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Pharmaceutical composition containing Iloperidone and preparation method thereof

A technology of iloperidone and its composition, which is applied in the field of pharmaceutical compositions with good dissolution and its preparation, can solve the problems of particle re-aggregation and incomplete dissolution, and achieve the effects of improved dissolution, complete dissolution and improved dissolution

Inactive Publication Date: 2012-01-25
北京德众万全医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The particle size can be reduced by ordinary crushing methods, but when the hydrophobic iloperidone is crushed alone, as the surface area increases, the free energy increases, and the particles are prone to re-agglomeration, and the dissolution is still incomplete
In addition, in the design of the traditional preparation formulation process, the dissolution rate is often improved by increasing the disintegration speed of the preparation. Although the iloperidone pharmaceutical composition prepared according to this method disintegrates rapidly in the early stage, the final dissolution is still incomplete.

Method used

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  • Pharmaceutical composition containing Iloperidone and preparation method thereof
  • Pharmaceutical composition containing Iloperidone and preparation method thereof
  • Pharmaceutical composition containing Iloperidone and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]

[0032] Preparation:

[0033] (1) Mix iloperidone and the prescribed amount of lactose uniformly, and use a jet mill to pulverize together to form a solid dispersion;

[0034] (2) Mix the above-mentioned solid dispersion with lactose, hypromellose, and low-substituted hydroxypropyl cellulose in the prescribed amount of filler, add purified water to make soft material, and granulate with 18 mesh sieve. It is ventilated and dried at a temperature of 50°C. The granules are sieved with a 24-mesh sieve, weighed, and an additional portion of low-substituted hydroxypropyl cellulose, magnesium stearate and micronized silica gel are added in proportion to mix evenly, and then compressed.

Embodiment 2

[0036]

[0037]

[0038] Preparation:

[0039] (1) Mix iloperidone and the prescribed amount of lactose uniformly, and use a jet mill to pulverize together to form a solid dispersion;

[0040] (2) Mix the above-mentioned solid dispersion with lactose, microcrystalline cellulose, hydroxypropyl cellulose and a portion of sodium carboxymethyl starch in the prescribed amount of filler, add purified water to make soft material, and use 18 mesh sieve Granulate, ventilate and dry at a temperature of 50°C, sizing with a 24-mesh sieve, weighing, adding an additional portion of sodium carboxymethyl starch and magnesium stearate in proportion, mixing uniformly, and compressing.

Embodiment 3

[0042]

[0043] Preparation:

[0044] (1) Mix iloperidone and the prescribed amount of lactose uniformly, and use a jet mill to pulverize together to form a solid dispersion;

[0045] (2) Mix the above-mentioned solid dispersion with the prescription amount of calcium hydrogen phosphate, sodium carboxymethyl cellulose, and part of croscarmellose sodium, add purified water to make soft material, and make it with 18 mesh sieve The granules are ventilated and dried at a temperature of 50°C, sieved with a 24-mesh sieve, weighed, and an additional part of croscarmellose sodium, magnesium stearate and micronized silica gel are added in proportion, mixed evenly, and compressed.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a pharmaceutical composition containing Iloperidone and a preparation method thereof. In the invention, Iloperidone and lactose are prepared into solid dispersion, and a hydrophilic gel material is added to the prescription at the same time, thus improving the water insolubility of Iloperidone. The pharmaceutical composition containing Iloperidone provided by the invention has the characteristics that the water insolubility of Iloperidone is improved, the in-vitro dissolution is different from the characteristic that the traditional common preparation rapidly releases at the early stage, and the in-vitro dissolution is mild at the early stage, but is completed within 30 minutes.

Description

Technical field [0001] The invention relates to a pharmaceutical composition for the treatment of schizophrenia, in particular to a pharmaceutical composition containing iloperidone as an active ingredient with good dissolution and a preparation method thereof. Background technique [0002] Imperidone is an antagonist of serotonin and dopamine D2 receptors and is mainly used for the treatment of affective disorders including bipolar affective disorders. [0003] The clinical dosages of iloperidone published by the FDA are 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, and 12 mg. [0004] US Patent No. 5364866 discloses that the compound iloperidone can be used as an antipsychotic and analgesic. US Patent No. 5955459 discloses a composition containing a conjugate of fatty acid and iloperidone for the treatment of schizophrenia. [0005] CN94194302.X and CN02821426.9 disclose depot preparations of iloperidone and star polymers for long-acting antipsychotics. The preparation process of this prep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61K47/26A61P25/18
Inventor 慕博郭夏宋雪梅
Owner 北京德众万全医药科技有限公司
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