Unlock instant, AI-driven research and patent intelligence for your innovation.

Antidote calcium folinate composition granules as folic acid antagonist

A technology of folic acid antagonist and calcium folinate, which is applied in the field of medicine, can solve problems such as unsatisfactory solubility of calcium folinate, non-negligible toxic effects, poor storage stability, etc., to achieve clinical application, solve poor water solubility, and stable good sex effect

Inactive Publication Date: 2015-12-02
杨献美
View PDF0 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Antidote calcium folinate composition granules as folic acid antagonist
  • Antidote calcium folinate composition granules as folic acid antagonist
  • Antidote calcium folinate composition granules as folic acid antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Calcium Folinate Crystals

[0025] Dissolve calcium folinate in a mixed solvent of water and dimethyl sulfoxide whose volume is 6 times the weight of calcium folinate at 35°C. The volume ratio of water to dimethyl sulfoxide is 5:1.5; Add the mixed solvent of ethanol and ether whose volume is 9 times of the weight of calcium folinate at a high speed, the volume ratio of ethanol and ether is 2:2, stir while adding, control the temperature at 35°C, grow the crystal for 3 hours; then add 20 ml Add isopropanol whose total volume is 7 times of the weight of calcium folinate at a speed of 1 / min. After growing the crystal for 1 hour, cool down to -5°C at a speed of 10°C / hour, and then keep stirring at a speed of 90 rev / min. crystallization and crystal growth for 3 hours; filtering, washing, and drying under reduced pressure to obtain calcium folinate crystal compound.

[0026] The X-ray powder diffraction pattern that the prepared calcium folinate c...

Embodiment 2

[0027] Example 2: Preparation of Calcium Folinate Granules

[0028] Prescription: in parts by weight

[0029]

[0030] Preparation:

[0031] (1) Weighing: Weighing according to the process prescription;

[0032] (2) Processing of raw and auxiliary materials: crush calcium folinate through a 100-mesh sieve;

[0033] (3) Mixing granulation: Add calcium folinate, mannitol, dioctyl sodium sulfosuccinate, and sucralose into the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared Wet mixed cutting with 95% ethanol, and made soft material with 16-mesh sieve;

[0034] (4) Drying and sieving: distribute the wet granules obtained from granulation evenly on the baking tray of the oven, set the temperature at 60-65°C, and the total drying time is 2.5-3.0 hours, and sieve the material to 16-30 mesh after drying;

[0035] (6) Mixing: Put the sieved particles into the three-dimensional motion mixer, set the pre-mixing speed to 10 rpm, and t...

Embodiment 3

[0037] Example 3: Preparation of Calcium Folinate Granules

[0038] Prescription: in parts by weight

[0039]

[0040] Preparation:

[0041] (1) Weighing: Weighing according to the process prescription;

[0042] (2) Processing of raw and auxiliary materials: crush calcium folinate through a 100-mesh sieve;

[0043] (3) Mixing granulation: Add calcium folinate, mannitol, dioctyl sodium sulfosuccinate, and sucralose into the wet mixing granulator, turn on the stirring motor and dry mix for 10 minutes; add the prepared Wet mixed cutting with 95% ethanol, and made soft material with 16-mesh sieve;

[0044] (4) Drying and sieving: distribute the wet granules obtained from granulation evenly on the baking tray of the oven, set the temperature at 60-65°C, and the total drying time is 2.5-3.0 hours, and sieve the material to 16-30 mesh after drying;

[0045](6) Mixing: Put the sieved particles into the three-dimensional motion mixer, set the pre-mixing speed to 10 rpm, and th...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the technical field of medicines, and relates to antidote calcium folinate composition granules as a folic acid antagonist. The composition is prepared from calcium folinate, mannitol, dioctyl sodium sulfosuccinate, sucralose and 95% ethyl alcohol. The calcium folinate is a new crystal form compound and is different from calcium folinate reported in existing technologies as shown in picture 1 of X-ray powder diffraction diagram obtained by Cu-Ka ray measurement; and as discovered in experiments, the calcium folinate crystal form compound provided by the invention is good in stability, low in impurity and good in stability compared with the existing technology, the solubility and mobility in water are remarkably improved compared with the prior art, and the problem that calcium folinate in the existing technology is poor in water solubility and stability and high in related substances is solved; the calcium folinate crystal form compound provides convenience for preparation of preparations, and the pharmacological efficacy is also greatly improved. The granules prepared from the new crystal form compound are good in stability, high in bioavailability and very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a folic acid antagonist antidote calcium folinate composition granule. 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 ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/16A61K31/519C07D475/04A61P35/00A61P39/02
Inventor 杨献美
Owner 杨献美