Diabetes treatment pharmaceutical composite and preparation method thereof

A composition and drug technology, applied in the field of epalrestat tablets and their preparation, can solve the problems of large differences in dissolution rate between tablets, low average dissolution rate of epalrestat tablets, etc. The effect of increasing the average dissolution rate, increasing the content and yield

CN105998012AActive Publication Date: 2016-10-12SUZHOU CHUNGHWA CHEM & PHARMA IND
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Publication Date
2016-10-12

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Abstract

The invention relates to an epalrestat tablet and a preparation method and application thereof. The epalrestat medicine composite comprises the following raw materials and auxiliary materials: 30-70 parts by weight of epalrestat, 30-70 parts by weight of filler, 5-25 parts by weight of binder, 1-10 parts by weight of surfactant, 1-10 parts by weight of disintegrant, 0.1-5 parts by weight of lubricant, 1-30 parts by weight of film-forming material, 1-10 parts by weight of sunscreen and 1-3 parts by weight of plasticizer. The epalrestat tablet prepared from the preparation method has a high average dissolution rate (more than 95%), the inter-tablet difference of the dissolution rate is small (RSD (Relative Standard Deviation) is smaller than 3%), and quality is obviously improved. The preparation method obviously reduces mixed powder residues on a fluidized bed pot wall and a drum bag, improves the contents and the yield of the epalrestat in particles, improves the average dissolution rate of the prepared epalrestat tablet and lowers the inter-tablet difference of the dissolution rate.
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Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an epalrestat tablet and 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 Alkaneacetic acid, a reversi...

Examples

Embodiment 1

[0053] The present embodiment epalrestat tablet, its raw material consists of:

[0054] Epalrestat 50mg, Mannitol 50mg, Hydroxypropylcellulose 5mg, Poloxamer 1883mg, Cross-linked carboxymethyl calcium 6mg, Magnesium stearate 1mg, Appropriate amount of water, Appropriate amount of 50% ethanol aqueous solution, Hypromellose Base cellulose 9mg, titanium dioxide 5.3mg, polyethylene glycol 0.7mg;

[0055] Its preparation method comprises the following steps:

[0056] Take the raw and auxiliary materials of the prescription amount respectively, pulverize and sieve respectively, and the particle diameter (D90) of epalrestat is 15 μm;

[0057] Add the prescribed amount of hydroxypropyl cellulose and the prescribed amount of poloxamer 188 to an appropriate amount of water, and stir until dissolved to obtain a solution;

[0058] The epalrestat of the prescribed amount and the mannitol of the prescribed amount are granulated by the fluidized bed granulation method with the solution, dr...

Embodiment 2

[0062] The present embodiment epalrestat tablet, its raw material consists of:

[0063] Epalrestat 50mg, Mannitol 44mg, Hydroxypropylcellulose 5mg, Poloxamer 1889mg, Cross-linked carboxymethylcalcium 6mg, Magnesium stearate 1mg, Appropriate amount of water, Appropriate amount of 50% ethanol aqueous solution, Hypromellose Base cellulose 9mg, titanium dioxide 5.3mg, polyethylene glycol 0.7mg;

[0064] Its preparation method comprises the following steps:

[0065] 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;

[0066] Add the prescribed amount of hydroxypropyl cellulose and the prescribed amount of poloxamer 188 to an appropriate amount of water, and stir until dissolved to obtain a solution;

[0067] The epalrestat of the prescribed amount and the mannitol of the prescribed amount are granulated by the fluidized bed granulation method with the solution, dr...

Embodiment 3

[0071] The present embodiment epalrestat tablet, its raw material consists of:

[0072] Epalrestat 50mg, Mannitol 48mg, Hydroxypropylcellulose 5mg, Poloxamer 1885mg, Cross-linked carboxymethylcalcium 6mg, Magnesium stearate 1mg, Appropriate amount of water, Appropriate amount of 50% ethanol aqueous solution, Hypromellose Base cellulose 9mg, titanium dioxide 5.3mg, polyethylene glycol 0.7mg;

[0073] Its preparation method comprises the following steps:

[0074] 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;

[0075] Add the prescribed amount of hydroxypropyl cellulose and the prescribed amount of poloxamer 188 to an appropriate amount of water, and stir until dissolved to obtain a solution;

[0076] The epalrestat of the prescribed amount and the mannitol of the prescribed amount are granulated by fluidized bed granulation in the solution, dried, and gran...