Orally rapidly disintegrating tablet comprising imidafenacin

一种迅速崩解、口腔内的技术,应用在含有效成分的医用配制品、有机活性成分、非有效成分的医用配制品等方向,达到给药容易、崩解性优异、光稳定性优异的效果

Active Publication Date: 2013-08-14
XINGLIN HLDG CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, it is difficult to coat the tablet with titanium oxide and ferric oxide while maintaining the disintegrating properties of the orally disintegrating tablet. agent has not yet been reported

Method used

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  • Orally rapidly disintegrating tablet comprising imidafenacin
  • Orally rapidly disintegrating tablet comprising imidafenacin

Examples

Experimental program
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preparation example Construction

[0039] In the preparation of the orally rapidly disintegrating tablet of the present invention, the coated granules containing midanacin or midanacin granules are mixed with a composition containing an excipient and a disintegrating agent. The amount of the composition containing the excipient and the disintegrating agent is, for example, 1 to 50 parts by mass, preferably 3 to 25 parts by mass, relative to 1 part by mass of the coated granulated product containing midanacine or midanacin granules. parts by mass.

[0040] The coated granules or midancin granules containing excipients and disintegrants, for example, can be prepared in a V-shaped mixer, a diamond mixer (diamond mixer), a drum Mixing in a mixer or the like.

[0041] Then, the resulting mixture is compression-molded to prepare the orally rapidly disintegrating tablet of the present invention.

[0042]Compression molding can be performed suitably using a tablet press such as a rotary tablet press, for example. Ho...

Embodiment 1

[0068] 4.0 g of midanacin and 2 g of Kollidon 90F (BASF) were dissolved in a mixed solution of 118.2 g of pure water and 275.8 g of ethanol. 394 g of Starch 1500G (Japanese カラコン) was loaded into a rotary fluidized bed granulator (manufactured by Dalton, NQ-160), and the solution was coated by top spray method (spray liquid volume 15g / min, spray pressure 0.1MPa, air supply temperature 70° C.) to obtain granules containing midanacin.

[0069] Separately, 60 g of a stomach-soluble polymer, EUDRAGIT EPO (Rohm GmbH & Co. KG), and 30 g of magnesium stearate (vegetable) (Taihei Chemical Industry) were dissolved in a mixed solution of 273 g of pure water and 637 g of ethanol.

[0070] 300 g of granulated matter containing midanacin was charged into a rotary fluidized bed granulator (manufactured by Dalton, NQ-160), and the solution was applied by the top spray method (spray liquid volume 20 g / min, spray pressure 0.15 MPa, Air supply temperature 80°C) to obtain coated particles.

[0...

Embodiment 2

[0073] 25.0 g of midanacin and 12.5 g of Kollidon 90F (BASF) were dissolved in a mixed solution of 738.75 g of pure water and 1723.75 g of ethanol. Starch 1500G (Japanese カラコン) 4962.5g is packed into a fluidized bed granulator (manufactured by FLOINT INDUSTRY, FL-5), and the solution is coated by the top spray method (spray liquid amount 100g / min, spray pressure 0.3MPa, air supply temperature 70° C.) to obtain midanacin-containing granules (average particle diameter: 128 μm). Separately, 750 g of EUDRAGITEPO (Rohm GmbH & Co. KG) and 375 g of magnesium stearate (vegetable) (Taihei Chemical Industry) were dissolved in a mixed solution of 3412.5 g of pure water and 7962.5 g of ethanol. 3750 g of the granulated matter containing midanacin was charged into a fluidized bed granulator (manufactured by Floint Industries, FL-5), and the solution was coated by the top spray method (spray liquid volume 100 g / min, spray pressure 0.3 MPa, Supply air temperature: 80° C.) to obtain coated p...

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Abstract

Provided herein is an imidafenacin-containing orally rapidly disintegrating tablet which is excellent in the photostability. The orally rapidly disintegrating tablets comprises (1) a granulated product containing imidafenacin or imidafenacin particles, which is or are coated with povidone or a gastric juice-soluble polymer; and (2) a composition containing an excipient and a disintegrating agent, wherein the resulting composition is subjected to compression molding.

Description

technical field [0001] The present invention relates to an orally rapidly disintegrating tablet containing imidafenacin as an active ingredient. Background technique [0002] Midanacin is a compound having muscarinic receptor M3 and M1 antagonistic activity (Patent Document 1), and is provided as a therapeutic drug for overactive bladder (Non-Patent Document 1). Oral solid preparations, percutaneous absorption preparations and the like containing midanacin are known as pharmaceutical formulations containing midanacin as a main component (Patent Documents 2 and 3). [0003] Patent Document 2 describes that since the midanacin preparation is unstable to light, photostability is achieved by coating a tablet with a coating liquid containing titanium oxide and ferric oxide. However, Patent Document 2 does not disclose the case where a coating is applied to the midanacin granules before tableting for photostabilization. [0004] In addition, Patent Document 3 is a percutaneous a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4164A61K9/20A61K47/32A61K47/36A61K47/38A61P13/10
CPCA61K9/205A61K9/2018A61K31/4164A61K9/0056A61K9/1652A61K9/5026A61P13/06A61P13/10
Inventor 石崎敏广青木芳延
Owner XINGLIN HLDG CO LTD
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