Riluzole tablets and preparation method thereof

Abstract

The invention provides riluzole tablets and a preparation method thereof. The riluzole tablets comprise riluzole, polyethylene glycol, an N-vinyl pyrrolidone / vinyl acetate linear copolymer, a filling agent, a disintegrating agent and a lubricating agent. According to the invention, riluzole and polyethylene glycol are melted firstly, then the melted riluzole and polyethylene glycol are added into an ethanol solution of the N-vinyl pyrrolidone / vinyl acetate linear copolymer, and finally the corresponding filling agent, the disintegrating agent and the lubricating agent are added for tabletting, so that the riluzole tablets are obtained. The dissolution effect of the prepared riluzole tablets is improved obviously and can reach 80% or above with 10 min, the long-term storage stability is good, the preparation process is simple, complex equipment is not required and industrial mass production is facilitated.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a riluzole tablet and a preparation process thereof. Background technique [0002] Riluzole is a glutamate antagonist that can inhibit the release of neurotransmitters in the brain, inhibit glutamatergic synaptic transmission, and inhibit the release of gamma-aminobutyric acid (GABA), dopamine, and glutamate. 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 obvious neuroprotective effects. It is mainly used for the treatment of motor neuron diseases. Riluzole is a difficult-to- The dissolution of soluble compounds is the rate-limiting step for drug absorption and utilization in the body. Commonly used methods to improve dissolution include: improving the selection of binders and disintegrants in prescriptions, improving the mixing ...

AI Technical Summary

Problems solved by technology

[0003] Chinese patent CN1780620 discloses the use of riluzole in local medicine for the treatment and / or prevention of neurological or brain diseases and / or injuries, wherein the emulsion of riluzole contains riluzole, glyceryl monostearate 60, ten Hexaol, medium-chain triglycerides, white petrolatum, polyethylene glycol-20-glyceryl monostearate, propylene glycol, purified water, but there is no mention in the patent of the dissolution rate determination of riluzole emulsion, the preparation Stability is not resolved

[0004] 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 method has been proposed for the stability of riluzole tablets

[0005] At present, the existing domestic technology does not provide a riluzole tablet with good stability, high dissolution rate and simple preparation process

Images