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Iloperidone 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 fluidity, large difference in tablet weight, loose particles, etc. Simple composition, rapid dissolution effect

Active Publication Date: 2012-12-05
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] 3. In the composition of CN101822673A and CN101822674A, sodium lauryl sulfate is used to solubilize insoluble drugs and improve their dissolution rate, but sodium lauryl sulfate has irritating effects on mucous membranes and upper respiratory tract, and is irritating to eyes and skin It can cause an allergic reaction in the respiratory system, and release toxic gas when it is decomposed by high heat, which is extremely unfavorable to the safety of operators and environmentally friendly when used in large quantities in production.
CN101822673A and CN101822674A think that no binder can be used, but for the variety of iloperidone, the direct consequence of not using binder is that the particles are loose, the fluidity becomes poor, and the difference in tablet weight becomes larger, which eventually leads to uneven content uniformity. qualified
[0017] It can be seen that the only two patents CN101822673A and CN101822674A on the rapid release of iloperidone do not provide an ideal iloperidone pharmaceutical composition

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1 High-pressure homogenization method, controlling more than 90% of the particle size to be less than 5 μm

[0080]

[0081]

[0082] Preparation Process:

[0083] i) The iloperidone raw material is pulverized and passed through a 100-mesh sieve (150 μm) for subsequent use;

[0084] ii) Disperse iloperidone passing through a 100 mesh sieve in 2.5% hydroxypropyl methylcellulose aqueous solution to form an initial suspension containing 13% iloperidone;

[0085] iii) The primary suspension is homogenized under high pressure until the particle size of iloperidone in the suspension is more than 90% and less than 5 μm;

[0086] iv) measure iloperidone content in the suspension after high-pressure homogenization, calculate, and dilute to the suspension that iloperidone content is 10% with 2.5% hydroxypropyl methylcellulose aqueous solution;

[0087] v) Weigh lactose, microcrystalline cellulose, 6% crospovidone and hydroxypropyl methylcellulose powder that has ...

Embodiment 2

[0092] Embodiment 2 High-pressure homogeneous method, controlling more than 90% of the particle size to be less than 10 μm

[0093]

[0094]

[0095] Preparation Process:

[0096] i) The iloperidone raw material is pulverized and passed through a 100-mesh sieve (150 μm) for subsequent use;

[0097] ii) Disperse iloperidone passing through a 100 mesh sieve in 2.5% hydroxypropyl methylcellulose aqueous solution to form an initial suspension containing 13% iloperidone;

[0098] iii) The initial suspension is homogenized under high pressure until the particle size of iloperidone in the suspension is more than 90% and less than 10 μm;

[0099] iv) measure iloperidone content in the suspension after high-pressure homogenization, calculate, and dilute to the suspension that iloperidone content is 10% with 2.5% hydroxypropyl methylcellulose aqueous solution;

[0100] v) Weigh lactose, microcrystalline cellulose, crospovidone and hydroxypropyl methylcellulose powder not config...

Embodiment 4

[0107] Embodiment 4 High-pressure homogenization method, controlling more than 90% of the particle size to be less than 25 μm

[0108]

[0109] Preparation Process:

[0110] i) The iloperidone raw material is pulverized and passed through a 100-mesh sieve (150 μm) for subsequent use;

[0111] ii) Disperse iloperidone passing through a 100 mesh sieve in 5% hydroxypropyl methylcellulose aqueous solution to form an initial suspension containing 21% iloperidone;

[0112] iii) The primary suspension is homogenized under high pressure until the particle size of iloperidone in the suspension is more than 90% and less than 25 μm;

[0113] iv) measure the iloperidone content in the suspension after high-pressure homogenization, calculate, and dilute to the suspension that the iloperidone content is 20% with 5% hydroxypropyl methylcellulose aqueous solution;

[0114] v) Weigh lactose, microcrystalline cellulose, 6% crospovidone and hydroxypropyl methylcellulose powder that has not...

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Abstract

The invention relates to an iloperidone composition and a preparation method thereof. According to the iloperidone composition, iloperidone which is taken as an active ingredient is pretreated, so that the particle size of the iloperidone is minimized; and therefore, the dissolution rate of the iloperidone is effectively increased.

Description

technical field [0001] The invention relates to an anti-schizophrenia pharmaceutical composition, in particular to a pharmaceutical composition containing iloperidone and a preparation method thereof. Background technique [0002] Schizophrenia is a disorder characterized by deep cognitive and emotional dissociations that affect the most basic human behaviors, such as language, thinking, perception, and self-awareness. The symptoms of the disease include a wide range, the most common being mental disorders, such as hallucinations, paranoia and delusions. [0003] Iloperidone not only effectively treats the positive symptoms of schizophrenia (hallucinations, delusions, disordered thinking, hostility, suspicion, and strange behavior), but also reduces the occurrence of extrapyramidal syndrome (EPS), and can improve Negative symptoms of schizophrenia (unresponsiveness, flat affect and language, social withdrawal, and lack of concentration). [0004] The structure of iloperido...

Claims

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Application Information

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IPC IPC(8): A61K31/454A61K9/20A61K9/48A61K9/14A61P25/18
Inventor 张志宏高子彬杜艳玲李硕陈勇军辛伟
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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