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Aripiprazole long-acting controlled-release microgranule injection and preparation method thereof

A technology of aripiprazole and sustained-release microparticles, which is applied in the field of aripiprazole long-acting sustained-release microparticle injections and its preparation, which can solve the problem that the drug cannot be completely released from the microparticles, and the ideal in vitro drug release behavior cannot be achieved. Slowness and other problems, to achieve the effect of overcoming sudden release, low burst release, and complete release

Active Publication Date: 2015-11-25
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Disclosed in CN1226821A is a method for preparing biodegradable microparticles. In order to reduce the use of halogenated solvents, benzyl alcohol is added as a mixed solvent, wherein the weight content of benzyl alcohol is less than 2%. Tests have proved that the ideal in vitro release rate cannot be achieved. drug behavior
The main weight content of the microparticles is 55-95%, that is, the drug loading is very high, but the release is quite slow, especially in the later stage of release, the drug cannot be completely released from the microparticles, and the high drug loading is easy to cause the burst release of the microparticles

Method used

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  • Aripiprazole long-acting controlled-release microgranule injection and preparation method thereof
  • Aripiprazole long-acting controlled-release microgranule injection and preparation method thereof
  • Aripiprazole long-acting controlled-release microgranule injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Preparation of Aripiprazole Microparticles:

[0055]

[0056] Dissolve polylactic acid-glycolic acid and aripiprazole with a solvent and a drug release characteristic modifier, then add it to the mixed solution of PVA and water, keep the curing temperature at 0°C, and emulsify at 1000 (rpm) for 30 minutes under magnetic stirring Finally, reduce the rotation speed and stir to 500 (rpm) for 1 hour to volatilize the solvent. After the microparticles are solidified, separate the microparticles and wash the microparticles continuously with sterile water for 8 hours. Filter out and dry in vacuum at room temperature for 24h;

[0057] The diameter of the obtained particles is 73.56±24.34 μm, the drug loading is 35.97%, and the encapsulation efficiency is 89.94%.

[0058] Adopt HPLC and GC method to detect, the weight percent content of each component of particle:

[0059]

[0060]

Embodiment 2

[0062] Preparation of Aripiprazole Microparticles:

[0063]

[0064] Dissolve polylactic acid and aripiprazole with a solvent and a drug release characteristic regulator, then add it to the mixed solution of PVA and water, keep the curing temperature at 5°C, and emulsify at 2000 (rpm) for 15 minutes under magnetic stirring, and then reduce Stir at a rotational speed of 500 (rpm) for 0.5 h to volatilize the solvent. After the microparticles are solidified, separate the microparticles and wash the microparticles continuously with sterile water for 8 hours. Filter out and dry in vacuum at room temperature for 24h;

[0065] The diameter of the obtained particles is 77.02±25.48 μm, the drug loading is 44.80%, and the encapsulation efficiency is 89.17%.

[0066] Adopt HPLC and GC method to detect, the weight percent content of each component of particle:

[0067]

Embodiment 3

[0069] Preparation of Aripiprazole Microparticles:

[0070]

[0071]

[0072] Dissolve polylactic acid-glycolic acid and aripiprazole with a solvent and a drug release characteristic regulator, then add it to the mixed solution of PVA and water, keep the curing temperature at 20°C, and emulsify at 1000 (rpm) for 20 minutes under magnetic stirring Finally, reduce the rotation speed and stir to 500 (rpm) for 1 hour to volatilize the solvent. After the microparticles are solidified, separate the microparticles and wash the microparticles continuously with sterile water for 8 hours. Filter out and dry in vacuum at room temperature for 24h;

[0073] The diameter of the obtained particles is 80.39±20.38 μm, the drug loading is 25.03%, and the encapsulation efficiency is 75.87%.

[0074] Adopt HPLC and GC method to detect, the weight percent content of each component of particle:

[0075]

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Abstract

The invention relates to an aripiprazole long-acting controlled-release microgranule injection and a preparation method thereof. The aripiprazole long-acting controlled-release microgranule injection is prepared from the following components in percentage by weight: 1-50% of aripiprazole, 48-97% of a high-molecular polymer, 1-5% of a medicine release characteristic regulator, and 0.01-0.5% of an emulgator, wherein the medicine release characteristic regulator is a mixed solvent of benzyl alcohol and dimethyl sulfoxide, and benzyl alcohol accounts of 70%-99% of the medicine release characteristic regulator based on the weight. The aripiprazole long-acting controlled-release microgranule injection has the advantages of controllable grain size, high medicine loading capacity, high encapsulation efficiency, low initial burst release, complete release, and continuous medicine release for one month or a longer time. According to the aripiprazole long-acting controlled-release microgranule injection, the medicine release characteristic regulator can regulate the medicine release characteristic of the preparation, so that the release amount of the medicine achieves 90% or above, the medicine is uniformly distributed in the microgranules and exists in the form of molecules, and therefore, the problem that during the release process, the medicine gradually forms crystals, and consequently, the release becomes slow is solved.

Description

technical field [0001] The invention relates to aripiprazole long-acting slow-release microparticle injection and a preparation method thereof. Background technique [0002] Aripiprazole (aripiprazole) is a quinolinone derivative with the chemical name "7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3, 4-dihydro-2(1H)-quinolinone” is a third-generation atypical antipsychotic drug. The drug has a unique mechanism of action, is a partial agonist of dopamine D2 and 5-HT1A receptors, and is a 5-HT2A receptor antagonist. It has the effect of stabilizing the activity of dopamine system. It has a significant effect on both positive and negative symptoms of schizophrenia, but it does not have some common side effects of other antipsychotic drugs. [0003] The common dosage forms of aripiprazole currently on the market include: tablet, orally disintegrating tablet, oral liquid, etc., making aripiprazole the first-line drug in the field of mental disease treatment and meeting t...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/50A61K31/496A61P25/18
Inventor 栾瀚森曹文佳王浩杨莉赵虹
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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