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Epalrestat enteric-coated and sustained-release tablets and preparation method thereof

A technology of epalrestat and sustained-release tablets, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., which can solve unfavorable industrial production, too fast alkali release, and uneven release and other problems, to achieve the effects of easy scale-up production, slow release, and excellent sustained-release effect

Active Publication Date: 2015-09-30
YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] WO2012100208A1 discloses an epalrestat sustained-release preparation. According to the results determined by the inventors, the drug prepared by this method has a dissolution phenomenon under acidic conditions, and the release is too fast and uneven in alkali; the method uses There are many kinds of auxiliary materials and the process is complicated, which is not conducive to industrial production

Method used

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  • Epalrestat enteric-coated and sustained-release tablets and preparation method thereof
  • Epalrestat enteric-coated and sustained-release tablets and preparation method thereof
  • Epalrestat enteric-coated and sustained-release tablets and preparation method thereof

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Embodiment 1

[0039] Patent WO2012100208A1 provides a preparation of epalrestat sustained-release tablets (150mg / tablet, a total of 1000 tablets)

[0040] Inner granular material:

[0041]

[0042] Prelubrication:

[0043] Colloidal silica 2.5

[0044] Talc 2.5

[0045] lubricating:

[0046] Hydrogenated vegetable oil 6g

[0047] Preparation method: Weigh the prescription amount of API, mannitol, hypromellose and sodium alginate and put them into a three-dimensional motion mixer and mix them for 10 minutes; put the mixed powder into a wet granulator, and use purified water to make soft materials. Use swinging granules to granulate with a 16-mesh sieve; put the wet granules on a tray and dry in a blast drying oven at 50°C for 90 minutes; pass the dry granules through a 30-mesh sieve for granulation; put the dry granules into three-dimensional motion mixing The prescription amount of colloidal silicon dioxide and talcum powder is added to the machine for pre-lubrication; the prescript...

Embodiment 2

[0056] Preparation of epalrestat enteric-coated sustained-release tablets (150mg / tablet, 1000 tablets in total)

[0057] Single-layer core:

[0058]

[0059]

[0060] Slow-release coating:

[0061]

[0062] Preparation method: pulverize epalrestat, hydroxypropyl methylcellulose (added in K4M), lactose, and povidone (K30), pass through a 100-mesh sieve, mix mechanically, add an appropriate amount of purified water during stirring, and granulate , drying, whole grain. Then add hydroxypropyl methylcellulose (K4M extra) and magnesium stearate to the dry granules after the above-mentioned granulation, place in a granulator and mix evenly, control the hardness of the tablet at 14-16Kg, and press the tablet to obtain Single layer core. Disperse 7.5g of talcum powder in 63g of purified water and stir evenly, then add 1.5g of triethyl citrate and 0.5g of yellow iron oxide and continue to stir evenly. Add the above suspension to 50g For L 30D-55, coat after stirring evenl...

Embodiment 3

[0064] Preparation of epalrestat enteric-coated sustained-release tablets (150mg / tablet, 1000 tablets in total)

[0065] Single-layer core:

[0066]

[0067] Slow-release coating:

[0068]

[0069] Preparation method: pulverize epalrestat, hydroxypropyl methylcellulose (added in K4M), lactose, and povidone (K30), pass through a 100-mesh sieve, mix mechanically, and add 5% povidone during stirring (K30) Appropriate amount of aqueous solution, granulate, dry, and granulate. Then add hydroxypropyl methylcellulose (K4M extra) and magnesium stearate to the dry granules after the above-mentioned granulation, place in a granulator and mix evenly, control the hardness of the tablet at 14-16Kg, and press the tablet to obtain Single layer core. Disperse 7.5g of talcum powder in 63g of purified water and stir evenly, then add 1.5g of triethyl citrate and 0.5g of yellow iron oxide and continue to stir evenly. Add the above suspension to 50g For L 30D-55, coat after stirring ev...

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Abstract

The invention discloses an epalrestat enteric-coated and sustained-release preparation and a preparation method thereof. The preparation comprises epalrestat or pharmaceutically acceptable salts of epalrestat, single-layer tablet cores of a sustained-release framework material and an enteric coating. The invention further provides a preparation method of epalrestat enteric-coated and sustained-release tablets. The Epalrestat enteric-coated and sustained-release tablets are simple in production process and stable in quality; compared with the common epalrestat preparation, the Epalrestat enteric-coated and sustained-release tablets provided by the invention have the advantages that drug release can be more smoothly and slowly achieved after oral administration, in-vivo drug release can be smoother and more consistent, and the therapeutic effect can be kept for a longer time.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to epalrestat enteric-coated sustained-release tablets and a preparation method thereof. Background technique [0002] Epalrestat (epalrestat) is a drug that specifically acts on the polyol pathway and is mainly used to treat chronic complications of diabetes. Diabetic peripheral neuropathy (DPN) is one of the most common and complex chronic complications of diabetes, and is the main reason for repeated hospitalization of diabetic patients. At present, there are many drugs for the treatment of DPN. The classic drug methylcobalamin improves peripheral nerve symptoms by repairing nerve tissue, promoting axon regeneration and myelination. The representative drug of aldose reductase inhibitors, epalrestat, reversibly inhibits the activity of aldose reductase and reduces the production of carboxymethyllysine in diabetic patients, thereby treating DPN. [0003] The chemical na...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/426A61K47/38A61K47/36A61K47/32A61P3/10
Inventor 吴小涛宋先宏何红艳束志凌邓飞黄丁菲刘淑敏
Owner YANGTZE RIVER PHARM GRP NANJING HAILING PHARM CO LTD
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