Aripiprazole solid preparation and preparation method thereof

Abstract

The invention discloses the preparation method of aripiprazole solid preparation. The method comprises the following steps of dissolving aripiprazole into acidic solution containing an acidifying agent to obtain medicine-containing acidic solution; and then uniformly mixing accessory with the medicine-containing acidic solution to granulate by a wet method. The invention also discloses aripiprazole solid preparation prepared by the method. According to the method disclosed by the invention, the defects of the serious pollution, high loss and serous potential safety hazards brought by mechanical crushing treatment are avoided; and the method is simple, convenient and feasible for operation and easy for industrial production and has high safety coefficient. The aripiprazole solid preparation prepared by the method has the advantages of excellent dissolution property, stability, and content uniformity.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid preparation of aripiprazole and a preparation method thereof. Background technique [0002] Aripiprazole, chemical name 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1 hydrogen)- Quinolinone, molecular weight 448.39, belongs to quinolinone derivatives. It was developed by Otsuka Corporation of Japan and was first approved by the US FDA in November 2002. Aripiprazole is an atypical antipsychotic that exhibits presynaptic dopamine agonism and postsynaptic dopamine D 2 Antagonist action, with 5-HT 1a Partial receptor agonism and 5-HT 2 Receptor antagonism. Clinical trial studies have shown that aripiprazole can significantly improve the positive and negative symptoms of schizophrenia, and reduce the relapse rate of schizophrenia, while the effects of extrapyramidal side effects and weight gain are small, and it is also It does not cause an ...

AI Technical Summary

Problems solved by technology

[0009] The technical problem to be solved by the present invention is to overcome the existing aripiprazole solid preparation method to select and control the particle size of aripiprazole through mechanical pulverization, which will cause environmental pollution, large loss, and serious safety hazards. Moreover, the dissolution characteristics of aripiprazole solid pharmaceutical preparations are still not ideal, and a method is provided that is easier to operate, less polluted, does not have the aforementioned safety hazards, and can ensure that the obtained solid preparations have excellent dissolution characteristics, stability and content. Preparation method of uniformity, and aripiprazole solid preparation prepared by the method

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