Orally disintegrating tablet containing Brexpiprazole or salt and preparation method thereof

Abstract

The invention relates to an orally disintegrating tablet containing Brexpiprazole or salt and also relates to a preparation method thereof. The orally disintegrating tablet contains 0.06-15.0% of Brexpiprazole, 40.0-95.0% of an excipient, 3.0-50.0% of a disintegrating agent, 0.0-6.0% of a lubricant and 0.05-5.0% of a corrective agent. The orally disintegrating tablet is prepared by the following steps: firstly preparing a solid dispersion from the active component Brexpiprazole; and then mixing the active component Brexpiprazole with other auxiliary materials. The orally disintegrating tablet has the following advantages: disintegration is fast; mouthfeel is good; bioavailability is high; quality is stable and controllable; auxiliary materials are safe and easily available; the preparation method is simple; no expensive special equipment is required; and the product is easy to store and transport.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to an orally disintegrating tablet of ebiprazole or a salt thereof, and also relates to a preparation method of the orally disintegrating tablet. Background technique [0002] Ebiprazole (English name: Brexpiprazole), its chemical name is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinoline -2-ketone is a new drug with anti-schizophrenia and anti-depressant effects developed by Lundbeck Pharmaceuticals of Denmark and Otsuka Pharmaceuticals of Japan for multiple targets of monoamine neurotransmitters. It is a serotonin-dopamine activity regulator , except mainly possess dopamine D 2 In addition to partial receptor agonism, it also has D 3 Partial receptor agonism, 5-HT 1 Part A receptor agonism and 5-HT 2 Part A receptor antagonism. [0003] in dopamine D 2 In receptor-like, D 2 Partial receptor agonists can produce functional antagonism on the mesolimbic pathway, whic...

AI Technical Summary

Problems solved by technology

[0005] Japanese Otsuka Pharmaceutical Co., Ltd. patent WO2013054872, and its Chinese counterpart CN103889425 discloses containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinoline- Tablets of 2-ketone or its salts, although there is the name of orally disintegrating tablets, but no specific solution is proposed for the orally disintegrating tablets, and the tablets are wet granulated

The Chinese patent CN105078910A discloses a freeze-dried oral preparation containing ebiprazole and its preparation method. The invention adopts a freeze-drying method to prepare orally disintegrating tablets, although the preparation of orally disintegrating tablets by this method has the advantage of rapid disintegration. However, special equipment is required for production, the product cost is high, and it is not suitable for people with various consumption capabilities, and the freeze-dried orally disintegrating tablets are easy to break and require special packaging, which increases the difficulty of packaging and transportation.

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