A medicinal composition for treating diabetic neuropathy and preparation method thereof

A prescription and uniform mixing technology, which can be used in drug combinations, nervous system diseases, pharmaceutical formulations, etc., can solve the problems of low average dissolution rate of epalrestat tablets and large differences between dissolution rate tablets, etc., so as to reduce the dissolution rate difference. Small size, improved average dissolution rate, and high stability

CN105853383BActive Publication Date: 2019-04-30SUZHOU CHUNGHWA CHEM & PHARMA IND
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2019-04-30

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Abstract

The invention relates to a medicine composition for treating diabetic neuropathy and a preparing method thereof. The medicine composition for treating diabetic neuropathy is prepared from, by weight, 30-70 parts of epalrestat, 40-70 parts of a solid carrier material, 60-100 parts of filler, 1-20 parts of a binding agent, 1-20 parts of a disintegrating agent, 0.1-5 parts of a lubricating agent, 0.5-30 parts of a film-forming material, 0.5-15 parts of a light-screening agent and 0.1-3 parts of plasticizer. Epalrestat is smashed into the solid dispersed material with the particle size D90 being 10-20 micrometers and polyethylene glycol being 4000, a proper amount of the light-screening agent titanium dioxide is added, a hot-melting extruding method is used for preparing the solid dispersed body, granulating, tabletting and coating are carried out, the average dissolution rate of epalrestat tablets is higher (larger than 95%), the difference among the dissolution rates is small (RSD is smaller than 3%), and stability is higher.
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Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an epalrestat pharmaceutical composition, a preparation method and application 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.

[0003] Since the 1970s, the study of aldose reductase (AR) inhibitors has become a new focus in the treatment of chronic complications of diabetes, especially in the field of peripheral neuropathy. Epalrestat, chemical name: 5-[(1Z,2E)-2-methyl-3-phenyl-2-propenylidene]-4-oxo-2-thio-3-thiazole Alkaneaceti...

Examples

Embodiment 1

[0061] The present embodiment epalrestat tablet, its raw material consists of:

[0062] Epalrestat 50mg, polyethylene glycol 4000 50mg, mannitol 80mg, hydroxypropyl cellulose 10mg, croscarmellose calcium 10mg, magnesium stearate 3mg, appropriate amount of water, appropriate amount of 50% ethanol aqueous solution, hydroxypropyl Methylcellulose 16.2mg, titanium dioxide 9.5mg, polyethylene glycol 1.3mg;

[0063] Its preparation method comprises the following steps:

[0064] Take the raw and auxiliary materials of the prescription amount respectively, pulverize and sieve respectively, and the particle diameter (D90) of epalrestat is 15 μ m;

[0065] Preparing the extrudate by hot-melt extrusion method at 55-70°C with the prescribed amount of epalrestat and polyethylene glycol 4000, cooled at room temperature, pulverized, and sieved to obtain mixed powder;

[0066] Mix the mixed powder with the prescribed amount of filler evenly, use the prescribed amount of hydroxypropyl cellulo...

Embodiment 2

[0070] The present embodiment epalrestat tablet, its raw material consists of:

[0071] The composition of the raw and auxiliary materials of the epalrestat tablet of this embodiment is identical with the composition of the raw and auxiliary materials of the epalrestat tablet of embodiment 1;

[0072] The difference between the raw and auxiliary material composition of the epalrestat tablet in this embodiment and the preparation method of the epalrestat tablet in Example 1 is only that the particle diameter (D90) of epalrestat is 110 μm, and all the other experimental conditions and operating steps Same as embodiment 1;

Embodiment 3

[0074] The present embodiment epalrestat tablet, its raw material consists of:

[0075] Epalrestat 50mg, polyethylene glycol 4000 55mg, titanium dioxide 4.4mg, mannitol 80mg, hydroxypropyl cellulose 10mg, cross-linked carboxymethyl calcium 10mg, magnesium stearate 3mg, appropriate amount of water, appropriate amount of 50% ethanol aqueous solution , hydroxypropyl methylcellulose 2.5mg, polyethylene glycol 0.2mg;

[0076] Its preparation method comprises the following steps:

[0077] Take the raw and auxiliary materials of the prescription amount respectively, pulverize and sieve respectively, and the particle diameter (D90) of epalrestat is 15 μ m;

[0078] Prepare the extrudate by hot-melt extrusion from the prescribed amount of epalrestat, 3 mg of titanium dioxide and polyethylene glycol 4000 at 55-70°C, cool at room temperature, pulverize, and sieve to obtain a mixed powder;

[0079] Mix the mixed powder with the prescribed amount of filler evenly, use the prescribed amou...