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Central stimulant meclofenoxate hydrochloride composition

A technology of meclofenoxate hydrochloride and composition, which is applied in the field of meclofenoxate hydrochloride composition of the central nervous system stimulant, can solve the problems of high incidence of side reactions and low bioavailability, and achieve low moisture and impurity content, biological High utilization and good stability

Inactive Publication Date: 2015-12-02
杨献美
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention also provides a composition preparation whose active ingredient is the meclofenoxate hydrochloride compound described in the present invention and a preparation method thereof. The preparation that can be prepared according to the content of the present invention maintains extremely high stability, which is obviously better than the commercially available variety, greatly improving the safety and effectiveness of meclofenoxate hydrochloride use, but its bioavailability is low and the incidence of side effects is high

Method used

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  • Central stimulant meclofenoxate hydrochloride composition
  • Central stimulant meclofenoxate hydrochloride composition
  • Central stimulant meclofenoxate hydrochloride composition

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Example 1: Preparation of Meclofenoxate Hydrochloride Crystals

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

[0024] (2) Add diethyl ether while stirring, and lower the temperature to -5°C at the same time; the stirring speed is 240 rpm; the weight of diethyl ether is 7 times the weight of the mixed solution of meclofenoxate hydrochloride and 45% N-methylacetamide aqueous solution , the adding rate 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 to obtain the meclofenoxate hydrochloride...

Embodiment 2

[0027] Example 2: The preparation of meclofenoxate hydrochloride composition

[0028] The composition comprises: 1 part by weight of meclofenoxate hydrochloride crystal prepared by the present invention, and 0.1 part by weight of anhydrous sodium carbonate.

[0029] The preparation method is:

[0030] (1) Weigh meclofenoxate hydrochloride 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: The preparation of meclofenoxate hydrochloride composition

[0033] The composition comprises: 1 part by weight of meclofenoxate hydrochloride crystal prepared by the present invention, and 0.15 part by weight of anhydrous sodium carbonate.

[0034] The preparation method is:

[0035] (1) Weigh meclofenoxate hydrochloride 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 relates to a central stimulant meclofenoxate hydrochloride composition and belongs to the technical field of medicines. The composition is prepared from meclofenoxate hydrochloride and anhydrous sodium carbonate, wherein the meclofenoxate hydrochloride is crystal and an X-ray powder diffraction pattern obtained through measurement by using Cu-K alpha rays is as shown in picture 1. The new crystal form of the meclofenoxate hydrochloride provided by the invention is different from the crystal form structures in the prior art. As proved by tests, compared with the prior art, the meclofenoxate hydrochloride crystal compound provided by the invention has the advantages that the moisture absorption and flowability are obviously improved, the content of water and impurities is extremely low, the stability is better and convenience is provided for the preparation of preparations. Compared with the prior art, the meclofenoxate hydrochloride crystal compound provided by the invention has higher bioavailability and the side reaction rate is reduced. Compared with the prior art, powder-injection prepared by using the compound of the new crystal form has the advantages of good flowability, extremely low content of water and impurities, better stability, high bioavailability and low side reaction rate.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a composition of meclofenoxate hydrochloride, a central stimulant drug. Background technique [0002] The chemical name of meclofenoxate hydrochloride is 2-(dimethylamino)ethyl p-chlorophenoxy acetate hydrochloride, which is a central nervous system stimulant and brain neurotrophic drug, which can improve the central nervous system Functions, including causing awakening, invigorating the spirit, exciting breathing, improving nerve reflexes and increasing free activities, it can promote protein assimilation, and can be used as raw materials for the synthesis of choline and acetylcholine in the body, and then synthesize lecithin, thereby changing the neurotransmitter of the central nervous system content, increase the amount of acetylcholine in the brain, have an anti-hypoxic effect, promote the oxidation-reduction reaction of brain cells, promote brain energy metabolism, improve le...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61K9/14C07C219/06C07C213/10A61P25/26
Inventor 杨献美
Owner 杨献美
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