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A kind of Mirabegron sustained-release tablet and preparation method thereof

A technology of mirabegron and sustained-release tablets, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, and medical preparations containing active ingredients. Incomplete release and other problems, to achieve convenient clinical use, good clinical application prospects, and increase the effect of compliance

Active Publication Date: 2019-04-26
SHANGHAI SUNTECH PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Osmotic pump preparations have small intra-individual differences and are not affected by food, but the process is relatively complicated, the release is often incomplete, and the production process is difficult to control
However, the price of products prepared by osmotic pump technology is too high, and the technology is very difficult, difficult to control, and the shell of the prepared product cannot be metabolized, and will be excreted in the prototype, which has an impact on the patient's psychological state
Therefore, relatively speaking, the product prepared by the membrane control technology is stable and less affected by food in the body, but the membrane control agent requires good water solubility of raw materials, and the water solubility of mirabegron is extremely poor. Membrane control agent is very difficult, therefore, it is necessary to study the difficulty of the preparation of its membrane control agent

Method used

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  • A kind of Mirabegron sustained-release tablet and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

total

686

[0039] Preparation steps: take 180g mirabegron, 70g hydroxypropyl methylcellulose E6 and 30g sodium lauryl sulfate and carry out micronization with an airflow mill, the airflow pressure is 2.0Mpa, the feed rate is 500g / h, pulverize After measuring the particle size, the D90 is 8.9um; put the above micronized material into the hot melt granulator KJL-100, heat to 150°C, stir evenly, add 28g of 80°C hot water to granulate, and make wet granules. Cool to 28°C while stirring, and determine that the weight loss on drying is 3.4%; add microcrystalline cellulose, silicon dioxide and magnesium stearate, stir for 5 minutes, and mix well to obtain the final mixture before tableting; use Fette to tablet Machine 102i compresses the mixture into tablets to obtain 6,000 Mirabegron tablets; coats the aqueous dispersion prepared from polyacrylic acid resin NE30D, triethyl citrate and talcum powder to obtain sustained-release tablets. The tablet after coating was aged ...

Embodiment 2

total

900

[0048] Preparation steps: take 240g mirabegron, 200g hydroxypropyl cellulose and 30g vitamin E TPGS and use a jet mill to micronize, the air pressure is 2.0Mpa, the feed rate is 700g / h, and the particle size is measured after the pulverization, D90 8.0um; put the above micronized material into a hot-melt granulator, heat to 180°C, stir evenly, add 55g of 80°C hot water to granulate, and make wet granules, cool to 25°C while stirring, measure the dryness The weight loss is 2.4%; add lactose, silicon dioxide and magnesium stearate, stir for 10 minutes, and mix well to obtain the final mixture before tableting; use the Fette tablet machine to compress the mixture to obtain Mirabegron tablets 6000 tablets; sustained-release tablets are prepared by coating an aqueous dispersion prepared from ethyl cellulose, triethyl citrate and talcum powder. The coated tablet was aged at 40°C for 48 hours to obtain the final Mirabegron sustained-release tablet.

[0049] ...

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Abstract

The invention provides a mirabegron sustained release tablet. The sustained release tablet is characterized by consisting of the following components in percentage by weight (as shown in description). The invention can overcome shortcomings of the prior art; the mirabegron can slowly release and absorb in vivo, so that a stable blood concentration is kept and patient's compliance is enhanced, and the sustained release tablet is good in clinical application prospect. The preparation method disclosed by the invention is simple and convenient, applicable to industrial production and is relatively high in practical value.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a mirabegron sustained-release tablet and a preparation method thereof. Background technique [0002] Mirabegron was developed by Japan's Astellas Pharmaceuticals and was launched in Japan on September 16, 2011. It was approved by the US Food and Drug Administration on June 28, 2012 for the treatment of overactive bladder in adults. Chinese chemical name of mirabegron: (R)-2-(2-amino-1,3-thiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino ] Ethyl] phenylacetamide, molecular formula: C 21 h 24 N 4 o 2 S, molecular weight: 396, CA registration number: 223673-61-8. [0003] Mirabegron is a beta-adrenergic agonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Overactive bladder is a syndrome characterized by symptoms of urinary urgency, often accompanied by frequency and nocturia, with or without urge ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/426A61K47/36A61K47/10A61P13/10
Inventor 钱晓明刘学军陈历胜
Owner SHANGHAI SUNTECH PHARMA
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