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Meclofenoxate hydrochloride pharmaceutical composition capable of promoting brain energy metabolism

A technology of meclofenoxate hydrochloride and energy metabolism, applied in the field of medicine, can solve the problems of high incidence of side reactions, limited effect, and low bioavailability, and achieve low water and impurity content, high bioavailability, and bioavailability high degree of effect

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

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
Some prior art attempts to obtain meclofenoxate hydrochloride with higher stability by changing the crystal form, such as: Chinese application CN103214382B, the meclofenoxate hydrochloride compound and its drug combination provided by this application compared with the prior art, have Better storage stability and fluidity, the inventor found in the test that although the meclofenoxate hydrochloride obtained in the application has good stability under normal temperature and accelerated conditions, it has not been tested in other factors affecting drug quality. Poor stability in medium, especially still has high hygroscopicity, which makes meclofenoxate hydrochloride easy to attract moisture and hydrolyze
Chinese application CN103396328B, the inventor of this application unexpectedly obtained a crystal form of meclofenoxate hydrochloride compound in the course of long-term and extensive research. This compound has very low hygroscopicity, is not easy to hydrolyze by hygroscopicity, and has extremely high quality stability. However, its bioavailability is low and the incidence of side effects is high

Method used

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  • Meclofenoxate hydrochloride pharmaceutical composition capable of promoting brain energy metabolism
  • Meclofenoxate hydrochloride pharmaceutical composition capable of promoting brain energy metabolism
  • Meclofenoxate hydrochloride pharmaceutical composition capable of promoting brain energy metabolism

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of Meclofenoxate Hydrochloride Crystals

[0023] 1) Prepare mixed solution A by mixing dimethylformamide and water at a volume ratio of 1:4;

[0024] 2) Take the meclofenoxate hydrochloride raw material, add the mixed solution A prepared in step 1), wherein the ratio of the volume of the mixed solution A to the mass of meclofenoxate hydrochloride is 10ml:1g, stir to dissolve all Add 0.1% g / ml activated carbon to the resulting solution for decolorization and filtration to obtain a clear solution;

[0025] 3) Prepare mixed solution B with isopropyl ether and isopropanol at a volume ratio of 5:1.5;

[0026] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) under an ultrasonic field with a power of 0.6KW, where the amount of mixed solution B added is 5 times the volume of mixed solution A, and turn off the ultrasonic field after adding , cooled to 0° C., allowed to stand for 3 hours, crystals were precipitated,...

Embodiment 2

[0028] Example 2: The preparation of meclofenoxate hydrochloride composition

[0029] The composition is: 1 part by weight of meclofenoxate hydrochloride crystal prepared by the present invention, and 0.05 part by weight of sodium dihydrogen phosphate.

[0030] The preparation method is:

[0031] (1) Weigh meclofenoxate hydrochloride crystals and sodium dihydrogen phosphate in proportion, and mix them thoroughly;

[0032] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0033] Example 3: The preparation of meclofenoxate hydrochloride composition

[0034] The composition is: 1 part by weight of meclofenoxate hydrochloride crystal prepared by the present invention, and 0.06 part by weight of sodium dihydrogen phosphate.

[0035] The preparation method is:

[0036] (1) Weigh meclofenoxate hydrochloride crystals and sodium dihydrogen phosphate in proportion, and mix them thoroughly;

[0037] (2) Dispense into sterilized vials and stopper them.

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PUM

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Abstract

The invention discloses a meclofenoxate hydrochloride pharmaceutical composition capable of promoting brain energy metabolism, and belongs to the technical field of medicines. The composition is prepared from meclofenoxate hydrochloride and sodium dihydrogen phosphate, wherein the meclofenoxate hydrochloride is crystal, and an X-ray powder diffraction pattern obtained by measuring through using a Cu-K alpha ray is shown as a figure 1. The novel crystal form of the meclofenoxate hydrochloride provided by the invention is different from the structure of an existing crystal from in the prior art. Through experimental verification, a meclofenoxate hydrochloride crystal compound provided by the invention is greatly improved in hygroscopicity and fluidity in comparison with those in the prior art, the water content and the impurity content are extremely low, the stability is good, and convenience is brought for the preparation of a preparation.

Description

Technical field [0001] The present invention is a pharmaceutical technology field involving a pinetic acid hydrochloride composition that promotes brain energy metabolism. Background technique [0002] The chemical name of methyl microscin hydrochloride is 2- (dihydramamin) ethyl acel oxide acetate hydrochloride hydrochloride.Functions, including causing awakening, exciting spirit, excitement of breathing, increasing neurode reflexes and increasing freedom activity. It can promote protein assimilation. In the body, it can be used as a raw material for synthetic choline and acetyl.Quality content, increase the amount of acetylcholine in the brain, have anti -hypoxia effects, promote the oxidation reaction of brain cells, promote brain energy metabolism, improve learning, memory, and cognitive functions, improve cerebral blood flow, promote the recovery of clinical symptoms signsEssence [0003] At present, namifafen hydrochloride preparations listed in China are mostly used for tr...

Claims

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Application Information

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