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A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby

A technique for acetaminophen and its composition, applied in the field of preparing a pharmaceutical composition comprising Nefopam and acetaminophen and the pharmaceutical composition obtained therefrom, capable of solving problems affecting the efficacy and safety of the pharmaceutical composition

Active Publication Date: 2021-09-07
APTYS PHARMACEUTICALS SAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, one of the problems with pharmaceutical compositions is that impurities may appear in said composition, for example due to the choice of synthetic route, quality of starting materials, reaction conditions, final purification steps, design of process equipment, etc.
The presence of these unwanted chemicals, even in trace amounts, may affect the efficacy and safety of the pharmaceutical composition

Method used

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  • A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby
  • A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby
  • A method of manufacturing a pharmaceutical composition comprising nefopam and acetaminophen, and the pharmaceutical composition obtained thereby

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0065] Effect of Process Steps on the Stability of Nefopam

[0066] In order to assess whether the stability of Nefopam is affected by the process step of adding it to the pharmaceutical composition, the following experiments were carried out.

[0067] The method according to the invention involves the preparation of two phases: a granulated powder containing the majority of the components (first process step) and an external phase containing one or more lubricants (second process step).

[0068] Nefopam is added in the granulated powder (first process step) or in the external phase (second process step).

[0069] Two batches using the external phase process and two batches using the internal process were prepared as described below.

[0070] In the context of the present invention, the term % refers to percentage by weight of the composition.

Embodiment I

[0072] Batch F192H043 - Nefopam added in first process step

[0073] Step a): First process step

[0074] In a first process step, a granulated powder was prepared by adding the following components to a planetary mixer: acetaminophen, microcrystalline cellulose (diluent), starch and povidone K90 (binder), cross-linked Sodium carboxymethylcellulose (disintegrant) and anhydrous citric acid (pH adjuster).

[0075] The components were added to the planetary mixer in the following order: first half of acetaminophen, microcrystalline cellulose, starch, PVP K90, Nefopam HCL, croscarmellose sodium, anhydrous citric acid , and finally the second half of acetaminophen.

[0076] 800 g of the powder were mixed for 10 min at 105 rpm.

[0077] The final composition of the initial mixture was as follows:

[0078]

[0079] Pure water (235g) was added to the planetary mixer containing the initial mixture, stirred at a constant speed of 80rpm to 115rpm for 20min, and then stirred at 11...

Embodiment II

[0110] Batch F193H044 - Nefopam added in first process step

[0111] first process step

[0112] A granulated powder was prepared as described in Example I for batch F192H043.

[0113] The final composition of the powder is as follows:

[0114]

[0115] The remaining steps such as drying and quantification were the same as disclosed for batch F192H043.

[0116] second process step

[0117] The second process step was carried out as described in Example 1, the composition of the external phase being:

[0118] Microcrystalline Cellulose 2.02%

[0119] The resulting pharmaceutical composition (357 g) was then tableted.

[0120] Batch F195H046 - Nefopam added in second process step

[0121] first process step

[0122] A granulated powder was prepared as described in Example I.

[0123] The final composition of the powder is as follows:

[0124]

[0125] The remaining steps such as drying and quantification were the same as disclosed for batch F194H045.

[0126] s...

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Abstract

The present invention relates to a method of preparing a pharmaceutical composition comprising acetaminophen and nefopam, said method comprises - in a first process step providing a wet granulated powder by mixing acetaminophen with one or more excipients; - in a second process step adding nefopam and a lubricant to the granulated powder, and - in a third process step, forming the pharmaceutical composition. Since the nefopam is added to the mixture in the second process step the impurities originating from nefopam is reduced to such an extend that said impurities cannot be detected in the final pharmaceutical composition using a conventional HPLC method.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising two active ingredients of nefopam and acetaminophen, a method for manufacturing the pharmaceutical composition and uses of the composition. Background technique [0002] The literature suggests that the management of pain such as postoperative pain remains a challenge for several reasons, including delayed recovery for patients and the risk of developing persistent postoperative pain. [0003] Opioids, nonsteroidal anti-inflammatory drugs (NSAIDs), and acetaminophen are widely used to treat moderate to severe pain, and they are the most commonly used analgesics used today to manage chronic, inflammatory, and postoperative pain. [0004] These agents all produce analgesic effects, but they have many adverse side effects that limit their clinical utility. Side effects of opioids include nausea, vomiting, constipation, respiratory depression, urinary retention, sedation, tolerance, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/167A61K31/395
CPCA61K9/2013A61K9/2077A61K9/4858A61K31/167A61K31/395A61K31/5545A61K9/2027A61K9/2054A61K9/2059
Inventor 弗朗索瓦·布蒂尼翁瓦赫纳·伯纳德克劳迪·马森-辛特夫
Owner APTYS PHARMACEUTICALS SAS
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