Vortioxetine-hydrobromide-containing coated granules, solid dispersion and preparation for masking oral breath

Abstract

The application discloses coated granules, solid dispersion, composition and preparation for masking oral breath. The breath masking effect of vortioxetine hydrobromide is improved, and the dependenceand compliance of a sufferer are improved.

Description

technical field [0001] The application relates to the technical field of pharmaceutical preparations, in particular to coating particles, solid dispersions, compositions and preparations for oral taste masking. Background technique [0002] Vortioxetine (also known as vortioxetine) is a multi-target antidepressant with 5-HT 3 Receptor Antagonism and 5-HT 1A Receptor agonism for the treatment of major depression. At present, the hydrobromide of vortioxetine is used clinically as its active ingredient. It was jointly developed by Takeda Pharmaceutical Company (Takeda) and Lundbeck Company (Lundbeck). It was approved for marketing by FDA on September 30, 2013. The trade name is Brintellix has four approved specifications, namely 5mg, 10mg, 15mg and 20mg, and the dosage form is film-coated tablet. [0003] The chemical name of vortioxetine hydrobromide is: 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine hydrobromide, the English name is Vortioxetine hydrobromide, and the m...

AI Technical Summary

Problems solved by technology

In order to reduce the irritation of the drug in the oral cavity, it is necessary to reduce the exposure of the drug in the oral cavity and the dissolution rate of the drug; however, while reducing the dissolution rate of the drug, it will also slow down the absorption of the drug, thereby affecting the absorption and absorption of the immediate-release dosage form. Metabolism speed, affecting drug efficacy and safety

This technical contradiction is also the main technical obstacle to the marketing of this product without an oral taste-masking immediate-release dosage form.

Especially when the patient's condition improves and he is willing to cooperate with the medication to switch to the ordinary immediate-release coated tablet, the two dosage forms are different in dissolution and absorption metabolism, resulting in potential physiological and pathological problems after the patient changes the drug.

[0009] The use of flavoring agents is also a method to adjust the bad taste of raw materials such as bitterness, but the effect of flavoring agents on improving the irritation of vortioxetine is very poor

[0010] Vortioxetine Lactate Oral Solution, which has been approved for marketing, has not been approved by the market for many years due to strong irritation

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