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: 2016-07-20
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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  • Mirabegron sustained release tablet and preparation method thereof

Examples

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Effect test

Embodiment 1

[0037] formula Amount (g) Mirabellon 180

[0038] Hydroxypropyl methylcellulose E6 70 microcrystalline cellulose 210 Sodium dodecyl sulfate 30 silica 6 Magnesium stearate 6 Polyacrylic resin NE30D (30% water dispersion) 110 Triethyl citrate 12 talcum powder 62 total 686

[0039] Preparation steps: take 180 g of Mirabegron, 70 g of hydroxypropyl methylcellulose E6 and 30 g of sodium lauryl sulfate for micronization using an airflow pulverizer, the airflow pressure is 2.0 Mpa, the feed rate is 500 g / h, and the powder is pulverized. After the end, measure the particle size, D90 is 8.9um; add the above-mentioned micronized material into the hot melt granulator KJL-100, heat it to 150°C, stir evenly, add 28g of 80°C hot water for granulation to obtain wet granules, Cool to 28°C while stirring, and the weight loss on drying is determined to be 3.4%; add microcrystalline cellulose, silicon dioxide an...

Embodiment 2

[0046] formula Amount (g) Mirabellon 240

[0047] Hypromellose 200 lactose 250 Vitamin E TPGS 30 silica 6 Magnesium stearate 6 Ethyl cellulose aqueous dispersion (30%) 100 Triethyl citrate 10 talcum powder 58 total 900

[0048] Preparation steps: take 240 g of mirabegron, 200 g of hydroxypropyl cellulose and 30 g of vitamin ETPGS for micronization using an airflow pulverizer, the airflow pressure is 2.0Mpa, the feed rate is 700g / h, and the particle size is measured after the pulverization, D90 is 8.0um; add the above micronized material into a hot melt granulator, heat it to 180°C, stir evenly, add 55g of 80°C hot water to granulate to obtain wet granules, cool to 25°C while stirring, and measure the loss on drying The value 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...

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PUM

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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 a pharmaceutical preparation, 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, and was approved by the U.S. Food and Drug Administration on June 28, 2012 for the treatment of adults with overactive bladder. The Chinese chemical name of mirabegron: (R)-2-(2-amino-1,3-thiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenethyl)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 incontinence, urge, and urinary frequency. Overactive bladder is a syndrome characterized by symptoms of urinary urgency, often accompanied by symptoms of frequent urination and nocturia, with ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/426A61K47/36A61K47/34A61P13/10
Inventor 钱晓明刘学军陈历胜
Owner SHANGHAI SUNTECH PHARMA
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