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Flupirtine maleate sustained release tablet

A technology of flupirtine acid sustained-release tablet and flupirtine maleate, which can be used in medical preparations with non-active ingredients, nervous system diseases, active ingredients of heterocyclic compounds, etc., and can solve side effects and fluctuations in blood drug concentration. Larger, short half-life of flupirtine maleate, etc., to achieve the effect of alleviating pain

Active Publication Date: 2012-11-07
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the short half-life of flupirtine maleate, common oral preparations need to be administered frequently (3-4 times a day, 100 mg each time), the blood concentration fluctuates greatly, and it is easy to produce obvious side effects

Method used

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  • Flupirtine maleate sustained release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: A flupirtine maleate sustained-release tablet, consisting of the following components (the coating weight of the sustained-release granules increases by 1%):

[0029] Flupirtine maleate immediate-release granules: (based on the amount of flupirtine maleate) 100g

[0030] Flupirtine maleate sustained-release granules: (based on the amount of flupirtine maleate) 300g

[0031] Sodium carboxymethyl starch 30g

[0032] Micronized silica gel 25g

[0033] Magnesium Stearate 5g

[0034] Microcrystalline Cellulose 20g

[0035] Among them, flupirtine maleate immediate-release granules consist of the following components:

[0036] Flupirtine Maleate 100g

[0037] Hypromellose (E50) 1g

[0038] Flupirtine maleate sustained-release granules are composed of the following components:

[0039] Flupirtine Maleate 300g

[0040] Hypromellose (E50) 9g

[0041] Microcrystalline Cellulose 30g

[0042] Eudragit NE30D 15ml

[0043] Calcium hydrogen phosphate 0.6g

[0044...

Embodiment 2

[0053] Example 2: A flupirtine maleate sustained-release tablet, consisting of the following components (the coating weight of sustained-release granules increased by 2%):

[0054] Flupirtine maleate immediate-release granules: (based on the amount of flupirtine maleate) 100g

[0055] Flupirtine maleate sustained-release granules: (according to the amount of flupirtine maleate) 300g

[0056] Sodium carboxymethyl starch 30g

[0057] Micronized silica gel 25g

[0058] Magnesium Stearate 5g

[0059]Microcrystalline Cellulose 20g

[0060] Among them, flupirtine maleate immediate-release granules consist of the following components:

[0061] Flupirtine Maleate 100g

[0062] Hypromellose (E50) 1g

[0063] Flupirtine maleate sustained-release granules are composed of the following components:

[0064] Flupirtine Maleate 300g

[0065] Hypromellose (E50) 9g

[0066] Microcrystalline Cellulose 30g

[0067] Eudragit NE30D 30ml

[0068] Calcium hydrogen phosphate 1.2g

[0069]...

Embodiment 3

[0071] Example 3: A flupirtine maleate sustained-release tablet, consisting of the following components (the coating weight of the sustained-release granules increases by 3%):

[0072] Flupirtine maleate immediate-release granules: (based on the amount of flupirtine maleate) 100g

[0073] Flupirtine maleate sustained-release granules: (according to the amount of flupirtine maleate) 300g

[0074] Sodium carboxymethyl starch 30g

[0075] Micronized silica gel 25g

[0076] Magnesium Stearate 5g

[0077] Microcrystalline Cellulose 20g

[0078] Among them, flupirtine maleate immediate-release granules consist of the following components:

[0079] Flupirtine Maleate 100g

[0080] Hypromellose (E50) 1g

[0081] Flupirtine maleate sustained-release granules are composed of the following components:

[0082] Flupirtine Maleate 300g

[0083] Hypromellose (E50) 9g

[0084] Microcrystalline Cellulose 30g

[0085] Eudragit NE30D 45ml

[0086] Calcium hydrogen phosphate 1.8g

[...

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PUM

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Abstract

The invention discloses a flupirtine maleate sustained release tablet which is composed of the following ingredients of: by weight, 90-110 parts of flupirtine maleate intermediate-release particles, 290-310 parts of flupirtine maleate sustained release particles, 25-35 parts of sodium carboxymethyl starch, 20-30 parts of aerosol, 3-8 parts of magnesium stearate and 15-25 parts of microcrystallinecellulose. Weight proportions of the flupirtine maleate intermediate-release particles and the flupirtine maleate sustained release particles are both weighed according to the weight of flupirtine maleate.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy and relates to a flupirtine maleate slow-release tablet. Background technique [0002] Flupirtine maleate (Chemical name: 2-amino-6-[(4-fluorobenzyl)amino]-3-pyridine carbamate ethyl ester maleate) opens selective neuronal potassium channels It is a non-opioid analgesic that acts on the central nervous system and does not produce dependence and tolerance. Flupirtine maleate activates G protein-coupled K on nerve cell membranes + Channel, K + Outflow stabilizes the resting membrane potential and reduces cell membrane activity, thereby indirectly inhibiting the activation of NMDA receptors. Flupirtine maleate at therapeutic concentrations does not bind to α1, α2, 5HT1, 5HT2, dopamine, benzodiazepines, opiates, central M and N receptors. Flupirtine maleate has three main effects on the central nervous system: analgesic effect, muscle relaxant effect, and the effect of preventing the per...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61K9/26A61K47/38A61P25/04
Inventor 朱义龚涛王一茜廖彬
Owner SICHUAN BAILI PHARM CO LTD
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