Sitagliptin phosphate pharmaceutical preparation and preparation method thereof

A sitagliptin phosphate and pharmaceutical preparation technology, which is applied in the field of sitagliptin phosphate pharmaceutical preparations and preparations, can solve the problems of complex preparation process and poor compressibility of materials, and achieve good dissolution rate and good high temperature stability.

Pending Publication Date: 2022-07-05
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Aiming at the defects of the prior art, the present invention provides a sitagliptin phosphate pharmaceutical preparation and a preparation method thereof, which overcomes the problems of complex preparation process of the sitagliptin phosphate pharmaceu

Method used

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  • Sitagliptin phosphate pharmaceutical preparation and preparation method thereof
  • Sitagliptin phosphate pharmaceutical preparation and preparation method thereof
  • Sitagliptin phosphate pharmaceutical preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prescription composition: the following components are the content of 1500 tablets.

[0030]

[0031] Preparation:

[0032] 1. Total mixing: Add microcrystalline cellulose, magnesium aluminum silicate (viscosity: 400 mPa·s) and sitagliptin phosphate monohydrate into the mixer and mix evenly, and then add sodium stearyl fumarate to the above mixture. The latter material is mixed uniformly, and stearic acid is added and mixed uniformly to obtain a mixture.

[0033] 2. Tablet compression: directly tablet the above mixture, the tableting process is smooth, the surface is smooth and clean, and there is no sticking phenomenon.

Embodiment 2

[0035] Prescription composition: the following components are the content of 1500 tablets.

[0036]

[0037] Preparation:

[0038] 1. Mixing: Add microcrystalline cellulose, anhydrous calcium hydrogen phosphate, magnesium aluminum silicate (viscosity 250mPa s) and sitagliptin phosphate monohydrate into the mixer and mix evenly, and then add stearyl fumarate. Magnesium acid is added to the above-mentioned mixed materials and mixed uniformly, and magnesium stearate is added and mixed uniformly to obtain a mixture.

[0039] 2. Tablet compression: directly tablet the above mixture, the tableting process is smooth, the surface is smooth and clean, and there is no sticking phenomenon.

Embodiment 3

[0041] Prescription composition: the following components are the content of 1500 tablets.

[0042]

[0043] Preparation:

[0044] 1. Mixing: Add microcrystalline cellulose, anhydrous calcium hydrogen phosphate, magnesium aluminum silicate (viscosity 400mPa s) and sitagliptin phosphate monohydrate into the mixer and mix evenly, and then add stearyl fumarate. Magnesium acid is added to the above-mentioned mixed materials and mixed uniformly, and magnesium stearate is added and mixed uniformly to obtain a mixture.

[0045] 2. Tablet compression: directly tablet the above mixture, the tableting process is smooth, the surface is smooth and clean, and there is no sticking phenomenon.

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Abstract

The invention provides a sitagliptin phosphate pharmaceutical preparation and a preparation method thereof. The sitagliptin phosphate pharmaceutical preparation comprises the following components in percentage by weight: 20-40% of sitagliptin phosphate monohydrate, 50-70% of a filler, 1-5% of a disintegrating agent, 0.5-2% of a hydrophobic lubricant and 1-4% of a hydrophilic lubricant, wherein the disintegrating agent is selected from one of magnesium aluminum silicate, magnesium aluminum metasilicate and silicon dioxide. According to the sitagliptin phosphate pharmaceutical preparation disclosed by the invention, the problems of complex preparation process, poor material compressibility and poor raw material stability of the sitagliptin phosphate pharmaceutical preparation are solved, and the sitagliptin phosphate pharmaceutical preparation which is simple in preparation process, good in material compressibility, stable in raw material and high in release speed is obtained.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a sitagliptin phosphate pharmaceutical preparation and a preparation method. Background technique [0002] Sitagliptin phosphate is a potent and highly selective inhibitor of dipeptidyl peptidase IV (DPP-IV) in patients with type 2 diabetes by increasing the activity of the incretin hormone glucagon-like polypeptide-1 (GLP-1) and glucose-dependent insulin secretion-stimulating polypeptide (GIP) levels to improve glycemic control. In 2006, Merck developed sitagliptin phosphate tablets, which can be clinically used alone or combined with other oral hypoglycemic drugs (such as metformin or thiazolidinediones) to treat type 2 diabetes. [0003] Sitagliptin (Sitagliptin, CAS No.486460-32-6), chemical name: (3R)-3-amino-1-[3-(trifluoromethyl)-5,6,7,8-tetra Hydrogen-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one, its structural formula is a...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/02A61K47/04A61K47/12A61K47/38A61K9/28A61K31/4985A61P3/10
CPCA61K9/2009A61K9/2095A61K9/2806A61K9/2013A61K9/2054A61K31/4985A61P3/10
Inventor 黄玉锋杨文涛彭小玲吕海东产运霞耿玉先
Owner BEIJING WINSUNNY PHARMA CO LTD
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