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Anti-tumor adjuvant drug calcium folinate composition

A technology of calcium folinate and adjuvant medicine, applied in the field of medicine, can solve the problems of increased preparation cost, poor stability during storage period, instability, etc., and achieves the effects of low content of insoluble particles, improved fluidity and good stability

Inactive Publication Date: 2015-12-23
杨献美
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The solubility of calcium folinate in water is not ideal. In practice, it is found that calcium folinate is not easy to dissolve when the water temperature is lower than 30°C. If the dissolution is not good, the content will decrease. It is sensitive to factors such as temperature, PH value, and oxygen, resulting in the increase of related substances. , unstable, easy to decompose when exposed to light, and poor storage stability, which limits the application and clinical application of its preparations, and increases the cost of preparations
Although calcium folinate reduces the toxic effect of the antineoplastic drug MTX, its toxic effect cannot be ignored
The existing technology solves the problems of water solubility and stability by changing the excipients and preparation methods of the preparation. It must rely on specific prescriptions and processes to achieve its stable effect, which brings certain limitations to the preparation of preparations and the selection of excipients. sex

Method used

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  • Anti-tumor adjuvant drug calcium folinate composition
  • Anti-tumor adjuvant drug calcium folinate composition
  • Anti-tumor adjuvant drug calcium folinate composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of Calcium Folinate Crystals

[0023] (1) Grind the crude calcium folinate, pass through a 90-mesh sieve, add it to 45% aqueous solution of N-methylacetamide, and raise the temperature to 30°C while stirring; mix the crude calcium folinate with 45% N-methyl The weight ratio of the acetamide aqueous solution is 1:10; the stirring speed is 180 rpm; adding activated carbon, stirring for 50 minutes and sterile filtering;

[0024] (2) Add ethanol while stirring, and lower the temperature to -5°C at the same time; the stirring speed is 240 rpm; the weight of ethanol is 7 times the weight of the mixed solution of calcium folinate and 45% N-methylacetamide aqueous solution, add The speed is 95 ml / min; the cooling rate is 10°C / hour;

[0025] (3) After adding the mixed solvent, the obtained crystals were left to stand for crystallization; filtered, washed, and dried in vacuum for 6 hours to obtain the calcium folinate compound.

[0026] The X-ray powder...

Embodiment 2

[0027] Example 2: Preparation of calcium folinate composition

[0028] The composition is: 1 part by weight of the calcium folinate crystal prepared by the present invention, and 0.001 part by weight of anhydrous sodium carbonate.

[0029] The preparation method is:

[0030] (1) Weigh calcium folinate crystals and anhydrous sodium carbonate in proportion and mix them thoroughly;

[0031] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0032] Example 3: Preparation of calcium folinate composition

[0033] The composition is: 1 part by weight of the calcium folinate crystal prepared by the present invention, and 0.0015 part by weight of anhydrous sodium carbonate.

[0034] The preparation method is:

[0035] (1) Weigh calcium folinate crystals and anhydrous sodium carbonate in proportion and mix them thoroughly;

[0036] (2) Dispense into sterilized vials and stopper them.

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Abstract

The invention belongs to the technical field of medicines and relates to anti-tumor adjuvant drug calcium folinate composition. The composition comprises calcium folinate and anhydrous sodium carbonate, wherein the calcium folinate is crystal, and an X-ray powder diffraction diagram obtained through measurement by Cu-K alpha rays is shown in figure 1. The new crystal form of provided calcium folinate is different from a structure of a crystal form in the prior art. A test proves that compared with the prior art, the provided composition with the calcium folinate crystal form has good stability and low impurity content; by comparison with the prior art, the solubility and the flowability in water are remarkably improved, and the problems of poor water solubility of calcium folinate, poor stability and high content of related substances in the prior art are solved, convenience is provided for preparation of a preparation, and the medicine efficacy is greatly improved. A powder injection prepared from the new crystal-form composition has good stability, contains very few insoluble microparticles, is very suitable for clinic application and has good stability after being compatible with a solvent.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a calcium leucovorin composition for anti-tumor auxiliary medicine. Background technique [0002] Calcium folinate has a detoxifying effect on methotrexate (MTX). MTX is a folic acid antagonist. The anti-tumor mechanism of MTX is that its structure is similar to folic acid, which can inhibit the activity of dihydrofolate reductase, resulting in the lack of tetrahydrofolate (FH4) in cells, thereby affecting the synthesis of purine and pyrimidine nucleotides. Inhibits tumor cell growth. While MTX inhibits the growth of tumor cells, it also makes normal cells, especially fast-growing cells, lack FH4, resulting in greater toxicity. Therefore, the anti-tumor effect of MTX not only depends on its inhibition of tumor cells, but also the body's tolerance to MTX affects its final result. CF is a formylated derivative of folic acid reduction, which is the activated form of folic acid in ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/14A61P35/00C07D475/04
Inventor 杨献美
Owner 杨献美
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