Asenapine composition and preparation method thereof

A composition and substance technology, applied in the field of asenapine composition, can solve the problems of large-scale freeze-drying equipment, long production cycle, fragility, etc.

Active Publication Date: 2014-07-02
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this technology is that the resulting product has an open network skeleton structure, low strength, fragile, and difficult to maintain the integrity of the tablet
Moreover, the production line of this technology is expensive, requires large-scale freeze-drying equipment, the production cycle is long, and the cost of the finished product is too high

Method used

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  • Asenapine composition and preparation method thereof
  • Asenapine composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Prescription composition:

[0036] components content Asenapine Maleate 5 copies Anhydrous Directly Compressed Lactose 20 copies Spray Dried Mannitol 52.5 copies Camphor 17.5 servings PEG6000 5 copies

[0037] Preparation:

[0038] i) Asenapine maleate is passed through a 100-mesh sieve, and camphor is pulverized through a 60-mesh sieve for subsequent use;

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

[0040] iii) The mixed powder is directly compressed into tablets, and the hardness is maintained at 4-5kg / cm 2 about;

[0041] iv) Place the tablet at 80°C for heat treatment;

[0042] v) After 5 hours, take it out and weigh it to confirm that the camphor is completely removed.

Embodiment 2

[0044] Prescription composition:

[0045] components content Asenapine Maleate 5 copies Anhydrous Directly Compressed Lactose 20 copies Spray Dried Mannitol 52.5 copies Camphor 17.5 servings PEG6000 5 copies

[0046] Preparation:

[0047] i) Asenapine maleate is passed through a 100-mesh sieve, and camphor is pulverized through a 60-mesh sieve for subsequent use;

[0048] ii) mixing the prescribed amount of asenapine maleate, anhydrous direct compression lactose, spray-dried mannitol and camphor, and dry granulating;

[0049] iii) Add PEG6000 to the dry granules, mix well, and press into tablets;

[0050] iv) placing the tablet under the condition of 80° C., and heat treatment;

[0051] v) After 5 hours, take it out and weigh it to confirm that the camphor is completely removed.

Embodiment 3

[0053] Prescription composition:

[0054] components content Asenapine Maleate 10 copies Anhydrous Directly Compressed Lactose 17.5 servings Spray Dried Mannitol 52.5 copies Camphor 20 copies PEG6000 5 copies

[0055] Preparation:

[0056] i) Asenapine maleate is passed through a 100-mesh sieve, and camphor is pulverized through a 60-mesh sieve for subsequent use;

[0057] ii) First mix the prescribed amount of camphor with PEG6000 evenly, and then mix with the remaining ingredients in the prescription;

[0058] iii) The mixed powder is directly compressed into tablets, and the hardness is maintained at 4-5kg / cm 2 about;

[0059] iv) Place the tablet at 80°C for heat treatment;

[0060] v) After 5 hours, take it out and weigh it to confirm that the camphor is completely removed.

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Abstract

The invention relates to a composition which contains asenapine maleate and is taken by sublingual or buccal administration and a preparation method of the compositionBy using the asenapine maleate as an active ingredient and using an easy-sublimating pore-foaming agent, sublingual tablets which are quickly dispersed and dissolved under the tongue in tens of seconds are prepared, thus the active ingredient can be absorbed quickly through sublingual veins so as to enter blood circulation directly. The composition takes effect quickly and is convenient to take. The invention also discloses a novel in vitro evaluation method.

Description

technical field [0001] The invention relates to an asenapine composition, in particular to a composition for sublingual or buccal administration of asenapine, a preparation method thereof, and an accurate and controllable in vitro evaluation device and method. Background technique [0002] Asenapine was first disclosed in U.S. Patent US4145434, which disclosed trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenzo[2,3:6,7 ] Oxazo [4,5-c] pyrrole and preparation method thereof, its structural formula is as follows: [0003] [0004] Subsequent research reports have clarified that the maleate of asenapine is a very effective dopamine and serotonin antagonist with strong antipsychotic activity. The results of phase I clinical studies of oral asenapine show that it has serious cardiotoxicity, but this serious side effect can be basically avoided after sublingual or buccal administration. [0005] The pharmaceutical composition for sublingual or buccal administration has t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/407A61K47/34A61K47/10A61K47/26A61P25/18
Inventor 王悦张志宏梁敏耿佳金丽丽
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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