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Aripiprazole long-acting suspension and preparation method thereof

A technology of aripiprazole and suspension, which is applied in the field of medicine, can solve the problems of poor dispersibility of aripiprazole freeze-dried suspension, and achieve the effects of improving drug safety, improving preparation stability, and low production cost

Inactive Publication Date: 2016-06-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The present invention mainly solves the problem of poor dispersibility of the aripiprazole freeze-dried suspension when it is reconstituted with water before use, so as to obtain a long-acting aripiprazole preparation with good slow-release effect and safety, and meet the clinical medication needs of patients

Method used

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  • Aripiprazole long-acting suspension and preparation method thereof
  • Aripiprazole long-acting suspension and preparation method thereof
  • Aripiprazole long-acting suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: Preparation of Aripiprazole Long-acting Suspension (400mg / 2ml)

[0039]

[0040] First, the aripiprazole was pulverized with a jet mill (MX-50 supersonic jet mill, Yixing Juneng Superfine Pulverization Equipment Co., Ltd.), with an average particle size of 1-15 μm. Then, add 100 g of pulverized aripiprazole, 201.25 g of polysorbate and appropriate amount of water into a horizontal grinder (SWZX-0.4 horizontal grinder, Shanghai Shihe Electromechanical Equipment Co., Ltd.), and start grinding at 20 Hz. Grind for 10 minutes to pre-disperse the drug with water, add 3.125 g of sodium carboxymethylcellulose, 18.75 g of mannitol, 0.2 g of sodium dihydrogen phosphate monohydrate and the remaining water, increase the grinding speed, and continue grinding for 30 minutes at 45 Hz. Adjust the pH to 7 with 2N sodium hydroxide solution to obtain a preliminary suspension. Finally, the sample was transferred to a three-dimensional movable colloid mill, and circulated ...

Embodiment 2

[0043] Embodiment 2: Preparation of Aripiprazole Long-acting Suspension (300mg / 2ml)

[0044]

[0045] First, the aripiprazole was pulverized with a jet mill (MX-50 supersonic jet mill, Yixing Juneng Superfine Pulverization Equipment Co., Ltd.), with an average particle size of 1-15 μm. Then, 75g of crushed aripiprazole, 201.25g of polysorbate and appropriate amount of water were added to a horizontal grinder (SWZX-0.4 horizontal grinder, Shanghai Siehe Electromechanical Equipment Co., Ltd.), and the grinding was started at 20 Hz. Grind for 10 minutes to pre-disperse the drug with water, add 3.125 g of sodium carboxymethylcellulose, 18.75 g of mannitol, 0.2 g of sodium dihydrogen phosphate monohydrate and the remaining water, increase the grinding speed, and continue grinding for 30 minutes at 45 Hz. Adjust the pH to 7 with 2N sodium hydroxide solution to obtain a preliminary suspension. Finally, the sample was transferred to a three-dimensional movable colloid mill, and ci...

Embodiment 3

[0048] Embodiment 3: Preparation of Aripiprazole Long-acting Suspension (400mg / 2ml)

[0049]

[0050]

[0051] First, the aripiprazole was pulverized with a jet mill (MX-50 supersonic jet mill, Yixing Juneng Superfine Pulverization Equipment Co., Ltd.), with an average particle size of 1-15 μm. Then, add 100 g of pulverized aripiprazole, 201.25 g of polysorbate and appropriate amount of water into a horizontal grinder (SWZX-0.4 horizontal grinder, Shanghai Shihe Electromechanical Equipment Co., Ltd.), and start grinding at 20 Hz. Grind for 10 minutes to pre-disperse the drug with water, add 6.25 g of sodium carboxymethylcellulose, 18.75 g of mannitol, 0.2 g of sodium dihydrogen phosphate monohydrate and the remaining water, increase the grinding speed, and continue grinding for 30 minutes at 45 Hz. Adjust the pH to 7 with 2N sodium hydroxide solution to obtain a preliminary suspension. Finally, the sample was transferred to a three-dimensional movable colloid mill, and ...

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Abstract

The purpose of the invention is to provide an aripiprazole long-acting freeze-dried powder preparation which can be compounded with water to easily disperse in order to obtain a uniform suspension. The invention concretely relates to an aripiprazole long-acting preparation and a preparation method thereof. The preparation method comprises the following steps: commonly grinding micronized aripiprazole, a surfactant and water, adding a suspending aid, a freeze-drying excipient, a pH adjusting agent and residual injection water, grinding and dispersing to obtain a suspension, and freeze-drying the suspension to obtain the aripiprazole long-acting preparation. The above surfactant, medicine and water grinding process can increase the interaction of the medicine and water, and promotes the rapid dispersion of the medicine in the water compounding process before use. The preparation slowly releases in 1 month, and has the advantages of good and stable slow release effect, simple dosage form and preparation method, low cost, and convenient use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a long-acting intramuscular injection preparation of aripiprazole, which can be released slowly within one month. The present invention also relates to the preparation method and application of the sustained-release preparation. Background technique [0002] US Patent No. 5,006,528 discloses the structural formula and use of Aripiprazole. As a quinolinone derivative, aripiprazole is a partial agonist of dopamine and 5-HT1A receptors. It was approved for marketing by the US FDA in November 2002. It is mostly used clinically for the treatment of atypical psychiatric diseases. Studies have shown that aripiprazole is effective in treating positive and negative symptoms of schizophrenia, has few adverse reactions, and is well tolerated by patients. [0003] [0004] At present, aripiprazole has several oral preparations on the market, mainly including tablets, oral l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/496A61K47/44A61K47/36A61K47/32A61P25/18
CPCA61K9/19A61K9/0002A61K9/0019A61K31/496A61K47/26A61K47/32A61K47/44
Inventor 柯学杨淼吕会茹常双延刘艳红袁梦
Owner CHINA PHARM UNIV
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