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Antidote calcium folinate composition for folic acid antagonist

The technology of folic acid antagonist and calcium folinate, which is applied in the field of medicine, can solve the problems of increased preparation cost, poor stability during storage period, instability and the like, and achieves the effects of low content of insoluble particles, improved fluidity and improved drug efficacy

Inactive Publication Date: 2015-12-16
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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  • Antidote calcium folinate composition for folic acid antagonist
  • Antidote calcium folinate composition for folic acid antagonist
  • Antidote calcium folinate composition for folic acid antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of Calcium Folinate Crystals

[0024] 1) Prepare mixed solution A by mixing dimethylformamide and water at a volume ratio of 1:4;

[0025] 2) Take the raw material of calcium folinate, add the mixed solution A prepared in step 1), wherein the ratio of the volume of the mixed solution A to the mass of calcium folinate is 10ml:1g, stir to dissolve all of it, and pour it into the obtained solution Add 0.1% g / ml activated carbon to decolorize and filter to obtain a clear solution;

[0026] 3) Prepare mixed solution B with isopropyl ether and isopropanol at a volume ratio of 2:3.5;

[0027] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) under an ultrasonic field with a power of 0.6KW, where the amount of mixed solution B added is 5 times the volume of mixed solution A, and turn off the ultrasonic field after adding , cooled to 0° C., left standing for 3 hours, crystals were precipitated, and dried to obtain t...

Embodiment 2

[0029] Example 2: Preparation of calcium folinate composition

[0030] The composition is: 1 part by weight of the calcium folinate crystal prepared by the present invention, and 0.003 part by weight of sodium dihydrogen phosphate.

[0031] The preparation method is:

[0032] (1) Weigh calcium folinate crystals and sodium dihydrogen phosphate in proportion, and mix them thoroughly;

[0033] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0034] Example 3: Preparation of calcium folinate composition

[0035] The composition is: 1 part by weight of the calcium folinate crystal prepared by the present invention, and 0.004 part by weight of sodium dihydrogen phosphate.

[0036] The preparation method is:

[0037] (1) Weigh calcium folinate crystals and sodium dihydrogen phosphate in proportion, and mix them thoroughly;

[0038] (2) Dispense into sterilized vials and stopper them.

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Abstract

The invention discloses an antidote calcium folinate composition for a folic acid antagonist, and belongs to the technical field of medicines. The composition comprises calcium folinate and sodium biphosphate, wherein calcium folinate is a crystal; the X-ray powder diffraction pattern of calcium folinate is measured by using Cu-K alpha rays and shown in figure 1. The new crystal structure of calcium folinate provided by the invention differs from the conventional crystal structure; tests prove that the composition, namely a calcium folinate crystal compound, has higher stability and a lower impurity content than that in the prior art; besides, compared with those in the prior art, the solubility and liquidity of the calcium folinate crystal compound in water are obviously improved, so that convenience is provided for preparation production and the medicine effect is greatly improved; a powder injection prepared by utilizing the new crystal compound is high in stability, and the stability is kept high after the new crystal compound is compatible with a solvent; the content of insoluble particles is extremely low; the new crystal compound is very suitable for clinical application.

Description

Technical field [0001] The present invention is a pharmaceutical technology field and involves a detoxifying agent of a folic acid antagonist. Background technique [0002] Calcium foliar acid has a detoxifying effect on methotrexate (MTX).MTX is a folic acid antagonist. The mechanism of anti -tumor action of MTX is that its structure is similar to folic acid, which can inhibit the activity of dihydrocarbonate restoration enzymes, resulting in cell tetrahydrogen folic acid (FH4) deficiency, which affects the synthesis of purine and pyrine nucleotide.Inhibit the growth of tumor cells.The MTX inhibits tumor cell growth while making normal cells, especially the fast -growing intracellular FH4 deficiency, and has a large toxic effect.Therefore, the anti -tumor effect of MTX depends not only on its inhibition of tumor cells, but the body's tolerance to MTX also affects its final result.CF is a formalized derivative of folic acid. It is a activated form of folic acid in the body. It ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/14A61K47/02A61P39/02C07D475/04
Inventor 杨献美
Owner 杨献美
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