol, and the constant temperature water bath of the rotary evaporator is 45 °C, rotation speed 100r / min, vacuum degree greater than 0.09MPa, wait for a dry film to form on the bottle wall, and continue to evaporate until the solvent evaporates completely. Add the prescribed amount of phosphate buffered saline solution in the flask, and the probe is ultrasonicated for 10 minutes for hydration, and the solution is filtered with a 0.45um microporous memb...

Embodiment 2

[0042] Tetrazinedicarboxamide liposome preparation, this liposome comprises following composition and quality:

[0043] Tetrazine dicarboxamide: 4mg;

[0044] Cholesterol: 15mg;

[0045] Lecithin (PC content 98%): 150mg;

[0046] Vitamin E: 2mg;

[0047] Diethyl ether: 15mL;

[0048] Phosphate buffer solution (pH 6.4): 25 mL.

[0049]Dissolve the prescribed amount of tetrazinedicarboxamide, lecithin, cholesterol, and vitamin E in ether, stir and dissolve to prepare solution A; inject solution A into the continuously stirring phosphate buffer solution through the syringe, and obtain a milky white mixture solution, the mixed solution is placed in a 55°C constant temperature water bath, continuously stirred, the organic solvent is volatilized and removed, and then filtered with a 0.45um microporous membrane to obtain a slightly clear milky white drug liposome solution.

[0050] The obtained tetrazinedicarboxamide liposome solution has a particle diameter of 105.4 nm, a polyd...

Embodiment 3

[0052] Tetrazinedicarboxamide liposome preparation, this liposome comprises following composition and quality:

[0053] Tetrazine dicarboxamide: 8mg;

[0054] Cholesterol: 10mg;

[0055] Soy lecithin (PC content 70%): 80mg;

[0056] Vitamin E: 6mg;

[0057] Chloroform: 25mL;

[0058] Phosphate buffer solution (pH 7.0): 12 mL.

[0059] Dissolve the prescribed amount of tetrazinedicarboxamide, lecithin, cholesterol, and vitamin E in chloroform, and ultrasonically dissolve to prepare solution A; put solution A in a flask, use a rotary evaporator to remove the organic solvent ethanol, and use a rotary evaporator to keep the temperature constant The temperature of the water bath is 40°C, the rotation speed is 100r / min, and the vacuum degree is greater than 0.09MPa. After a dry film is formed on the bottle wall, continue to evaporate until the solvent evaporates completely. Add the prescribed amount of phosphate buffered saline solution in the flask, and the probe is ultrasonic...

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Abstract

The invention discloses a tetrazine diformamide liposome preparation and a preparation method thereof. The preparation is prepared from, by weight, 1.0-2.0 parts of tetrazine diformamide, 12.5-62.5 parts of phospholipid, 2.5-6.25 parts of cholesterol, 0-2.0 parts of vitamin E, 2.5-7.5 parts of an organic solvent and 3000-11000 parts of a phosphate buffering solution, wherein the phospholipid material is one of lecithin, soybean phospholipid, phosphatidyl inositol, phosphatidylserine, phosphatidyl glycerol and sphingomyelin, the organic solvent is one of alcohol, ethyl ether, chloroform and dichloromethane, and pH value of the phosphate buffering solution is 6.4-7.6. A liposome solution is prepared through a thin film dispersion method or an injection method, and the organic solvent in a medicine solution is removed by selecting a method of vacuum drying or constant-temperature heating and stirring in the preparation process, so that residue of the organic solvent is avoided.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of a new tetrazine dicarboxamide dosage form, in particular to a tetrazine dicarboxamide liposome preparation and a preparation method thereof. Background technique [0002] Tetrazine, also known as tetraazine, is a class of anti-tumor compounds with good biological activity. Tetrazine dicarboxamide (ZGDHu21) was synthesized by Hu Weixiao and others. It is a new type of tetrazine compound with independent intellectual property rights. It can Inhibit the proliferation of leukemia cells, lung cancer cells, liver cancer cells, gastric cancer cells, etc., and play a certain role in inducing differentiation and apoptosis. In vivo activity studies in nude mice show that tetrazinedicarboxamide has good therapeutic activity on lung cancer. Statistics show that lung cancer is the malignant tumor with the highest morbidity and mortality among men toda...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/395A61P35/00
CPCA61K9/127A61K31/395
Inventor 石雷吴翰桂刘永丽梅艳丘永秀金琳琳
Owner 石雷
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