Meclofenoxate hydrochloride compound and pharmaceutical composition thereof

A technology for meclofen axetil and a compound, applied in the field of medicine, can solve the problems of high storage conditions, unstable raw material stages of easy hydrolysis of meclofen axetil, easy hydrolysis of meclofen axetil, etc.

Active Publication Date: 2014-10-15
HUNAN WUZHOUTONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the existing technology has a certain effect in improving the stability of meclofenoxate hydrochloride in preparation, it needs to add more auxiliary materials and needs to cooperate with relatively complicated processes. Although it has a certain effect, the effect is limited, which limits the application of meclofenoxate hydrochloride. , because the easily hydrolyzed meclofenoxate hydrochloride is unstable in the raw material stage and requires extremely high storage conditions
There are also prior art attempts to obtain meclofenoxate hydrochloride with higher stability from changing the crystal form, such as: Chinese application CN103214382A, the meclofenoxate hydrochloride compound and its drug combination provided by this application are compared with the prior art , have better storage stability and fluidity, and the inventors have found in tests that although the meclofenoxate hydrochloride obtained in this application has good stability under normal temperature and accelerated conditions, it is not effective in other conditions that affect the quality of drugs. Poor stability in the factor test, especially still has high hygroscopicity, which makes meclofenoxate hydrochloride easy to attract moisture and hydrolyze

Method used

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  • Meclofenoxate hydrochloride compound and pharmaceutical composition thereof
  • Meclofenoxate hydrochloride compound and pharmaceutical composition thereof
  • Meclofenoxate hydrochloride compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1 The preparation of meclofenoxate hydrochloride compound

[0048] 1. Add the raw material of meclofenoxate hydrochloride into the mixed solution of chloroform and ethanol with a volume ratio of 9:1 at a weight ratio of 1:15, adjust the temperature of the solution to 30°C, and stir to dissolve.

[0049] 2. Keep the solution temperature at 30°C, add activated carbon with a weight of 0.7% of the weight of meclofenoxate hydrochloride, stir at 120 rpm for 25 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane to obtain the filtrate;

[0050] 3. Adjust the temperature of the filtrate to 22°C, and at a stirring speed of 90 rpm, slowly and uniformly add the weight of the mixture of chloroform and ethanol in step 1 to the filtrate obtained in step 1 at a speed of 50ml / min while stirring. Double the volume ratio of the mixed solution of diethyl ether and petroleum ether with a volume ratio of 8:2; at the same time, cool down to 8°...

Embodiment 2

[0053] Embodiment 2 Preparation of Meclofenoxate Hydrochloride Compound

[0054] 1. Add the raw material of meclofenoxate hydrochloride into the mixed solution of chloroform and ethanol with a volume ratio of 9:1 at a weight ratio of 1:18, adjust the temperature of the solution to 35°C, and stir to dissolve.

[0055] 2. Keep the solution temperature at 35°C, add activated carbon with a weight of 0.7% of the weight of meclofenoxate hydrochloride, stir at 150 rpm for 25 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane to obtain the filtrate;

[0056] 3. Adjust the temperature of the filtrate to 27°C, and at a stirring speed of 110 rpm, slowly and uniformly drop the weight of the mixture of chloroform and ethanol in step 1 to the filtrate obtained in step 2 at a speed of 75ml / min while stirring. Double the volume ratio of the mixed solution of diethyl ether and petroleum ether with a volume ratio of 8:2; at the same time, cool down to 10...

Embodiment 3

[0059] Example 3 Preparation of Meclofenoxate Hydrochloride Freeze-dried Powder (Specification: 0.06g)

[0060] prescription:

[0061] Meclofenoxate hydrochloride compound: 60g

[0062] Mannitol: 240g

[0063] Add water for injection to 2000ml

[0064]

[0065] Made 1000 pieces

[0066] Process:

[0067] 1. Add the prescribed amount of meclofenoxate hydrochloride into 1400ml of water for injection, stir to dissolve, add water for injection to 1600ml, then add mannitol according to the prescribed amount, stir to dissolve, add water for injection to 2000ml, and stir evenly.

[0068] 2. Add 0.10% (g / ml) activated carbon to 1, stir for 20 minutes, decarbonize by filtration, sterilize by filtration with 0.22μm filter membrane, and carry out intermediate detection.

[0069] 3. Freeze-drying:

[0070] ① Pre-freezing: Put the filtrate in 2 into a half-pack and put it in a freezer that has been cooled to -24°C in advance, keep it for 1.5 hours, ...

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Abstract

Meclofenoxate hydrochloride compound, described meclofenoxate hydrochloride compound is crystal, adopts X-ray powder diffraction to measure, and characteristic peak is 6.1°, 7.7°, 9.3°, 12.2°, 14.3°, 17.8°, 18.9°, 20.5°, 22.2°, 23.3°, 24.5°, 25.8°, 27.0° display. The pharmaceutical composition preparation of the above-mentioned meclofenoxate hydrochloride compound, the described pharmaceutical composition preparation is a dispersible tablet, a capsule, a freeze-dried powder injection and a sterile powder for injection. In addition to stable quality, the meclofenoxate hydrochloride compound of the present invention also has the characteristics of excellent fluidity. The active ingredient prepared by the invention is the dispersible tablet, capsule and freeze-dried powder of meclofenoxate hydrochloride prepared by the invention, which has good stability and low impurity content.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a meclofenoxate hydrochloride compound and a pharmaceutical composition thereof. Background technique [0002] Meclofenoxate hydrochloride, chemical name: 2-(dimethylamino)ethyl p-chlorophenoxyacetate hydrochloride. Meclofenoxate hydrochloride mainly acts on the cerebral cortex. It can promote the redox of brain cells, regulate the metabolism of nerve cells, increase the utilization of carbohydrates and have an excitatory effect on the inhibited central nervous system. It is suitable for traumatic coma, enuresis in children, disturbance of consciousness, senile psychosis, various dementias, alcoholism, etc. [0003] Meclofenoxate hydrochloride has poor stability, and because of containing ester bond in the molecule, the aqueous solution is unstable and easily hydrolyzed. As the pH of the aqueous solution increases, the rate of hydrolysis increases. In order to solve this proble...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C219/06C07C213/10A61K31/216A61P25/26A61P25/28
Inventor 李美林马虹
Owner HUNAN WUZHOUTONG PHARMA
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