Lurasidone hydrochloride tablets

Abstract

The invention belongs to the novel technical field of medicine preparation, and particularly relates to lurasidone hydrochloride tablets and a preparing method thereof. The lurasidone hydrochloride tablets are prepared with lurasidone hydrochloride as the main ingredient through direct compression of lurasidone hydrochloride solid dispersion particles and auxiliaries. The lurasidone hydrochloride solid dispersion particles are prepared in the way of heating potassium citrate and sorbitol in a hot melt extruder to be molten, then adding lurasidone hydrochloride for melting, and extruding melt liquid for pelleting, wherein the weight ratio of lurasidone hydrochloride to potassium citrate is 1 : (0.5-2), and the weight ratio of lurasidone hydrochloride to sorbitol is 1 : (1-5). By the adoption of the lurasidone hydrochloride tablets, the problem that the in vitro dissolution rate of lurasidone hydrochloride is low is solved, the curative effect is improved, and a more ideal curative effect is realized.

Description

technical field [0001] The invention belongs to the field of new technology for medicine manufacture, and in particular relates to a lurasidone hydrochloride tablet and a preparation method thereof. Background technique [0002] Lurasidone Hydrochloride (LurasidoneHydrochloride) is developed by Sumitomo Pharmaceutical Co., Ltd., and its trade name is LATUDA. On October 28, 2010, the U.S. Food and Drug Administration (FDA) approved its listing for the monotherapy of schizophrenia and type I bipolar disorder-related depressive episodes or adjuvant therapy in combination with lithium and sodium valproate. The chemical name of lurasidone hydrochloride is (3aR, 4S, 7R, 7aS)-2-{(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazine-1 -ylmethyl]cyclohexylmethyl}hexahydro-1H-4,7-methylisoindole-1,3-dione hydrochloride. The structural formula is as follows: [0003] [0004] Lurasidone hydrochloride is an atypical antipsychotic drug, the exact mechanism of its treatment of schizophr...

AI Technical Summary

Problems solved by technology

Lurasidone hydrochloride is a BCSII compound, and poor solubility is a key factor affecting the difference in clinical efficacy

The existing technology adopts various methods to solve the technical obstacle of poor solubility of lurasidone hydrochloride, but none of them can solve the dissolution rate of lurasidone hydrochloride during 0 days or long-term storage, and fail to solve the problem of lurasidone hydrochloride. During the validity period, more than 85% can be released within 15 minutes

[0006] CN103006661A discloses an oral preparation, which uses micronization technology to control the average particle size of the micronized particles of lurasidone hydrochloride and dispersing carrier at 0.1-12 μm, effectively increasing the lurasidone hydrochloride preparation in 0 days. Dissolution, but failed to address the trend toward decreased dissolution of lurasidone HCl over long-term storage

[0007] CN104248769A discloses a pharmaceutical composition of lurasidone, which uses cyclodextrin to clathrate lurasidone or its acid addition salt to increase the dissolution rate of lurasidone hydrochloride preparations on day 0, but The early dissolution was slow and failed to solve the trend of the dissolution rate of lurasidone hydrochloride falling during long-term storage. At the same time, the cyclodextrin inclusion yield was not high, which further increased the production cost

[0008] CN104971046A A lurasidone hydrochloride immediate-release granule, which uses micronization to control the average particle size of lurasidone hydrochloride to less than 5 μm, and increases the lurasidone hydrochloride preparation in a large amount by adding a large amount of surfactant poloxamer. 0 day dissolution rate, but failed to prevent the long-term storage of lurasidone hydrochloride dissolution rate decline trend, while adding a large amount of surfactant poloxamer increased gastrointestinal reactions when oral lurasidone hydrochloride tablets , a large dose of poloxamer can easily cause the reversal of the water-oil environment of the gastrointestinal mucosa, causing nausea and vomiting

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