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Brain neurotrophic drug meclofenoxate hydrochloride composition

A technology of meclofenoxate hydrochloride and composition, which is applied in the field of meclofenoxate hydrochloride composition of brain neurotrophic drug, can solve the problems of high occurrence rate of side reactions and low bioavailability, and achieve low moisture and impurity content, High bioavailability, high bioavailability effect

Inactive Publication Date: 2016-02-24
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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  • Brain neurotrophic drug meclofenoxate hydrochloride composition
  • Brain neurotrophic drug meclofenoxate hydrochloride composition
  • Brain neurotrophic drug meclofenoxate hydrochloride composition

Examples

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Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of Meclofenoxate Hydrochloride Crystals

[0020] Dissolve meclofenoxate hydrochloride in a mixed solvent of water and acetonitrile whose volume is 10 times the weight of meclofenoxate hydrochloride at 35 ° C. The volume ratio of water and acetonitrile is 3:1. After the dissolution is completed, add a volume of hydrochloric acid Diethyl ether solvent 6 times the weight of meclofenoxate, the temperature was lowered to room temperature within 2 hours, kept at room temperature for 3 hours, then further cooled to -5°C, and then placed at -5°C for 3 hours, crystals were precipitated , to obtain crystals of meclofenoxate hydrochloride.

[0021] The X-ray powder diffraction pattern that the prepared meclofenoxate hydrochloride crystal uses Cu-Kα ray to measure is as follows figure 1 shown.

Embodiment 2

[0022] Example 2: The preparation of meclofenoxate hydrochloride composition

[0023] The composition is: 1 part by weight of meclofenoxate hydrochloride crystal prepared by the present invention, and 0.01 part by weight of arginine.

[0024] The preparation method is:

[0025] (1) Weigh meclofenoxate hydrochloride crystals and arginine in proportion and mix them thoroughly;

[0026] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0027] Example 3: The preparation of meclofenoxate hydrochloride composition

[0028] The composition is: 1 part by weight of meclofenoxate hydrochloride crystal prepared by the present invention, and 0.02 part by weight of arginine.

[0029] The preparation method is:

[0030] (1) Weigh meclofenoxate hydrochloride crystals and arginine in proportion and mix them thoroughly;

[0031] (2) Dispense into sterilized vials and stopper them.

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Abstract

The invention belongs to the technical field of medicine and relates to a brain neurotrophic drug meclofenoxate hydrochloride composition, comprising meclofenoxate hydrochloride and arginine. The meclofenoxate hydrochloride is a crystal, its X-ray powder diffraction pattern measured using Cu-KAlpha ray is shown as in Figure 1. The novel crystal form of the meclofenoxate hydrochloride is different from prior art crystal form structures, experiments show that the meclofenoxate hydrochloride crystal form compound has significantly improved moisture absorption and fluidity when compared to the prior art, the moisture and impurity content is very low, the stability is better, and the preparation of preparations is facilitated. Compared with the prior art, the meclofenoxate hydrochloride crystal form compound is higher in bioavailability and lower in side effect rate. Compared with the prior art, a powder injection made with the novel crystal from compound has good fluidity, very low moisture and impurity content, better stability, high bioavailability and low side effect rate.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a brain neurotrophic drug meclofenoxate hydrochloride composition. 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 learnin...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P25/00C07C213/10C07C219/06
CPCA61K31/216A61K9/145C07B2200/13C07C213/10
Inventor 杨献美
Owner 杨献美
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