Mirabegron sustained-release pharmaceutical composition

A technology for mirabegron and sustained-release tablets, which is applied in the field of pharmaceutical preparations, can solve the problems of high price of polyethylene oxide and increase the cost of pharmaceutical manufacturing, and achieves the guarantee of drug efficacy and safety, excellent release duration, and guaranteed The effect of medication safety

Active Publication Date: 2017-05-03
深圳万乐药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The Mirabegron sustained-release tablets that have been on the market have adopted a hydrophilic gel matrix sustained-release means, and the adopted matrix material is polyethylene oxide (PEO). The disadvantage of using this matrix material is that PEO is due to the presence of A large number of ether bonds, so it is easy to be degraded by oxygen attack, high temperature, some heavy metal ions, oxidants and ultraviolet rays will accelerate the process of its oxidative degradation, so it is necessary to add antioxidant BHT (2,6-di tert-butyl p-cresol), and polyethylene oxide is more expensive, which increases the cost of drug manufacturing

Method used

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  • Mirabegron sustained-release pharmaceutical composition
  • Mirabegron sustained-release pharmaceutical composition
  • Mirabegron sustained-release pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] prescription composition

[0023]

[0024]

[0025] The total HPMC viscosity (20°C, 2% aqueous solution) of the skeleton material in the prescription is 120mPa·S.

[0026] Preparation:

[0027] With 1000g mirabegron crude drug, 330g HPMC K4MCR , 1670g HPMC K100LV Add 960g PEG6000 and 790g lactose into the fluidized bed granulator, granulate with 200g 10% HPC-SL aqueous solution, after granulation, add 25g magnesium stearate and 25g micropowder silica gel, press with rotary tablet press Tablets to obtain Mirabegron sustained-release tablets with a tablet weight of 250 mg.

[0028] Dissolution test:

[0029] Dissolution test was carried out to the prepared Mirabegron sustained-release tablets according to USP dissolution test method (basket method). Use 900mL of pH 6.8 phosphate buffer as the release medium, and use UV to measure the cumulative release at 2h, 4h, and 8h. The results are as follows:

[0030] time 2h 4h 8h cumulative release (...

Embodiment 2

[0040] prescription form

[0041]

[0042] The total HPMC viscosity (20°C, 2% aqueous solution) of the skeleton material in the prescription is 115mPa·S.

[0043] Preparation:

[0044] With 1000g mirabegron crude drug, 330g HPMC K4MCR 、HPMC K100LV 1670, 960g polyethylene glycol and 790g lactose were added to the fluidized bed granulator, granulated with 200g 10% HPC-SL aqueous solution, after granulation, 25g magnesium stearate and 25g micropowder silica gel were added, and the Tablet machine carries out tabletting, adopts high-efficiency coating machine to the prepared tablet, sprays the aqueous dispersion of coating film coating agent (Opadry 03F22733), obtains the Mirabegron sustained-release tablet of tablet weight 257.5mg.

Embodiment 3

[0046] prescription form

[0047]

[0048]

[0049] The total HPMC viscosity (20°C, 2% aqueous solution) of the skeleton material in the prescription is 85mPa·S.

[0050] Preparation:

[0051] With 100g mirabegron bulk drug, HPMC K4MCR 38g, HPMC K100LV 187g, PEG6000155g, placed in a mixing granulator to disperse evenly, adding 15g of 10% hydroxypropyl cellulose aqueous solution for granulation, after granulation, adding 5g of magnesium stearate and fully mixing, using a rotary tablet press for tableting, Obtain the mirabegron sustained-release tablet of tablet weight 250mg.

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PUM

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Abstract

The invention provides a mirabegron sustained-release tablet. The core of the sustained-release tablet is made of hydroxypropyl methyl cellulose serving as a framework material; the mirabegron sustained-release tablet can be continuously released for 8 hours after being orally taken by a human body, and the release amount is not smaller than 90%; and no antioxidants are adopted, so that the pharmacological function and the safety are ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a slow-release pharmaceutical composition of mirabegron, an active drug for treating overactive bladder, and a preparation method thereof. Background technique [0002] Mirabegron (mirabegron) tablets were developed by Japan's Astellas Pharmaceutical Company and were launched in Japan on September 16, 2011, and approved by the U.S. Food and Drug Administration (FDA) on June 28, 2012 For the treatment of overactive bladder (OAB) in adults, the trade name is Myrbetriq. The molecular formula of mirabegron is C 21 h 24 N 4 o 2 S, molecular weight 396, chemical name is (R)-2-(2-amino-1,3-thiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino] Ethyl] phenylacetamide, its structural formula is as follows: [0003] [0004] Mirabegron belongs to the class of aryl ethanolamines beta 3 Receptor agonist, acts on bladder detrusor smooth muscle beta 3 Adrenaline ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/28A61K31/426A61K47/38A61K47/10A61K47/26A61P13/10
Inventor 汤晨懿柏江涛张海龙李骞陈博
Owner 深圳万乐药业有限公司
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