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Olanzapine composition and preparation method thereof

A technology for olanzapine and its composition, which is applied in the field of olanzapine composition and its preparation, can solve the problems of reduced water solubility and stability, and achieve the effects of fewer auxiliary materials, easy scale-up production, and good fluidity

Pending Publication Date: 2021-07-23
杭州新诺华医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As in the previous complaint, after olanzapine is prepared into tablets, there is a high risk of stability under high temperature, high humidity, and light, so the wet granulation process is not the first choice for the process; the inventors have shown through experiments that olanzapine Raw materials also have great instability under the condition of high concentration of oxides, and there are certain peroxides in the crospovidone excipients, and the high concentration of binders and disintegrants in the formula will lead to the hygroscopicity of the product , leading to a decrease in stability; on the other hand, olanzapine is a pH-dependent compound. As the pH increases, the water solubility decreases sharply. Excessive talcum powder and magnesium stearate in the formula will lead to dissolution of the product and the risk of BE

Method used

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  • Olanzapine composition and preparation method thereof
  • Olanzapine composition and preparation method thereof
  • Olanzapine composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] A kind of preparation method method of olanzapine composition, when it produces 10,000, comprise the steps:

[0034] (1) Pretreatment: Take olanzapine, lactose microcrystalline cellulose, and low-substituted hydroxypropyl cellulose to pass through 40 meshes respectively, and set aside; wherein the particle size of olanzapine is 4.58 μm-317 μm, and low-substituted hydroxypropyl cellulose Base cellulose, its content is 4%;

[0035] (2) Weighing: Olanzapine 0.1kg, MICROCELAC R 100 is 3.834kg, low-substituted hydroxypropyl cellulose is 0.125kg, magnesium stearate is 0.041kg;

[0036] (3) Mixing: put lactose microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and olanzapine in a mixer in sequence, and mix for 40 minutes at a speed of 15 r / min;

[0037] (4) Dry granulation: dry granulation parameters are: working pressure: 25bar; granulation screen: 0.8mm; make the granule Carr index less than 20%, and the angle of repose less than 30°;

[0038] (5) Lubric...

Embodiment 2

[0045] A kind of preparation method of described olanzapine composition, when it produces 10,000, comprise the steps:

[0046] (1) Pretreatment: Weigh olanzapine, lactose microcrystalline cellulose, and low-substituted hydroxypropyl cellulose to pass through 40 meshes respectively, and set aside; wherein the particle size of olanzapine is 4.58 μm-317 μm, and the low-substituted hydroxypropyl cellulose Propyl cellulose, its content is 4%;

[0047] (2) Weighing: olanzapine 0.05kg, lactose microcrystalline cellulose MICROCELAC R 100 is 1.917kg, low-substituted hydroxypropyl cellulose is 0.063kg, and magnesium stearate is 0.021kg. Weigh each raw material and auxiliary material according to the weight ratio;

[0048] (3) Mixing: put lactose microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and olanzapine in a mixer in sequence, and mix for 20 minutes at a speed of 15 r / min;

[0049] (4) Dry granulation: dry granulation parameters are: working pressure: 25bar; gr...

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Abstract

The invention relates to an olanzapine composition and a preparation method thereof. The olanzapine composition consists of olanzapine, a diluent, a disintegrating agent and a lubricant. The olanzapine composition is simple in formula, few in auxiliary materials, more economical and low in production cost. The preparation method is simple, the powder fluidity of the preparation is good, large-scale production is easy, and the product is more stable.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to an olanzapine composition and a preparation method thereof Background technique [0002] Olanzapine, the chemical name is 2-methyl-10-(4-methyl-1-piperazine)-4H-thieno[2,3-b][1,5]benzodiazepine Zhuo, a new atypical neuroleptic, can bind to dopamine receptors, 5-HT receptors and cholinergic receptors, and has an antagonistic effect. Antagonizing D2 receptors is related to the treatment of positive symptoms of schizophrenia; antagonizing 5-HT2A receptors is related to the treatment of negative symptoms of schizophrenia. Unlike clozapine, this product does not cause agranulocytosis, no tardive disorders and severe mental depression symptoms. Oral absorption is good, and food has no effect on its absorption rate, and the peak plasma concentration can be reached 5 to 8 hours after oral administration. It is mainly metabolized in the liver, and about 75% of this ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K47/26A61K47/38A61K31/5513A61P25/18
CPCA61K9/2806A61K9/2018A61K9/2054A61K9/2095A61K31/5513A61P25/18
Inventor 石晓宝余永华杨峰叶磊
Owner 杭州新诺华医药有限公司
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