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Aripiprazole preparation and preparation method thereof

A technology for aripiprazole and preparations, applied in the field of aripiprazole preparations and its preparation, capable of solving problems such as unsatisfactory stability of aripiprazole preparations

Active Publication Date: 2013-01-02
SHANGHAI ZHONGXI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide an aripiprazole preparation with excellent dissolution characteristics, stability and lower content of related substances in order to overcome the unsatisfactory defects of the existing aripiprazole preparations. and its preparation method

Method used

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  • Aripiprazole preparation and preparation method thereof
  • Aripiprazole preparation and preparation method thereof

Examples

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Embodiment 1

[0060] Comparative example 1 Aripiprazole tablet (10mg / tablet) formula and preparation method (unit: gram)

[0061]

[0062] (10mg / tablet) formula and preparation method of embodiment 1 aripiprazole tablet (unit: gram)

[0063]

Embodiment 2

[0064] Embodiment 2 Aripiprazole Capsules (10mg / grain) formula and preparation method

[0065] The granules (including sodium starch glycolate and magnesium stearate) before the tablet compression of Example 1 were passed through a 30-mesh sieve and mixed homogeneously, and packed into capsules.

Embodiment 3

[0066] Embodiment 3 Formula and preparation method of aripiprazole tablet (20mg / tablet) (unit: gram)

[0067]

[0068]

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PUM

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Abstract

The invention discloses an aripiprazole preparation which comprises aripiprazole and / or its pharmaceutically acceptable salts, and an auxiliary material, wherein the auxiliary material comprises an anti-oxidant. The anti-oxidant is preferably selected from one or more than one of sodium pyrosulfite, sodium bisulfite, sodium sulfite, thiourea, sodium hyposulfite, L-cysteine, sodium ascorbate, citric acid, sodium citrate, tartaric acid, sodium tartrate, malic acid, butylated hydroxyanisole, butylated hydroxytoluene, ascorbyl palmitate, and propyl gallate; the content of the anti-oxidant is 0.1-10% of the mass of the aripiprazole and / or its pharmaceutically acceptable salts. The invention also discloses a preparation method of the aripiprazole preparation. The aripiprazole preparation of the invention has significantly reduced amounts of related materials, good dissolution property and stability, high bioavailability, and less individual difference. The preparation method of the invention is simple in operation, and low in cost, requires no special equipment, and is easily applicable to industrial production.

Description

technical field [0001] The invention relates to an aripiprazole preparation 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)-quinolin Linone, a quinolinone derivative, was approved by the US FDA in November 2002 for the treatment of schizophrenia. [0003] Aripiprazole is known to exist in various crystal forms such as type I crystal and II crystal, and the currently marketed aripiprazole preparation products use type I crystal. Existing conventional methods to prepare Type I crystals cannot obtain fine particles. Generally, the particle size of the particles is relatively large (the average volume particle diameter D[4,3] is greater than 80 microns or greater than 100 microns), and the preparation of Type I crystals with larger particle sizes is used. When the drug is used, the dissolution rate in vitro is lower than 70% in 45 minutes, and the bioavailabi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P25/18
Inventor 郑斯骥谭波刘潇怡傅麟勇朱振明丁云晖张胤杰费海峰
Owner SHANGHAI ZHONGXI PHARMA
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