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A composition containing flupirtine or a pharmaceutically acceptable salt thereof and a preparation method thereof

The technology of a composition and flupirtine is applied in the field of compositions containing flupirtine or its pharmaceutically acceptable salts and its preparation, which can solve the problems of poor fluidity of raw materials, and avoid uneven coating or particle surface adhesion, Sustained-release preparations are safe and the effect of simplifying the preparation process

Active Publication Date: 2022-05-20
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the deficiencies of the prior art, the present invention discloses a flupirtine sustained-release preparation with strong stability, sustainable release and simple process. For granulation, the inventors added a specific proportion of micropowder silica gel to the formula, which effectively improved the problem of poor fluidity of the bulk drug, and the bulk drug can be directly compressed with sustained-release granules to prepare flupirin with sustained-release effect. Sustained-release preparations

Method used

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  • A composition containing flupirtine or a pharmaceutically acceptable salt thereof and a preparation method thereof
  • A composition containing flupirtine or a pharmaceutically acceptable salt thereof and a preparation method thereof
  • A composition containing flupirtine or a pharmaceutically acceptable salt thereof and a preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of a composition containing flupirtine or a pharmaceutically acceptable salt thereof

[0029] Composition 1

[0030] 1. Preparation of sustained-release part: sieve flupirtine maleate, Eudragit RL100, pregelatinized starch, yellow iron oxide and talcum powder in Table 1, and mix the above-mentioned components in the prescription amount in Table 1 Uniform, use 5% hydroxypropyl cellulose aqueous solution as binder to prepare soft material, granulate with 30 mesh sieve, dry the granules prepared by wet method at 60°C until the moisture content is lower than 3.0%;

[0031]2. Mix the flupirtine maleate of the prescription amount in Table 2 and the flupirtine maleate sustained-release granules prepared above, and then add the croscarmellose sodium and stearin of the prescription amount in Table 2 Magnesium acid and micropowder silica gel are mixed evenly;

[0032] 3. Determining the content of the blended granule intermediate, submitting the pressure, ...

Embodiment 2

[0056] The selection test of embodiment 2 disintegrating agent

[0057] Sustained-release granules composition:

[0058]

[0059] Preparation method of sustained-release granules: sieve flupirtine maleate, methyl cellulose and yellow iron oxide, mix the above-mentioned ingredients evenly, use Eudragit NE30D as a binder to prepare a soft material, 30 Granulate with a mesh sieve, and dry the granules prepared by the wet method at 60°C until the moisture content is less than 3.0%.

[0060] Composition 5

[0061] Mix the flupirtine maleate and flupirtine maleate sustained-release granules in the prescription amount in Table 5 evenly, then add the CMS-Na, pregelatinized starch, magnesium stearate and micropowder silica gel in the prescription amount in Table 5 Mix evenly; measure the content of the blended granule intermediate, submit the pressure, compress the tablet, and obtain the sample.

[0062] Composition 6

[0063] The difference from composition 5 is that each compo...

Embodiment 3

[0081] This embodiment examines the influence of magnesium stearate and micropowder silica gel on the pharmaceutical composition described in this application, and the formulation and preparation of sustained-release granules are as follows:

[0082]

[0083] Sustained-release granule preparation method: Sustained-release granule preparation method: sieve flupirtine maleate, methylcellulose and yellow iron oxide, mix each component of the above prescription amount evenly, use Eudragit NE30D as a binder Prepare soft materials with 30-mesh sieve, and dry the wet-processed granules at 60°C until the water content is lower than 3.0%.

[0084] The specific implementation is as shown in Table 8:

[0085] Composition 10

[0086] Mix the flupirtine maleate and the flupirtine maleate sustained-release granules of the prescription amount in Table 8 evenly, then add the croscarmellose sodium, pregelatinized starch, and stearin of the prescription amount in Table 8 Magnesium acid and...

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Abstract

A composition containing flupirtine or a pharmaceutically acceptable salt thereof and a preparation method thereof. The invention discloses a flupirtine slow-release preparation with strong stability, sustainable release and simple process. Adopting the combination of immediate-release and sustained-release design, the sustained-release preparation contains immediate-release part, sustained-release part, disintegrant, magnesium stearate and micropowder silica gel, and the immediate-release part does not need to be granulated, and the raw material drug can be Tablets are directly compressed with sustained-release granules, and the sustained-release part is prepared by wet granulation, adding special sustained-release framework materials, and directly mixed with other pharmaceutical excipients to avoid drug release caused by uneven coating in dry granulation Problems, the sustained release of the drug is ensured, while the process is simplified and the production cost is reduced.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy and relates to a composition containing flupirtine or a medicinal salt thereof and a preparation method thereof. Background technique [0002] Flupirtine maleate is a centrally active non-opioid analgesic, which was synthesized in Germany in the 1980s and developed and produced by AWD Company. The mechanism of action of this drug is different from that of opioids and non-steroidal drugs, so there will be no adverse reactions caused by opioids and non-steroidal drugs. Clinically, flupirtine maleate is mainly used to treat acute and chronic pain, such as pain caused by increased muscle tone of static and moving muscles, tension pain, pain caused by tumors, dysmenorrhea and post-traumatic pain. Its mechanism of action is a selective neurogenic potassium channel opener with triple effects of analgesia, muscle relaxation and neuroprotection. Animal experiments have shown that flupirtine maleate has a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/44A61K47/38A61K47/36A61K47/32A61P25/04
Inventor 王辉吴越孙倩邓丽君徐佳佳
Owner BEIJING TIDE PHARMA
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