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Luseogliflozin pharmaceutical composition, and preparation method thereof

A composition and medicine technology, applied in the field of lupagliflozin pharmaceutical composition and preparation thereof, can solve the problems of low melting point of medicine, large specific surface area of ​​medicine, low density of medicine and the like

Inactive Publication Date: 2017-05-03
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The study found that before making rupagliflozin into a preparation, if the raw material is micronized to reduce the particle size, but due to the low melting point of the drug, it is easy to produce "sticky phenomenon", and subsequent crushing is difficult; if the particle size of the drug can be controlled at In a small range, due to the large specific surface area of ​​the drug and the low density of the drug, it is easy to float. When using 4-8% hydroxypropyl cellulose aqueous solution for wet granulation, uneven mixing is likely to occur, causing the drug to aggregate into balls. The particle size increases, resulting in low dissolution rate of prepared tablets or large discrepancies between tablets

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Prescription Composition of Luxagliflozin Tablets

[0020] Luxagliflozin 100g

[0021] Povidone 50g

[0022] Lactose 50g

[0023] Magnesium Stearate 5g

[0024] Preparation:

[0025] Step (1): Take 100g of Luxagliflozin, add 1500g of ethanol, stir to dissolve or disperse evenly, and use it as solution A for later use.

[0026] Step (2): Take 50g of povidone (K30) and 50g of lactose, add 500g of purified water, stir to dissolve, and make solution B.

[0027] Step (3): Add solution A to solution B, stir to make it evenly dispersed, and use it as solution C.

[0028] Step (4): Solution C is spray-dried in a spray dryer, and the temperature of the spray-drying is controlled to be 100°C; the spray-dried material is collected, passed through a 60-mesh sieve, added with an appropriate amount of lubricant, and compressed into tablets to obtain Delupagliflozin Tablets .

Embodiment 2

[0030] Prescription Composition of Luxagliflozin Tablets

[0031] Luxagliflozin 100g

[0032] Low-substituted hydroxypropyl cellulose 50g

[0033] Mannitol 150g

[0034] Magnesium Stearate 5g

[0035] Preparation

[0036] Step (1): Take 100g of Luxagliflozin, add 700g of acetone, stir to dissolve or disperse evenly, and use it as solution A for later use.

[0037] Step (2): Take 50 g of low-substituted hydroxypropyl cellulose and 150 g of mannitol, add 1000 g of purified water, stir, and dissolve them as solution B.

[0038] Step (3): Add solution A to solution B, stir to make it evenly dispersed, and use it as solution C.

[0039] Step (4): Solution C is spray-dried in a spray dryer, and the temperature of the spray-drying is controlled to be 115°C; the spray-dried material is collected, passed through a 60-mesh sieve, added with an appropriate amount of lubricant, and compressed into tablets to obtain Delupagliflozin Tablets .

Embodiment 3

[0041] Prescription Composition of Luxagliflozin Tablets

[0042] Luxagliflozin 100g

[0043] Low-substituted hydroxypropyl cellulose 50g

[0044] Xylitol 100g

[0045] Magnesium Stearate 5g

[0046] Preparation

[0047] Step (1): Take 100g of Luxagliflozin, add 1500g of ethanol-isopropanol solution (2:8, w / w), stir to dissolve or disperse evenly, and use it as solution A for later use.

[0048] Step (2): Take 50 g of low-substituted hydroxypropyl cellulose and 100 g of xylitol, add 800 g of aqueous solution, stir to dissolve, and make solution B.

[0049] Step (3): Add solution A to solution B, stir to make it evenly dispersed, and use it as solution C.

[0050] Step (4): Solution C is spray-dried in a spray dryer, and the temperature of the spray-drying is controlled to be 105°C; the spray-dried material is collected, passed through a 60-mesh sieve, added with an appropriate amount of lubricant, and compressed into tablets to obtain Delupagliflozin Tablets .

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PUM

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Abstract

The invention discloses a luseogliflozin pharmaceutical composition, and a preparation method thereof. The luseogliflozin pharmaceutical composition contains luseogliflozin, a disintegrating agent, and a filling agent at a mass ratio of 10:1-10:1-20, and preferably 10:(5-10):(10-15). The luseogliflozin pharmaceutical composition is high in fluidity and compressibility, less dust is generated, and problems of low dissolution rate and poor bioavailability caused by poor water solubility of luseogliflozin are solved.

Description

technical field [0001] The invention relates to a rupagliflozin pharmaceutical composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] SLGT2 inhibitor is a drug that can specifically inhibit glomerular proximal tubules to reabsorb filtered glucose, excrete excess glucose from urine, and directly lower blood sugar. Clinical studies have shown that SGLT2 inhibitors have good efficacy, safety and tolerance, can effectively lower blood sugar, and become a new method for treating hyperglycemia in type 2 diabetes. [0003] Luxagliflozin is an SLGT2 inhibitor, which is insoluble in aqueous solution. Therefore, in order to meet the clinical bioavailability requirements, it is necessary to increase the solubility of rupagliflozin in aqueous media. [0004] The study found that before making rupagliflozin into a preparation, if the raw material is micronized to reduce the particle size, but due to the low melt...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/32A61K47/38A61K47/26A61K31/382A61P3/10
Inventor 严洁
Owner TIANJIN HANKANG PHARMA BIOTECH
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