Asenapine tablets and preparation method thereof

A technology of asenapine tablets and flat tablets, which is applied in the field of new atypical antipsychotic preparations, can solve the problems of high manufacturing price and inconvenient administration for mental patients, and achieve the effect of improving the dissolution effect

Inactive Publication Date: 2017-05-17
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, sublingual lozenges and sublingual mucosa are both i

Method used

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  • Asenapine tablets and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Asenapine tablet of the present embodiment and preparation method, its each component is:

[0023] 1000 tablets Composition g

[0024] Asenapine 10

[0025] Mannitol 96

[0026] Croscarmellose Sodium 24

[0027] Sodium Lauryl Sulfate 2.5

[0028] Stevioside 1

[0029] Talc v 1.5

[0030] Total 135

[0031] The steps are:

[0032] 1. Micronize 100g of asenapine and 133g of mannitol together, and control the particle size to 0.5-5um;

[0033] 2. Dry and mix 36g of croscarmellose sodium and 2.9g of sodium lauryl sulfate through a 100-mesh sieve for 5 minutes;

[0034] 3. The fine powder obtained in the previous step and 1 / 2 of the disintegrating agent are made into a soft material with an aqueous ethanol solution, and granulated with a 20-mesh sieve;

[0035] 4. Dry the prepared granules at 50°C and sieve with 18 meshes;

[0036] 5. Add the remaining 1 / 2 of the disintegrating agent and 1g of stevioside to the dry granules and mix for 5 minutes, then add 2.1g of t...

Embodiment 2

[0038] Asenapine tablet of the present embodiment and preparation method, its each component is:

[0039] 1000 tablets Composition g

[0040] Asenapine 5

[0041] Lactose 100

[0042] Sodium carboxymethyl starch 16

[0043] Sodium Lauryl Sulfate 1.8

[0044] Aspartan 1.2

[0045] Magnesium Stearate 1

[0046] Total 125 The steps are:

[0047] 1. Micronize 100g of asenapine and 154g of lactose together, and control the particle size to 1-5um;

[0048] 2. Dry and mix 32g sodium carboxymethyl starch and 1.8g sodium lauryl sulfate through an 80-mesh sieve for 5 minutes;

[0049] 3. The fine powder obtained in the previous step and 1 / 2 of the disintegrating agent are made into a soft material with an aqueous ethanol solution, and granulated with a 20-mesh sieve;

[0050] 4. Dry the prepared granules at 60°C, and sieve with 18 meshes;

[0051] 5. Add the remaining 1 / 2 of the disintegrating agent and 1.2g of aspartame to the dry granules and mix for 10 minutes, then add 1g o...

Embodiment 3

[0052] Embodiment 3 The asenapine tablet of the present embodiment and preparation method, its each composition is:

[0053] 1000 tablets Composition g

[0054] Asenapine 10

[0055] Lactose 125

[0056] Low-substituted hydroxypropyl cellulose 32

[0057] Sodium Lauryl Sulfate 1

[0058] Aspartan 1.1

[0059] Magnesium stearate 0.9

[0060] Total 170

[0061] The steps are:

[0062] 1. Micronize 100g of asenapine and 137g of lactose together, and control the particle size to 2-8um;

[0063] 2. Dry and mix 28g of low-substituted hydroxypropyl cellulose and 2g of sodium lauryl sulfate through an 80-mesh sieve for 5 minutes;

[0064] 3. The fine powder obtained in the previous step and 1 / 2 of the disintegrating agent are made into a soft material with an aqueous ethanol solution, and granulated with a 20-mesh sieve;

[0065] 4. Dry the prepared granules at 70°C and sieve with 18 meshes;

[0066] 5. Add the remaining 1 / 2 of the disintegrating agent and 1.2g of aspartame ...

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Abstract

The invention provides Asenapine tablets and a preparation method thereof. The tablets comprise the following components in percentages by weight: 10-50% of Asenapine, 30-80% of a filler, 3-20% of a disintegrating agent, 0.5-1% of lubricant, and 0.2-2.5% of a flavouring. The preparation method comprises the following steps: micronization is carried out for Asenapine and the filler, and the particle size is controlled at 0.5-20[mu]m; the fine powder obtained in the last step and partial disintegrating agent are prepared into a soft material with an ethanol water, and granulation is carried out with 24 mesh sieve; prepared fine granules are dried at 50-70 DEG C, and granulation is carried out with 20 mesh sieve; the residual disintegrating agent, the flavouring and the lubricant are added into dried particles in order, total mixing is carried out twice, one mixing is carried out before the lubricant is added, the other mixing is carried out after the lubricant is added, till intermediate detection is qualified, the tablets are compressed, and the product is prepared. Asenapine tablets are common tablets with coating or without coating, the product is a novel atypical antipsychotic drug; the drug has the advantages of fast drug absorption, high bioavailability, and usage convenience.

Description

technical field [0001] The present invention relates to a novel atypical antipsychotic preparation, specifically a tablet, including coated or uncoated ordinary tablet, chewable tablet and orally disintegrating tablet. Background technique [0002] Asenapine is a new type of atypical antipsychotic drug for the treatment of adults with acute schizophrenia and acute mania or mixed episodes with bipolar I disorder. Its exact mechanism is still not very clear, it may be related to the antagonism of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A). Asenapine has high affinity to various dopamine, serotonin, norepinephrine receptor and histamine receptor subtypes, N-methyl-D-aspartic acid (NMDA) and α-amino- 3-Hydroxy-5-methyl-4-isoxazolepropionic acid (NMPA) receptors also have affinity. [0003] Asenapine sublingual tablet was approved for marketing by FDA on August 14, 2009, and was approved for marketing by EU on November 27, 2009. The trade name is Saphris. The bioavailabil...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/407A61K47/20A61P25/18
Inventor 严洁
Owner TIANJIN HANRUI PHARMA
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