Iloperidone drug composition and preparation method thereof

A technology for iloperidone and a composition is applied in the field of pharmaceutical compositions containing iloperidone and the preparation thereof, and can solve the problems of poor tablet compressibility, poor action force, incomplete dissolution and the like

Active Publication Date: 2010-09-08
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tablets prepared by the above process have poor interaction between particles, small solid bridging force, are brittle and easy to break, and the tablet has poor compressibility. It is checked by the dissolution test method and the dissolution is not complete.

Method used

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  • Iloperidone drug composition and preparation method thereof
  • Iloperidone drug composition and preparation method thereof
  • Iloperidone drug composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] components

[0036] Preparation process: Weigh the micronized iloperidone according to the prescription quantity, the particle size of the active ingredient is more than 90% and less than 75 μm, weigh lactose and microcrystalline cellulose according to the prescription quantity, mix with 5% hydroxypropyl methylcellulose The plain aqueous solution is used as a binder to granulate, dried at 50°C, mixed with cross-linked povidone, micropowder silica gel and magnesium stearate, and compressed into tablets.

Embodiment 2

[0038] components

[0039] Preparation process: Weigh the co-pulverized iloperidone and lactose mixture according to the prescription amount, the particle size of the mixture is more than 90% and less than 75 μm, add the prescription amount of microcrystalline cellulose and mix, and use 5% hydroxypropyl methylcellulose The aqueous solution is used as a binder to granulate, dried at 50°C, mixed with cross-linked povidone, micropowder silica gel and magnesium stearate, and compressed into tablets.

Embodiment 3

[0041] components

[0042] Preparation process: Weigh the micronized iloperidone according to the prescription quantity, the particle size of the active ingredient is more than 90% and less than 75 μm, add the prescription quantity of lactose, microcrystalline cellulose and low-substituted hydroxypropyl cellulose and mix, 10% starch slurry Granulation. Dried at 50°C, mixed with low-substituted hydroxypropyl cellulose and magnesium stearate, and compressed into tablets.

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Abstract

The invention discloses a drug composition containing an Iloperidone active ingredient, which contains micronization Iloperidone or Iloperidone smashed with other accessories, can effectively enhances dissolution effect of Iloperidone.

Description

technical field [0001] The invention discloses a pharmaceutical composition for treating schizophrenia, in particular to a pharmaceutical composition containing iloperidone and a preparation method thereof. Background technique [0002] Iloperidone (see formula Ⅰ, iloperidone, Fanapt) is 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl ]propoxyl]-3-methoxyphenyl]ethanone is an antagonist of 5-hydroxytryptamine and dopamine D2 receptors, and is mainly used for the treatment of schizophrenia. [0003] [0004] Formula Ⅰ [0005] Iloperidone compounds were first disclosed in EP402644. [0006] At present, the dosage form of iloperidone approved by the United States is ordinary tablets, and the excipients are lactose monohydrate, microcrystalline cellulose, hydroxypropyl methylcellulose, crospovidone, magnesium stearate, micronized silica gel and pure Water (evaporated during preparation), wet granulation followed by tableting. The tablet prepared by the above-me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61K9/20A61P25/18A61J3/10
Inventor 蔡巍刘海丽郭夏
Owner AVENTIS PHARMA HAINAN
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