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Solid oral medicine composition containing aripiprazole microcrystal

A technology of aripiprazole and its composition, which is applied in the field of solid oral pharmaceutical compositions, can solve the problems of low bioavailability and achieve the effects of high bioavailability, improved bioavailability, and uniform and stable content

Active Publication Date: 2007-11-07
SHANGHAI ZHONGXI PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But the fine particle (micron order) of the aripiprazole type I crystal that discloses on Japan and South Korea Analytical Chemistry Annual Meeting also does not have bibliographical information, finds through the research of the present invention, the in vitro dissolution rate of the type I wafer prepared by the disclosed method of CN02801754 Less than 70% in 45 minutes, its bioavailability is relatively low, therefore, it is necessary to make a preparation with a particle size below 100um to improve its bioavailability, and the present invention is therefore completed

Method used

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  • Solid oral medicine composition containing aripiprazole microcrystal

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Preparation of Type I Microcrystals of Aripiprazole

[0034] Add 20g of crude aripiprazole and 240ml of ethanol into a three-necked reaction flask with a reflux condenser, heat to reflux under stirring, stop heating after the aripiprazole is completely dissolved, adjust the line speed to 500 m / min, and add 1 37ml of low-temperature water at ℃, cooled rapidly with ice-water mixture for 30min, suction filtered, washed, and the obtained crystals were dried in a desiccator at 80℃ for 10 hours under reduced pressure to obtain 19.2g of powdery aripiprazole crystals. By using water as a dispersant, it is measured with a Mastersizer 2000 laser particle size analyzer, and its volume average particle diameter is 26.456um.

Embodiment 2

[0036] Aripiprazole type I microchips (except type I microcrystals, the prescription is the same as the reference example, and the preparation method of microcrystals is shown in the examples)

[0037] prescription:

[0038] Aripiprazole (type I microcrystalline) 15g

[0039] Lactose 57g

[0040] Starch 10g

[0041] Microcrystalline Cellulose 10g

[0042] Hypromellose 2g

[0043] Magnesium stearate 0.9g

[0044] 94.9g 1000 pieces

[0045] Preparation process: with reference example.

Embodiment 3

[0047] Aripiprazole type I microchips

[0048] prescription

[0049] Aripiprazole (type I microcrystalline) 5g

[0050] Lactose 75g

[0051] Microcrystalline Cellulose 11g

[0052] Sodium starch glycolate 2.8g

[0053]Hypromellose 2.2g

[0054] Sodium starch glycolate (additional) 3.2g

[0055] Magnesium stearate 0.8g

[0056] 100g 1000 pieces

[0057] Preparation: Mix aripiprazole type I microcrystalline, hydroxymethyl starch sodium, microcrystalline cellulose, starch and lactose evenly, add hypromellose alcohol solution, mix, granulate, dry, sieve, and then add Sodium carboxymethyl starch, mix well, then add magnesium stearate, mix well, press into tablets.

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Abstract

The present invention relates to one kind of solid oral medicine composition containing aripiprazole microcrystal. The solid oral medicine composition contains type I microcrystal of aripiprazole in the average grain size below 50 micron in 1-50 mg and pharmaceutically acceptable supplementary material. The medicine composition has obviously raised aripiprazole dissolution, and raised bioavailability and curative effect of aripiprazole. It is used in treating metal diseases, such as schizophrenia.

Description

technical field [0001] The invention belongs to the field of preparations, and specifically relates to a solid oral pharmaceutical composition containing aripiprazole microcrystals, containing 1-50 mg of aripiprazole type I crystals and pharmaceutically acceptable pharmaceutical excipients, characterized in that: Aripiprazole The average particle size of the type I crystal of ripiprazole is not more than 50um. The dissolution rate of the aripiprazole of the composition of the invention is obviously improved, and the bioavailability and curative effect of the aripiprazole can be improved. Background technique [0002] Aripiprazole, an atypical psychotropic drug used to treat schizophrenia, has been marketed worldwide. Its chemical name is 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-butoxy}-3,4-dihydroquinolone or 7-{4-[4 -(2,3-Dichlorophenyl)-1-piperazinyl]-butoxy}-3,4-2(1H)-quinolone. [0003] Aripiprazole is a poorly soluble drug. When it is made into oral preparations s...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K47/36A61K47/38A61K47/10A61K47/34A61K9/20A61K9/48A61P25/18
Inventor 邓杰张涛王有妹郑斯骥樊斌
Owner SHANGHAI ZHONGXI PHARMA
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