Pharmaceutical composition containing safinamide mesylate and preparation method of pharmaceutical composition

A technology of safinamide mesylate and its composition, which is applied in the field of pharmaceutical preparations and can solve the problems of producing neuroprotective effects and insufficient support

Inactive Publication Date: 2015-04-29
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

First, it is highly specific for MAO-B, so it can limit or eliminate dietary restrictions, which is still a big problem among other drugs in this class; second, safinamide has a dual mechanism of action, in addition to inhibiting In addition to MAO-B, it also has the additional function of inhibiting the release of glutamate. In theory, this may have a neuroprotective effect. Compared with the current situation where only symptomatic treatment is provided, safinamide can better meet the unmet needs in the market , current MAO-B inhibitors, especially Azilect, have also been proposed to be neuroprotective, but clinical data do not fully support this hypothesis

Method used

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  • Pharmaceutical composition containing safinamide mesylate and preparation method of pharmaceutical composition
  • Pharmaceutical composition containing safinamide mesylate and preparation method of pharmaceutical composition
  • Pharmaceutical composition containing safinamide mesylate and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weight ratio based on a tablet containing 50 mg of safinamide mesylate.

[0021]

[0022] Co-micronize the active ingredient safinamide methanesulfonate and part of lactose in the prescription, control the particle size of 90% or more particles in the range of 5-50 μm, pass all excipients through 100 mesh sieves, and mix the micronized product with The remaining lactose, microcrystalline cellulose, and cross-linked povidone are mixed evenly by the method of equal addition, and an appropriate amount of PVP K30 is added to make a soft material, which is extruded through a 18-mesh sieve to granulate, and the wet granules are dried at a constant temperature at 50°C After 2 hours, the dry granules were sieved with a 24-mesh sieve, added with additional magnesium stearate, mixed evenly, and compressed into tablets.

Embodiment 2

[0024] Weight ratio based on a tablet containing 50 mg of safinamide mesylate.

[0025]

[0026] Co-micronize the active ingredient safinamide methanesulfonate and part of mannitol in the prescription, and control the particle size of 90% of the volume or more particles in the range of 5-50 μm, so the excipients are passed through 100 mesh sieves, and the Mix the micronized product with the remaining mannitol, pregelatinized starch, and crospovidone evenly in equal amounts, add an appropriate amount of PVP K30, make a soft material, squeeze and sieve through a 18-mesh sieve to granulate, and place the wet granules at 50°C Dry at a constant temperature for 2 hours under certain conditions, sieve the dry granules through a 24-mesh sieve, add additional magnesium stearate, mix well, and compress into tablets.

Embodiment 3

[0028] Based on the weight ratio of the tablet containing 50 mg safinamide mesylate

[0029]

[0030] Co-micronize the active ingredient safinamide mesylate and part of mannitol in the prescription, control the particle size of 90% or more of the particles in the range of 10-20μm, and pass all the excipients through a 100-mesh sieve. Compound and the remaining mannitol, microcrystalline cellulose, and crospovidone were uniformly mixed in equal amounts, and an appropriate amount of hydroxypropylmethylcellulose was added to make a soft material, extruded through a 18-mesh sieve to granulate, and the wet granules were placed Dry at a constant temperature of 50°C for 2 hours, sieve the dry granules through a 24-mesh sieve, add additional magnesium stearate, mix well, and press into tablets.

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Abstract

The invention belongs to the technical field of medicines, and relates to a safinamide mesylate pharmaceutical composition having a good dissolution effect. The pharmaceutical composition contains safinamide mesylate, a water-soluble excipient, a disintegrant, a lubricant and the like, wherein the safinamide mesylate undergoes micronization treatment, and the grain size of 90% of the safinamide mesylate is controlled within 5-50microns, preferably within 10-20microns. The medicine prepared by the method disclosed by the invention is good in dissolution effect, so that the bioavailability of the medicine is effectively improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and describes a pharmaceutical preparation whose active ingredient is safinamide mesylate. Safinamide mesylate is used as an active ingredient in oral solid preparations for the treatment of Parkinson's disease (idiopathic Parkinson's disease, PD). The invention additionally relates to a process for the preparation of this formulation. Background technique [0002] On December 5, 2013, Newron, which is committed to developing drugs for central nervous system diseases, and its market partner Zambon announced the development progress of its lead candidate drug safinamide for the treatment of Parkinson's disease. After submitting a marketing authorization application to the European Medicines Agency, Zambon and Newron plan to submit a new drug application to the US Food and Drug Administration in the first quarter of 2014. [0003] Safinamide is a monoamine oxidase B (MAO-B) inhibitor. M...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/165A61P25/16
Inventor 付珊珊刁媛媛马苏峰
Owner AVENTIS PHARMA HAINAN
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