Riluzole orally disintegrating tablet and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a riluzole orally disintegrating tablet and a preparation method thereof. The riluzole orally disintegrating tablet is prepared from 5 parts of 2-amino-6-trifluoromethoxy benzothiazole, 70 to 120 parts of a filling agent, 60 to 100 parts of a disintegrating agent, 2 to 25 parts of a stabilizing agent and 40 to 60 parts of a flavoring agent. The disintegrating time limit is shortened and the toughness of the orally disintegrating tablet is improved by preferably selecting the disintegrating agent, the stabilizing agent and other auxiliary materials and optimizing the preparation process, so that the tablet is not easy to break and convenient to transport, the content of related substances is reduced, and the stability of the medicine is improved.

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, chemical name 2-amino-6-trifluoromethoxybenzothiazole, is a benzothiazole derivative that blocks glutamatergic neurotransmission in the central nervous system. In 1995, the US FDA approved riluzole as the first drug for the treatment of ALS. Although riluzole is mostly safe and well tolerated in clinical practice, it has limited efficacy in ALS, prolonging tracheostomy-free survival by only 2–3 months. However, some researchers have successively shown through clinical trials that riluzole treatment can make the median survival time of patients reach 6 months to 19 months, which is much longer than the above-mentioned 2-3 months, so riluzole The treatment benefit for ALS is still very considerable. [0003] Most patients with amyotrophic latera...

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Problems solved by technology

[0003] Most patients with amyotrophic lateral sclerosis have symptoms such as muscle atrophy, dysphagia, and difficulty speaking. Ordinary tablets or capsules have poor compliance with taking drugs. Orally disintegrating tablets are suitable for patients with dysphagia who cannot actively Or patients who do not cooperate with medication

[0004] However, the riluzole drug itself has some limitations, such as extremely low solubility in water, poor oral palatability, stability dependent on pH, direct administration will stimulate the oral mucosa to produce numbness and other shortcomings, so riluzole should be made into oral Collapsing needs to solve the above problems

[0005] Chinese patent CN101390854A discloses a pharmaceutical composition containing riluzole, including active ingredient riluzole and water-soluble fillers and water-insoluble fillers, binders, disintegrants, lubricants, flavoring agents, which The dissolution rate of riluzole was increased mainly by improving fillers and preferred disintegrants, but did not solve the problems of stability and stimulation of oral mucosa

However, this patent does not control the stability of the orally disintegrating tablet, and cannot guarantee the safety of medication.

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