Meclofenoxate hydrochloride compound and pharmaceutical composition thereof

A technology for meclofen axetil hydrochloride and a compound, applied in the field of medicine, can solve the problems of reducing the content of the active ingredient meclofen axetil hydrochloride, increasing the medication risk of patients, increasing the content of impurities, etc., so as to improve storage stability and improve medication safety. , the effect of less impurity content

Active Publication Date: 2013-07-24
SHANXI C&Y PHARMACEUTICAL GROUP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The meclofenoxate hydrochloride provided in the above-mentioned patents and the prior art is basically obtained by crystallization in isopropanol. The stability of the meclofenoxate hydrochloride is poor, and the impurity content continues to increase after long-term storage. The active ingredient meclofenoxate hydrochloride The content of esters is reduced, which increases the risk of medication for patients

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

[0042] The preparation of meclofenoxate hydrochloride compound:

[0043]Dissolve the meclofenoxate hydrochloride crude drug 50 in 150ml of n-butanol, place it in a 60°C water bath, stir for 30 minutes, slowly add acetone dropwise, and the stirring rate during the dropwise addition of acetone is 27rpm, the acetone and n-butanol The volume ratio of the solution is 1:5, continue to stir for 20 minutes after the dropwise addition, add activated carbon, the amount of activated carbon is 0.2% g / ml of the total volume of the liquid, stir for 20 minutes, filter, stand for more than 24 hours, volatilize the solvent and grow crystals , cooled to 0°C, filtered to obtain a filter cake, washed the filter cake, and then dried under reduced pressure for 4 hours to obtain a white microcrystalline powder. Yield 71.2%, HPLC content 99.85%. mp: 182-185°C.

[0044] The X-ray powder diffraction spectrum obtained by Cu-Kα ray measurement is figure 1 displayed.

Embodiment 2

[0046] The preparation of meclofenoxate hydrochloride compound:

[0047] Dissolve the meclofenoxate hydrochloride crude drug 50 in 250ml of n-butanol, place it in a water bath at 50°C to insulate, stir for 20 minutes, slowly add acetone dropwise, and the stirring rate during the dropwise addition of acetone is 28rpm, the acetone and n-butanol The volume ratio of the solution is 1:8. After the dropwise addition, continue to stir for 30 minutes, add activated carbon, the amount of activated carbon is 0.3% g / ml of the total volume of the liquid, stir for 20 minutes, filter, stand for more than 24 hours, volatilize the solvent and grow crystals , cooled to 5°C, filtered to obtain a filter cake, washed the filter cake, and then dried under reduced pressure for 2 hours to obtain a white microcrystalline powder. Yield 70.9%, HPLC content 99.88%. mp: 182-185°C.

[0048] The X-ray powder diffraction pattern obtained by Cu-Kα ray measurement is consistent with the result of Example 1....

Embodiment 3

[0050] Meclofenoxate hydrochloride sterile powder injection

[0051] Weigh 998 g of meclofenoxate hydrochloride and 2 g of sodium benzoate prepared in Example 1 under aseptic conditions, place them in a solid powder mixer and mix them evenly, and the raw materials obtained are transferred to a sterile preparation workshop for precise metering and subpackaging. Each bottle contains Meclofenoxate hydrochloride 0.25g, stoppered and capped, the finished product is packaged for storage and sent for inspection.

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Abstract

The invention provides a meclofenoxate hydrochloride compound. A structural formula of the meclofenoxate hydrochloride compound is as shown in the specification, and the meclofenoxate hydrochloride compound uses an X-ray powder diffraction spectrogram obtained through Cu-K alpha ray measurement, as shown in Figure 1 in the specification. The invention further provides a preparation method of the meclofenoxate hydrochloride compound, and a pharmaceutical composition containing the meclofenoxate hydrochloride compound. The pharmaceutical composition of the meclofenoxate hydrochloride compound is an aseptic powder injection, a freeze-drying powder injection, a dispersible tablet, a tablet or oral liquid. Compared with the prior art, the meclofenoxate hydrochloride compound and the pharmaceutical composition of the meclofenoxate hydrochloride compound have better storage stability and fluidity, and greatly improve the medication safety of a patient.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a meclofenoxate hydrochloride compound, a preparation method of the meclofenoxate hydrochloride compound and a pharmaceutical composition thereof. Background technique [0002] Meclofenoxate Hydrochloride, English name Meclofenoxate Hydrochloride, chemical name 2-(dimethylamino)ethyl p-chlorophenoxy acetate hydrochloride, is a white crystalline powder, easily soluble in water. [0003] 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 clinically used as a central nervous system stimulant, which can regulate the metabolism of nerve cells and promote their excitability. Studies have shown that it also has the effects of delaying aging, preventing Alzheimer's...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C219/06C07C213/10A61K31/216A61P25/26A61P25/28
Inventor 梁宏平
Owner SHANXI C&Y PHARMACEUTICAL GROUP CO LTD
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