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Industrial preparation method of micronized iloperidone

A micronization technology of iloperidone, which is applied in the field of preparation of iloperidone ultrafine powder, and achieves the effects of safe operation, simple process and low cost

Inactive Publication Date: 2015-02-04
山东省生物医药科学院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] In view of the deficiencies in the prior art, the purpose of the present invention is to provide a method for preparing micronized iloperidone with simple process, safe operation, low cost and easy industrial scale-up production. controllable problem

Method used

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  • Industrial preparation method of micronized iloperidone
  • Industrial preparation method of micronized iloperidone
  • Industrial preparation method of micronized iloperidone

Examples

Experimental program
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Effect test

Embodiment 1

[0051] Add 100g of commercially available iloperidone raw material drug into 500ml of methanol, heat to reflux to dissolve, add the methanol solution of iloperidone into 5000ml of water at 50°C at a stirring speed of 1000rpm, cool to 30°C and age for 2h, filter , dried at 50-60°C to obtain the micronized iloperidone product, the particle size test is as follows: image 3 Shown, the product average particle size D 90 =4.692μm, purity 99.975%, the chromatogram of related substances is as follows Figure 4 .

Embodiment 2

[0053]Add 100g of commercially available iloperidone raw material drug into 1000ml of ethanol, heat to reflux to dissolve, add the ethanol solution of iloperidone into 10000ml of 50°C water at a stirring speed of 1000rpm, cool down to 40°C and age for 3h, then filter , dried at 50-60°C to obtain the micronized iloperidone product, tested by particle size analyzer as Figure 5 Shown, the product average particle size D 90 =4.996μm, purity 99.974%, the chromatogram of related substances is as follows Figure 6 .

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Abstract

An industrial preparation method of micronized iloperidone belongs to the field of medical ultrafine powder preparation, especially preparation of an iloperidone ultrafine powder. Specifically, iloperidone is dissolved in an organic solvent to obtain an iloperidone solution; at a certain temperature, the iloperidone solution is added into an anti-solvent according to a certain volume ratio of the solution to the anti-solvent; after full stirring and mixing, iloperidone crystals are precipitated; and after aging at a certain temperature, filtration and drying are carried out successively to obtain the iloperidone ultrafine powder product. The method is simple, and all operations are safe. In addition, the method is low-cost and is easy for industrial large-scale production. The product obtained has higher purity and faster dissolution rate.

Description

technical field [0001] The invention belongs to the field of medicine ultrafine powder preparation, in particular to the preparation of iloperidone ultrafine powder. Background technique [0002] Iloperidone is a benzisoxazole compound, its English name is Iloperidone, its chemical name is 4,-[3-[4-(6-fluoro-1,2-benzisoxazole-3- ) piperidinyl] propoxy]-3,-methoxyacetophenone, its structural formula is: [0003] [0004] Iloperidone was developed by Norvatis Pharmaceutical Company of the United States (produced by VANDA Pharmaceutical Company), and its tablet FANAPT (iloperidone tablets) was approved by the FDA on May 6, 2009 for listing, which is clinically used for the treatment of adult schizophrenia. Iloperidone is a mixed dopamine D2 / 5HT2A receptor blocker, which belongs to atypical antipsychotics. Compared with the currently used antipsychotic drugs, iloperidone has fewer side effects and will not induce diabetes in patients. There were also fewer extracorporeal sy...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/454A61P25/18
Inventor 郑德强毋立华纪红英李大伟王长斌张利剑
Owner 山东省生物医药科学院有限公司
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