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Spongy asenapine sublingual film agent with micropores and preparation method thereof

A kind of asenapine and sponge-like technology, applied in the field of asenapine preparations, can solve problems such as unfavorable production, transportation, storage and use, failure to achieve rapid onset of effect, unfavorable film formation, etc.

Active Publication Date: 2012-09-12
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not conducive to production, transportation, storage and use
The usual practice is to add a sufficient amount of plasticizer, but while increasing the proportion of plasticizer, the proportion of polymer materials is relatively reduced, which is not conducive to the formation of the film
In order to ensure the strength of the membrane when the proportion of polymer is small, it is necessary to use materials with higher molecular weight and higher viscosity, so that the dissolution of the membrane will be slowed down, and the effect of rapid onset of action will not be achieved.
[0009] And when adopting the technique disclosed by the inventor's prior patent application to prepare the asenapine film, the test found that there was also the defect that the film was brittle and fragile in the process of cutting and packaging, which needed to be improved.

Method used

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  • Spongy asenapine sublingual film agent with micropores and preparation method thereof
  • Spongy asenapine sublingual film agent with micropores and preparation method thereof
  • Spongy asenapine sublingual film agent with micropores and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] 80 g of PVA with a molecular weight of 130,000 Daltons and 20 g of HPC with a molecular weight of 600,000 Daltons were dissolved in 500 g of water to form a water slurry.

[0057] Add 100g of pore forming agent, 10g of asenapine, 2g of aspartame, 5g of glycerin, 0.1g of antioxidant BHA (tert-butyl p-hydroxyanisole) and 3g of titanium dioxide into the above water slurry, stir and mix.

[0058] The components of the pore-forming agent are chitin with a particle size of 0.5 μm and acetone adsorbed thereon, and the parts by weight of chitin and the parts by weight of the solvent are:

[0059] Chitosan 100 parts

[0060] Acetone 400 parts

[0061] (2) Then use the method reported in the literature of the study of nitroglycerin membranes (Chinese Journal of Pharmaceutical Industry, 1977, 12 (5)) to coat and form membranes to obtain thin film precursors;

[0062] (3) Dry the thin film precursor obtained in step (2) at 80°C to obtain the thin film for drug film preparation wi...

Embodiment 2

[0070] 60 g of PVP with a molecular weight of 10,000 Daltons and 30 g of HPC with a molecular weight of 1,000,000 Daltons were dissolved in 400 g of water to form a water slurry.

[0071] Add 90g pore-forming agent, 20g asenapine, 5g sucralose, 3g citric acid, 0.1g chelating agent EDTA (disodium ethylenediaminetetraacetic acid), 0.1g orange flavor and 2g titanium dioxide to the above water slurry In, stir and mix.

[0072] The components of the pore-forming agent include silicon dioxide micropowder with a particle size of 10 μm and acetone adsorbed thereon, the parts by weight of the microsilica powder and the parts by weight of the solvent are:

[0073] Silica powder 100 parts

[0074] Acetone 900 parts

[0075] Others are the same as embodiment 1.

[0076] The weight ratio of each component:

[0077] Low molecular weight water-soluble polymer material: high molecular weight water-soluble polymer material=2:1;

[0078] Water-soluble polymer material: water-insoluble micr...

Embodiment 3

[0082] Dissolve 60 g of sodium alginate with a molecular weight of 32,000 Daltons and 120 g of CMC-Na with a molecular weight of 700,000 Daltons in 700 g of water to form a water slurry.

[0083] Add 90g pore-forming agent, 50g asenapine, 5g cyclamate, 3g maleic acid, 0.1g antioxidant BHT (tert-butyl hydroxytoluene), 2g PEG400 and 3g titanium dioxide to the above water slurry, stir and mix .

[0084] The components of the pore-forming agent include CaCO3 with a particle size of 1 μm and ethanol adsorbed thereon, and the parts by weight of CaCO3 and the parts by weight of the solvent are:

[0085] CaCO3 100 parts

[0086] Ethanol 100 parts

[0087] Others are the same as embodiment 1.

[0088] The weight ratio of each component:

[0089] Low molecular weight water-soluble polymer material: high molecular weight water-soluble polymer material=1:2;

[0090] Water-soluble polymer material: water-insoluble micropowder = 1:0.25;

[0091] The diameter of the micropores is 10 nm...

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Abstract

The invention provides a spongy asenapine sublingual film agent with micropores and a preparation method thereof. The film agent comprises asenapine, water-soluble macromolecular materials and water-insoluble micro powder dispersed in the water-soluble macromolecular materials, wherein the molecular weight of at least one of the water-soluble macromolecular materials is 10000 to 200000 daltons, and the molecular weight of at least one of the water-soluble macromolecular materials is 200000 to 10000000 daltons. The film agent has a very remarkable effect, the film is quickly dissolved through the macromolecular material with low molecular weight, and the physical strength and the toughness of the film are ensured through the macromolecular material with high molecular weight, so that the aim of quick release is fulfilled and the strength of the film is ensured.

Description

technical field [0001] The invention relates to an asenapine preparation. Background technique [0002] Since Clozapine (Clozapine) was used in psychiatric clinics in the 1990s, new atypical antipsychotics have been widely used one after another. 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 for various dopamine, serotonin, norepinephrine receptor and histamine receptor subtypes, and has high affinity for 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 by FDA on August 14, 2009 for listing, and on November 27, 2009, it was approved for listing by the European Union und...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/407A61K47/38A61K47/36A61K47/34A61K47/32A61P25/18
Inventor 陈芳侯惠民沈利沈芃夏怡然张桦
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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