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Epalrestat slow-release tablet and preparation method thereof

A technology of epalrestat and sustained-release tablets, which is applied in the field of sustained-release preparations and its preparation, can solve the problems of short half-life and poor patient compliance, and achieve the effects of convenient taking, easy operation, good clinical significance and commercial significance

Inactive Publication Date: 2012-05-09
NANJING HAILING TRADITIONAL CHINESE MEDICINE RES CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Epalrestat is well absorbed orally, with a tmax (peak time) of about 2 hours, but a short half-life, and the elimination half-life t1 / 2β is only 1 hour
The common epalrestat tablet currently available on the market must be taken three times a day to inhibit the polyol pathway for a long time, and the patient's compliance is poor

Method used

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  • Epalrestat slow-release tablet and preparation method thereof
  • Epalrestat slow-release tablet and preparation method thereof
  • Epalrestat slow-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation of Epalrestat Sustained Release Tablet 1 (25mg / tablet, 1000 tablets in total)

[0041] Epalrestat 25g

[0042] Hydroxypropyl methylcellulose (K4M) 50g

[0043] Hydroxypropyl methylcellulose (K100) 20g

[0044] Lactose 652g

[0045] Magnesium Stearate 3g

[0046] Preparation method: crush epalrestat, hydroxypropyl methylcellulose (K4M), hydroxypropyl methylcellulose (K100), lactose, pass through a 100-mesh sieve, mix mechanically, and add 3% polyvinyl chloride into the stirring An appropriate amount of 95% ethanol solution of ketone (K30), granulated, dried, and granulated. Add magnesium stearate to the above-mentioned dry granules after granulation, place in a granulator and mix evenly, control the hardness of the tablet at 7-8Kg, and tablet to obtain. A total of 1000 tablets were produced.

[0047]

Embodiment 2

[0049] Preparation of Epalrestat Sustained Release Tablet 1 (50mg / tablet, 1000 tablets in total)

[0050] Epalrestat 50g

[0051] Hydroxypropyl methylcellulose (K4M) 50g

[0052] Hydroxypropyl methylcellulose (K100) 50g

[0053] Lactose 547g

[0054] Magnesium Stearate 3g

[0055] Preparation method: crush epalrestat, hydroxypropyl methylcellulose (K4M), hydroxypropyl methylcellulose (K100), lactose, pass through a 100-mesh sieve, mix mechanically, and add 3% polyvinyl chloride into the stirring An appropriate amount of 95% ethanol solution of ketone (K30), granulated, dried, and granulated. Add magnesium stearate to the above-mentioned dry granules after granulation, place in a granulator and mix evenly, control the hardness of the tablet at 7-8Kg, and tablet to obtain. A total of 1000 tablets were produced.

[0056]

Embodiment 3

[0058]Preparation of Epalrestat Sustained Release Tablet 2 (75mg / tablet, 1000 tablets in total)

[0059] Epalrestat 75g

[0060] Hydroxypropyl methylcellulose (K4M) 50g

[0061] Ethyl cellulose (N20) 50g

[0062] Lactose 522g

[0063] Magnesium Stearate 3g

[0064] Preparation method: Grind epalrestat, hydroxypropylmethylcellulose (K4M), ethylcellulose (N20), lactose, pass through a 100-mesh sieve, mix mechanically, add 3% povidone (K30 ) in an appropriate amount of 95% ethanol solution, granulated, dried, and granulated. Add magnesium stearate to the above-mentioned dry granules after granulation, place in a granulator and mix evenly, control the hardness of the tablet at 7-8Kg, and tablet to obtain. A total of 1000 tablets were produced.

[0065]

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Abstract

The invention provides an epalrestat slow-release tablet and a preparation method thereof. The slow-release tablet is prepared from the following components in parts by weight: 1-40 parts of epalrestat, 5-60 parts of slow-release material, 0-90 parts of filler, 0.1-2 parts of lubricant and right amount of adhesive. The slow-release material comprises hydroxypropyl methylcellulose or a mixture of hydroxypropyl methylcellulose and ethyl cellulose. The preparation method comprises the following steps: evenly mixing the epalrestat, slow-release material and filler according to the prescription amounts, adding the adhesive to obtain a soft material, granulating the soft material, drying, finishing, adding the lubricant, and tabletting. Compared with the conventional oral epalrestat common preparation, the epalrestat slow-release tablet provided by the invention can smoothly and slowly release the medicines after being orally dosed, and can maintain therapeutic action for a longer time.

Description

technical field [0001] The invention relates to a sustained-release preparation for treating diabetic complications and a preparation method thereof, in particular to an epalrestat sustained-release tablet and a preparation method thereof. Background technique [0002] In recent years, with the improvement of people's daily life and the increase of life pressure, the prevalence of diabetes has risen sharply. Diabetes can cause many chronic complications if it is not diagnosed and treated in time. According to statistics, more than 1 / 2 of diabetic patients are complicated with vascular and neuropathy, about 30% are complicated with proliferative retinopathy, and 1-2% of them may develop into blindness. One of the causes of diabetic complications is abnormal osmotic pressure caused by hyperactivity of polyol metabolism. polyol pathway ( figure 1 shown) is jointly regulated by aldose reductase (AR) and sorbitol dehydrogenase (SDH). AR uses reduced coenzyme II (NADPH) as a c...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/426A61K47/32A61K47/36A61K47/38A61P3/10
Inventor 王宇李琴张明明卓敏潘睿睿
Owner NANJING HAILING TRADITIONAL CHINESE MEDICINE RES CO LTD
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