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Mirabegron sustained-release composition as well as preparation method and application thereof

A technology for a composition and a sustained-release tablet, which is applied in the field of mirabegron sustained-release composition and its preparation, can solve the problems of cumbersome granulation operation, difficulty in the content uniformity of active ingredients, etc. Particle size requirements, the effect suitable for industrial production

Pending Publication Date: 2021-11-19
重庆世森医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are certain defects in its process: its preparation method adopts wet granulation and dry granulation, and the granulation operation is cumbersome; and the content uniformity of active ingredients is a difficult point to control in the process

Method used

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  • Mirabegron sustained-release composition as well as preparation method and application thereof
  • Mirabegron sustained-release composition as well as preparation method and application thereof
  • Mirabegron sustained-release composition as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] The formulation of Mirabegron extended-release tablets:

[0069]

[0070] The preparation method of Mirabegron sustained-release tablet, comprises the steps:

[0071] (1) Pass the hydroxypropyl cellulose, micronized silica gel and magnesium stearate through a 60-mesh sieve for later use.

[0072] (2) Under nitrogen protection, heat 468g of polyoxyethylene and 490g of polyethylene glycol 8000 in a water bath (60°C-80°C), and stir until melting.

[0073] (3) Add 225 g of mirabegron and 2.5 g of dibutyl hydroxytoluene to the above co-melt, stir for 10 min, and mix well. Allow to cool to room temperature and become solid.

[0074] (4) Use a water-cooled pulverizer (installed with a 20-mesh screen) to pulverize the above solid, use an ice-water bath to control the pulverization temperature below 20°C, measure the particle size after the pulverization, D 90 is 506 μm.

[0075] (5) Mix the pulverized material and 15 g of hydroxypropyl cellulose in a mixer for 10 minutes...

Embodiment 2

[0081] The formulation of Mirabegron extended-release tablets:

[0082]

[0083] The preparation method of Mirabegron sustained-release tablet, comprises the steps:

[0084] (1) Pass the hydroxypropyl cellulose, micronized silica gel and magnesium stearate through a 60-mesh sieve for later use.

[0085] (2) Under nitrogen protection, heat 434g of polyoxyethylene and 544g of polyethylene glycol 8000 in a water bath (60°C-80°C), and stir until melting.

[0086] (3) Add 225 g of mirabegron and 2.5 g of dibutyl hydroxytoluene to the above co-melt, stir for 10 min, and mix well. Allow to cool to room temperature and become solid.

[0087] (4) Use a water-cooled pulverizer (installed with a 20-mesh screen) to pulverize the above solid, use an ice-water bath to control the pulverization temperature below 20°C, measure the particle size after the pulverization, D 90 is 500 μm.

[0088] (5) Mix the pulverized material and 20 g of hydroxypropyl cellulose in a mixer for 10 minutes...

Embodiment 3

[0094] The formulation of Mirabegron extended-release tablets:

[0095]

[0096] The preparation method of Mirabegron sustained-release tablet, comprises the steps:

[0097] (1) Pass the hydroxypropyl cellulose, micronized silica gel and magnesium stearate through a 60-mesh sieve for later use.

[0098] (2) Under nitrogen protection, heat 400g of polyoxyethylene and 568g of polyethylene glycol 8000 in a water bath (60°C-80°C), and stir until melting.

[0099] (3) Add 225 g of mirabegron and 2.5 g of dibutyl hydroxytoluene to the above co-melt, stir for 10 min, and mix well. Allow to cool to room temperature and become solid.

[0100] (4) Use a water-cooled pulverizer (installed with a 20-mesh screen) to pulverize the above solid, use an ice-water bath to control the pulverization temperature below 20°C, measure the particle size after the pulverization, D 90 is 518 μm.

[0101] (5) Mix the pulverized material and 35 g of hydroxypropyl cellulose in a mixer for 10 minutes...

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Abstract

The invention discloses a mirabegron sustained-release composition as well as a preparation method and application thereof. The composition comprises an active component mirabegron and a pharmaceutical adjuvant, the pharmaceutic adjuvant at least contains an antioxidant, and the antioxidant is selected from at least one of butylated hydroxytoluene, butylated hydroxyanisole and vitamin E. The preparation method comprises the steps: preparing a co-melt mixture containing mirabegron, a gelling agent, a gel reinforcing agent and an antioxidant under the protection of nitrogen, and crushing the co-melt mixture with a water-cooling crusher to form particles with uniformly distributed active ingredient mirabegron. A prepared sustained-release tablet has an excellent sustained-release effect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a mirabegron sustained-release composition and its preparation method and application. Background technique [0002] Mirabegron belongs to the aryl ethanolamine β3 adrenergic receptor agonist. It acts on the β3 adrenergic receptor of the detrusor smooth muscle of the bladder to relax the bladder, promote bladder filling and increase urine storage volume, which can effectively reduce the frequency of urination and improve bladder function. Frequent urination caused by hyperactivity; the advantage of mirabegron sustained-release tablets is that it can reduce the impact of food on its absorption, can be taken before and after meals, can maintain a long-term stable effective blood drug concentration, and increase the efficacy of the drug. Only one tablet is needed a day, which is convenient to take and improves patient compliance. Therefore, it is of great signi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/22A61K31/426A61P13/10A61P13/00
CPCA61K9/2866A61K9/2054A61K31/426A61P13/10A61P13/00
Inventor 崔东冬刘保全代红娟
Owner 重庆世森医药科技有限公司
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