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Asenapine maleate tablet and preparation method thereof

A technology of asenapine maleate and excipients, which is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of increasing production cycle and production cost, increasing related substances, Complex formulation process and other problems, to avoid the increase of total impurities, to solve the friability, and to achieve the effect of simple process

Inactive Publication Date: 2019-02-01
天津仁生医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The preparation of asenapine maleate sublingual tablets in the prior art is mainly divided into freeze-drying technology and porogen sublimation technology: freeze-drying technology can prepare rapidly disintegrating preparations, but its product friability is relatively poor , and increase the production cycle and production cost
Porogen sublimation technology, the product obtained is also a loose structure, so it also has a certain impact on the friability, the prescription process is relatively complicated and the preparation process requires high temperature to sublimate the porogen, resulting in the increase of related substances

Method used

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  • Asenapine maleate tablet and preparation method thereof
  • Asenapine maleate tablet and preparation method thereof
  • Asenapine maleate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] prescription:

[0028]

[0029] The process steps are as follows:

[0030] 1. Mix asenapine maleate and antioxidant through a 40-mesh sieve;

[0031] 2. After "1" is mixed with the filler / disintegrant compound in equal increments, mix at a medium speed for 10 minutes;

[0032] 3. Pass magnesium stearate through a 40-mesh sieve, add "2" and mix at medium speed for 3 minutes;

[0033] 4. The mixture in "3" is pressed into tablets with a suitable punch (φ7mm), with a hardness of 65-85N.

Embodiment 2

[0035] prescription:

[0036]

[0037] Process steps are as follows:

[0038] 1. Pass asenapine maleate through a 100-mesh sieve and camphor through a 60-mesh sieve for later use;

[0039] 2. First mix the prescribed amount of camphor and PEG6000 evenly, and then mix with the remaining ingredients in the prescription;

[0040] 3. Press the mixed powder directly into tablets, and maintain the hardness at 4-5kg / cm 2 about;

[0041] 4. Heat the tablet at 80°C;

[0042] After 5.5 hours, it was taken out and weighed to confirm that the camphor was completely removed.

Embodiment 3

[0044] prescription:

[0045]

[0046] Process step is with embodiment 1.

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Abstract

The invention provides an asenapine maleate tablet and a preparation method thereof. The asenapine maleate sublingual tablet comprises a main drug and an auxiliary material. The main drug is asenapinemaleate. The auxiliary material includes a compound of filler and a disintegrating agent, a lubricant and an antioxidant. The preparation method adopts a direct compression technology, and specifically includes: sieving asenapine maleate with an antioxidant together and performing mixing, then conducting mixing with the compound of the filler and the disintegrating agent by equivalent progressiveincreasing process, then adding the lubricant, performing mixing, and then conducting punching tabletting. The technology adopted by the invention can realize rapid disintegration and dissolution, avoids the friability problem brought about by porous structure and related substance increase caused by high temperature or oxidation, also the technology has the characteristics of simple process andcost saving, and is easy for scale-up production.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, in particular to a kind of asenapine maleate tablet and a preparation method thereof. Background technique [0002] Schizophrenia is a chronic and disabling mental disorder characterized by incoordination among perception, thinking, emotion, and behavior, and separation of mental activities from reality. cause great pain. [0003] Asenapine maleate sublingual tablet, the original product name SAPHRIS, was developed by Allergan USA, Inc., and was first approved by the US FDA in 2009. For the treatment of schizophrenia and bipolar I disorder in adults. [0004] Chinese patent CN 95191906.7 discloses a sublingual tablet containing medicinal water-soluble or water-dispersible carrier substance, prepared by freeze-drying process and its preparation method. [0005] Chinese patent CN103893139B discloses a method for preparing rapidly disintegrating asenapine maleate sublingual tablets b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/407A61K47/36A61K47/26A61K47/32A61K47/10A61K47/02A61P25/18A61P25/24
CPCA61K9/006A61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2059A61K9/2095A61K31/407A61P25/18A61P25/24
Inventor 司宗为左人杰孙超
Owner 天津仁生医药科技有限公司
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