Application of malic acid, vortioxetine hydrobromide oral instant film agent and preparation method of vortioxetine hydrobromide oral instant film agent

Abstract

The invention relates to the technical field of medicaments, in particular to application of malic acid, a hydrobromic acid vortioxetine oral instant film agent and a preparation method. The invention relates to a hydrobromic acid vortioxetine oral instant film agent, which comprises the following components by weight: 1-30% of hydrobromic acid vortioxetine, 30-80% of a film forming material, 0-20% of a plasticizer, 0-30% of a filler, 0-20% of a disintegrating agent, 0-10% of a flavoring agent, 0-5% of an antioxidant, and 0-8% of other auxiliary materials. The other auxiliary materials comprise one or a combination of more than two of citric acid, malic acid, lactic acid, ascorbic acid and tartaric acid; the film-forming material comprises polyvinyl alcohol (PVA) and povidone (PVP), wherein the mass ratio of the polyvinyl alcohol to the povidone is (1: 6)-(6: 1). The oral cavity instant film agent obtained by the invention can be quickly dissolved or disintegrated in the oral cavity, releases medicines, is quickly absorbed in the gastrointestinal tract to take effect after being swallowed, and is used for treating adult depression.

Description

technical field [0001] The invention relates to the technical field of medicaments, in particular to an application of malic acid, vortioxetine hydrobromide oral instant film and a preparation method. Background technique [0002] Vortioxetine Hydrobromide, the chemical name is 1-[2-(2,4-dimethylphenylthio)-phenyl]-piperazine, hydrobromide, its chemical structure is as follows figure 1 shown. [0003] Vortioxetine hydrobromide is a new drug for the treatment of depression. It mainly exerts antidepressant effects by increasing the concentration of serotonin in the central nervous system. It was jointly developed by Lundbeck and Takeda in September 2013. On March 30, it was approved by the US Food and Drug Administration (FDA) for the treatment of major depressive disorder (MDD). Approved by the European Medicines Agency (EMA) in December, the dosage forms are oral film-coated tablets and drops. Because it is a new drug with clinical value, it has received priority review in...

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Problems solved by technology

[0005] According to the relevant review reports of vortioxetine tablets or oral solutions that have been marketed, vortioxetine is well absorbed orally, but the absorption is slow, and the peak time after oral administration is 7 to 11 hours, and the absolute bioavailability is 75%, and the elimination half-life is 66 hours, indicating that the drug has a long elimination cycle and long-lasting effect, but the problem is that the absorption is slow, and even the oral solution also shows a peak time close to that of the tablet; meanwhile, vortiazem Tablets or oral solutions will also affect the compliance of medication to a certain extent in view of the fact that depression patients are increasingly younger and the number and proportion of adolescents are increasing.

[0008] The oral instant film itself has limitations: for example, the prepared film must have a uniform thickness to ensure uniform content, so higher requirements are placed on the equipment; in addition, the product foams during the preparation process (heating or When the solvent evaporates), shedding (during the cutting process), cracking (during the cutting process) and other phenomena are also not conducive to the realization of industrialization

Because vortioxetine and its pharmaceutically acceptable salts dissolve very little, in order to effectively solubilize, will have to use a large amount of cyclodextrin, in the embodiment of patent CN113476427A, the consumption of cyclodextrin is up to 23.45% (w / w ), long-term use will increase the risk of nephrotoxicity

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