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Composition containing flupirtine or pharmaceutical salt thereof and preparation method thereof

A composition and flupirtine technology are applied in the field of compositions containing flupirtine or a medicinal salt thereof and in the field of preparation thereof, which can solve problems such as poor fluidity of raw materials, avoid uneven coating or particle surface adhesion, Simplify the preparation process and improve the effect of poor flowability

Active Publication Date: 2019-05-28
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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  • Composition containing flupirtine or pharmaceutical salt thereof and preparation method thereof
  • Composition containing flupirtine or pharmaceutical salt thereof and preparation method thereof
  • Composition containing flupirtine or pharmaceutical salt thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 For the preparation of a composition containing flupirtine or its pharmaceutically acceptable salt

[0029] Composition 1

[0030] 1. Preparation of the sustained-release part: sieve the flupirtine maleate, Eudragit RL100, pregelatinized starch, yellow iron oxide and talc in Table 1, and mix the above 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, and dry the granules prepared by wet method at 60°C until the moisture is less than 3.0%;

[0031] 2. Mix the flupirtine maleate in the prescription amount in Table 2 and the flupirtine maleate sustained-release granules prepared above, and then add the croscarmellose sodium and stearin in the prescription amount in Table 2 Mix the magnesium acid and micro-powder silica gel evenly;

[0032] 3. Determine the content of the total mixed granule intermediate, submit the pressure, press the tablet, and ob...

Embodiment 2

[0056] Example 2 Selection test of disintegrant

[0057] Composition of sustained-release granules:

[0058]

[0059] Preparation method of sustained-release granules: Sieve flupirtine maleate, methyl cellulose and yellow iron oxide, mix the components of the above prescription evenly, and use Eudragit NE30D as a binder to prepare soft materials, 30 Mesh granulation, the wet granules are dried at 60°C until the moisture content is less than 3.0%.

[0060] Composition 5

[0061] Mix the prescription amount of flupirtine maleate and flupirtine maleate sustained-release granules in Table 5, and then add the prescription amount of CMS-Na, pregelatinized starch, magnesium stearate and micronized silica gel in Table 5 Mix uniformly; determine the content of the total mixed particle intermediate, submit the pressure, press the tablet, and obtain the sample.

[0062] Composition 6

[0063] The difference from composition 5 is that each component is added according to Table 5, wherein the disin...

Embodiment 3

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

[0082]

[0083] Preparation method of sustained-release granules: Preparation method of sustained-release granules: sieving flupirtine maleate, methyl cellulose and yellow iron oxide, mixing the components of the above-mentioned prescription evenly, and using Eudragit NE30D as the binding agent Preparation of soft material, 30 mesh sieve granulation, the granules prepared by wet method are dried at 60 ℃ until the moisture is less than 3.0%.

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

[0085] Composition 10

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

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Abstract

The invention discloses a composition containing flupirtine or a pharmaceutical salt thereof and a preparation method thereof. The invention discloses a flupirtine slow-release preparation which is strong in stability, sustainable in release, and simple in process. A design of combining quick-release and slow-release is used. The slow-release preparation contains a quick-release part, a slow-release part, a disintegrant, magnesium stearate and colloidal silicon dioxide, wherein the quick-release part does not need to be pelletized. A crude drug can be directly subjected to tabletting with slow-release particles. While the slow-release part is prepared, a wet method is used for granulating, a special slow-release skeleton material is added, and directly mixed with other pharmaceutical auxiliaries. A drug release problem caused by uneven coating in a dry granulating process is avoided, sustained release of a drug is guaranteed, the process is simplified, and production cost is reduced atthe same time.

Description

Technical field [0001] The invention belongs to the field of chemical pharmacy, and relates to a composition containing flupirtine or its medicinal salt and a preparation method thereof. Background technique [0002] Flupirtine maleate is a central non-opioid analgesic. It was synthesized in Germany in the 1980s and developed and produced by AWD. The drug's mechanism of action is different from opioids and non-steroids, so adverse reactions caused by opioids and non-steroids will not occur. Clinically, flupirtine maleate is mainly used to treat acute and chronic pain, such as pain caused by increased muscle tension of resting and motor muscles, tension pain, pain caused by tumors, dysmenorrhea and post-traumatic pain. Its mechanism of action is a selective neurogenic potassium channel opener, which has the triple effects of pain relief, muscle relaxation and neuroprotection. Animal experiments show that flupirtine maleate has analgesic effects in various pain model experiments ...

Claims

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Application Information

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Patent Type & Authority Applications(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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