Hydrobromic acid vortioxetine oral soluble film agent and preparation method thereof

Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a hydrobromic acid vortioxetine oral soluble film agent and a preparation method thereof. The preparation method comprises the following steps: mixing the vortioxetine hydrobromide and auxiliary materials, and sequentially carrying out hot melting, film drawing and cooling to obtain the oral instant film agent. Compared with a solution casting method or other methods, the oral instant film agent prepared by adopting a hot melting method has the advantages that the tensile property of the oral instant film agent is improved, and meanwhile, the disintegration time limit is remarkably shortened. Known by technicians in the field, the improvement of the tensile property can prolong the disintegration time limit, but the invention has the opposite effect that the dissolving property of the mixture disclosed by the invention is possibly changed due to a hot melting method.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a vortioxetine hydrobromide oral solution and a preparation method thereof. Background technique [0002] Vortioxetine Hydrobromide, 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 effect by increasing the concentration of serotonin in the central nervous system. It was jointly developed by Denmark's Lundbeck and Japan's Takeda. It was approved by the U.S. Food and Drug Administration (FDA) on March 30 for the treatment of major depressive disorder (MDD). The trade name is Brintellix, and the dosage form is tablet. The specifications are 5mg, 10mg, 15mg and 20mg. In the same year In December, it was approved by the European Medicines Agency (EMA). The dosage forms are ora...

AI Technical Summary

Problems solved by technology

[0006] 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.

[0010] The oral instant film itself also has certain 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 (in the film-forming mixed solution When heating or solvent evaporates), shedding (during the cutting process), cracking (during the cutting process) and other phenomena are also not conducive to the realization of industrialization

In clinical application, due to the limited drug loading, the choice of drugs is limited, and children are sensitive to taste and are more picky about taste. Therefore, how to improve the taste-masking technology to prepare products that children love is also a big challenge for oral instant film. challenge

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