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Riluzole orally disintegrating tablet and preparation method thereof

A technology of riluzole mouth and riluzole, which is applied in the field of riluzole orally disintegrating tablets and its preparation, can solve the problem that there is no mention of the dissolution rate of riluzole emulsion and the stability of riluzole tablets. Solve problems such as increased dissolution of riluzole

Active Publication Date: 2020-10-27
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Regarding how to improve the dissolution rate of riluzole, Chinese patents have mentioned, for example: Chinese patent CN1780620A discloses the use of riluzole in local medicine for the treatment and / or prevention of neurological or brain diseases and / or injuries, wherein Riluzole emulsion contains riluzole, glyceryl monostearate 60, cetyl alcohol, medium chain triglycerides, white petrolatum, macrogol-20-glyceryl monostearate, propylene glycol, purified water , but the dissolution test of riluzole emulsion is not mentioned in the patent, and the stability of the preparation is not resolved
[0006] Chinese patent CN101390854A discloses a pharmaceutical composition containing riluzole, which discloses the method of using internal and external disintegrants and improving the selection of fillers, so that the dissolution of riluzole increases, which plays a certain technical role effect, but no good solution has been proposed for the stability of riluzole tablets
[0007] Chinese patent CN105030708B discloses a riluzole tablet, which discloses that riluzole and polyethylene glycol are heated and melted, and added to the ethanol solution of the dispersing carrier, the dissolution effect is improved to a certain extent, but for riluzole tablets The stability of the agent did not come up with a good solution

Method used

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  • Riluzole orally disintegrating tablet and preparation method thereof
  • Riluzole orally disintegrating tablet and preparation method thereof
  • Riluzole orally disintegrating tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1) Prescription

[0035]

[0036] 2) Preparation method

[0037] 1) Weigh the riluzole, sodium bicarbonate, microcrystalline cellulose, mannitol and 50% of the prescription amount of crospovidone and mix evenly, and the mixture is set aside;

[0038] 2) adding the mixture in step 1) into an aqueous ethanol solution with a mass concentration of 10% to 50% to granulate, passing through a 60-mesh sieve after drying, and dry the granules for later use;

[0039] 3) Add 50% of the prescribed amount of crospovidone and the prescribed amount of aspartame to the dry granules in step 2), mix well, then add the prescribed amount of magnesium stearate, mix evenly, and press to obtain Rilu Azole orally disintegrating tablets.

Embodiment 2

[0041] 1) Prescription

[0042]

[0043] 2) Preparation method

[0044] 1) Weigh the prescription amount of riluzole, sodium bicarbonate, microcrystalline cellulose, sorbitol and 50% of the prescription amount of low-substituted hydroxypropyl cellulose, mix well and set aside;

[0045] 2) adding the mixture in step 1) into an aqueous ethanol solution with a mass concentration of 10% to 50% to granulate, passing through a 60-mesh sieve after drying, and dry the granules for later use;

[0046] 3) Add 50% prescription amount of low-substituted hydroxypropyl cellulose and the prescription amount of aspartame to the dry granules in step 2), mix uniformly, then add the prescription amount of calcium stearate, mix uniformly, and compress to obtain a benefit Luzole orally disintegrating tablets.

Embodiment 3

[0048] 1) Prescription

[0049]

[0050]

[0051] 2) Preparation method

[0052] 1) Weigh the crospovidone, riluzole, sodium bicarbonate, microcrystalline cellulose, mannitol and 50% prescription quantity of the prescription, mix well and set aside;

[0053] 2) adding the mixture in step 1) into an aqueous ethanol solution with a mass concentration of 10% to 50% to granulate, passing through a 60-mesh sieve after drying, and dry the granules for later use;

[0054] 3) Add 50% of the prescription amount of crospovidone and the prescription amount of acesulfame-K to the dry granules in step 2), mix evenly, then add the prescription amount of sodium stearyl fumarate, mix evenly, and press to obtain the benefit Luzole orally disintegrating tablets.

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Abstract

The invention relates to a riluzole orally disintegrating tablet and a preparation method thereof, and belongs to the field of preparations. The tablet is prepared from riluzole, sodium bicarbonate, afilling agent, a disintegrating agent, a lubricating agent and a flavoring agent. The preparation method comprises the following steps of (1) weighing riluzole, sodium bicarbonate and filler according to prescription amounts, and uniformly mixing the riluzole, the sodium bicarbonate and the filler with 50% of the disintegrating agent according to prescription amounts for later use; 2) adding themixture obtained in the step 1) into an ethanol water solution, granulating, drying, and sieving to obtain dry granules for later use; and 3) adding 50% of a prescription amount of the disintegratingagent and a prescription amount of the flavoring agent into the dry particles obtained in the step 2, uniformly mixing, adding a prescription amount of the lubricant, uniformly mixing, and pressing toobtain the riluzole orally disintegrating tablet. The orally disintegrating tablet prepared by the invention has the advantages of short disintegration time limit, high dissolution rate and no gravelfeeling, meets the quality standard requirement of the orally disintegrating tablet, and is suitable for industrial scale-up production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a riluzole orally disintegrating tablet and a preparation method thereof. Background technique [0002] Riluzole, whose chemical name is 2-amino-6-trifluoromethoxybenzothiazole, is easily soluble in methanol or ethanol and almost insoluble in water, and is used for the treatment of amyotrophic lateral sclerosis. [0003] Riluzole is a glutamate antagonist, which can inhibit the release of neurotransmitters in the brain, inhibit glutamatergic synaptic transmission, and inhibit the production of γ-aminobutyric acid (GABA), dopamine, and glutamic acid. Reuptake; It can also significantly inhibit the activity of excitatory amino acids; It can stabilize the inactivation state of voltage-dependent sodium channels and has neuroprotective effects. It is mainly used for the treatment of motor neuron diseases. [0004] Riluzole is a poorly soluble compound, and its d...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P35/04
CPCA61K31/216A61P35/04
Inventor 张贵民朱会敏杨玲
Owner LUNAN PHARMA GROUP CORPORATION
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