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Compound sustained-release tablet of epalrestat and sitagliptin or pharmaceutically acceptable salt thereof and preparation method thereof

A technology of compound sustained-release tablets and epalrestat, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Active Publication Date: 2022-01-14
乐普制药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And there are no products or related reports on the market that make the pharmaceutical composition of epalrestat and sitagliptin or a pharmaceutically acceptable salt thereof into compound sustained-release tablets

Method used

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  • Compound sustained-release tablet of epalrestat and sitagliptin or pharmaceutically acceptable salt thereof and preparation method thereof
  • Compound sustained-release tablet of epalrestat and sitagliptin or pharmaceutically acceptable salt thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Epalrestat, sitagliptin film-controlled matrix sustained-release single-layer tablet (1000 tablets)

[0041] (1) Chip part

[0042] Epalrestat 75g, sitagliptin phosphate 50g, calcium hydrogen phosphate anhydrous 45g, mannitol 80g, hydroxypropyl methylcellulose 60g, hydroxypropyl cellulose 6g, croscarmellose sodium 5g, Colloidal silicon dioxide 2g, sodium stearyl fumarate 5g, magnesium stearate 2g;

[0043] (2) Membrane-controlled slow-release coating part

[0044] Ethyl cellulose 18g, hypromellose 5g, diethyl phthalate 2g, titanium dioxide 5g

[0045] Preparation method:

[0046](1) Pretreatment of raw materials and auxiliary materials: Pass epalrestat, sitagliptin or their pharmaceutically acceptable salt raw materials through a 100-mesh sieve, and pass fillers and other auxiliary materials through a 60-mesh sieve.

[0047] (2) Wet granulation: Weigh raw materials and mix them evenly with auxiliary materials other than hydroxypropyl cellulose, glidant...

Embodiment 2

[0051] Embodiment 2: Epalrestat, sitagliptin film-controlled matrix sustained-release single-layer tablet (1000 tablets)

[0052] (1) Chip part

[0053] Epalrestat 75g, sitagliptin 50g, calcium hydrogen phosphate anhydrous 50g, microcrystalline cellulose 52g, mannitol 35g, carboxymethyl cellulose 60g, hydroxypropyl methyl cellulose 5g, croscarmellose Sodium cellulose 6g, colloidal silicon dioxide 2g, sodium stearyl fumarate 4g, magnesium stearate 2g;

[0054] (2) Membrane controlled release coating material

[0055] Cellulose acetate 14g, hypromellose 9g, polyoxyethylene polyoxypropylene glycol 2g, titanium dioxide 5g.

[0056] Preparation method: consistent with the preparation method in Example 1, the core part of the tablet is changed from the hydroxypropyl cellulose aqueous solution in Example 1 as binder granulation to mixed granulation with purified water as wetting agent.

Embodiment 3

[0057] Embodiment 3: Epalrestat, sitagliptin film-controlled matrix sustained-release double-layer tablet (1000 tablets)

[0058] (1) Chip part

[0059] Epalrestat sustained-release layer: 75g of epalrestat, 42g of mannitol, 12g of lactose, 35g of hydroxypropyl methylcellulose, 4g of carboxymethylcellulose calcium, 2g of magnesium stearate;

[0060] Sitagliptin or its pharmaceutically acceptable salt immediate-release layer: 50g of sitagliptin phosphate, 50g of anhydrous calcium hydrogen phosphate, 40g of mannitol, 3g of croscarmellose sodium, 5g of sodium stearyl fumarate, Magnesium stearate 2g;

[0061] (2) Membrane-controlled slow-release coating part

[0062] Eudragit RS 14g, Eudragit RL 4g, polyethylene glycol 4g, diethyl phthalate 3g, titanium dioxide 5g.

[0063] Preparation method:

[0064] (1) Pretreatment of raw materials and auxiliary materials: Pass epalrestat, sitagliptin or their pharmaceutically acceptable salt raw materials through a 100-mesh sieve, and pas...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a compound sustained-release tablet of epalrestat and sitagliptin or pharmaceutically acceptable salt thereof and a preparation method thereof. The compound sustained-release tablet contains epalrestat, sitagliptin or pharmaceutically acceptable salt thereof and / or hydrate of the salt, anhydrous calcium hydrophosphate, a framework sustained-release material and other pharmaceutical excipients. The compound sustained-release tablet can be a single-layer tablet or a double-layer tablet, and is used for treating type 2 diabetes, especially peripheral neuropathy caused by the type 2 diabetes. The compound composition is prepared into the sustained-release tablet, so that the synergistic interaction time of the two active ingredients can be exerted and prolonged, the stimulation effect of the medicine on gastrointestinal tracts can be reduced, the compliance of patients can be improved, the peak valley phenomenon of a common preparation in blood after the common preparation is taken is avoided, the occurrence of adverse reactions is reduced, and the medication safety is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a compound sustained-release tablet of epalrestat and sitagliptin or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] Epalrestat is an aldose reductase inhibitor, mainly used in the treatment of diabetes and its complications. Epalrestat has an absolute therapeutic effect on neuropathy induced by diabetes, and at the same time it can treat diabetic nephropathy, diabetic cardiomyopathy, diabetic retinopathy, diabetic gastroparesis, cataract, foot ulcer, diabetic macroangiopathy, diabetic microangiopathy, Complications such as hyperglycemia and hyperglycated hemoglobin levels are treatable. [0003] Sitagliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor that increases active incretin, C-peptide levels, and decreases glucagon levels by reducing glucose production and increasing tissue response to blo...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/24A61K47/02A61K47/38A61K47/36A61K47/32A61K47/14A61K47/10A61K9/36A61K31/426A61K31/4985A61P3/10A61P25/02
CPCA61K9/2095A61K9/2009A61K9/2054A61K9/209A61K9/2059A61K9/2027A61K9/2866A61K9/282A61K9/2813A61K9/2853A61K31/426A61K31/4985A61P3/10A61P25/02A61K2300/00
Inventor 潘裕生肖新新陈岑波李浩王海翔
Owner 乐普制药科技有限公司
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