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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AI-Extracted 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 speci...

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.

Application Domain

Organic active ingredientsMetabolism disorder +2

Technology Topic

DrugSolubility +4

Examples

Experimental program(4)

Example Embodiment

[0018] Example 1

[0019] Prescription composition of lupagliflozin tablets

[0020] Lupagliflozin 100g

[0021] Povidone 50g

[0022] Lactose 50g

[0023] Magnesium Stearate 5g

[0024] Preparation:

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

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

[0027] Step (3): Add solution A to solution B, stir to make it evenly dispersed, and take solution C 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 materials after the spray-drying are collected, passed through a 60-mesh sieve, an appropriate amount of lubricant is added, compressed into tablets, and lupagliflozin tablets are obtained .

Example Embodiment

[0029] Example 2

[0030] Prescription composition of lupagliflozin tablets

[0031] Lupagliflozin 100g

[0032] Low Substituted Hypromellose 50g

[0033] Mannitol 150g

[0034] Magnesium Stearate 5g

[0035] Preparation

[0036] Step (1): Take 100 g of lupagliflozin, add 700 g 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 to dissolve, and take the solution B.

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

[0039] Step (4): solution C is spray-dried in a spray dryer, and the temperature of spray-drying is controlled to be 115 ° C; the materials after spray-drying are collected, passed through a 60-mesh sieve, an appropriate amount of lubricant is added, compressed into tablets, and lupagliflozin tablets are obtained .

Example Embodiment

[0040] Example 3

[0041] Prescription composition of lupagliflozin tablets

[0042] Lupagliflozin 100g

[0043] Low Substituted Hypromellose 50g

[0044] Xylitol 100g

[0045] Magnesium Stearate 5g

[0046] Preparation

[0047] Step (1): Take 100 g of lupagliflozin, add 1500 g 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 take the solution B.

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

[0050] Step (4): the solution C is spray-dried in a spray dryer, and the temperature of the spray-drying is controlled to be 105 ° C; the materials after the spray-drying are collected, passed through a 60-mesh sieve, an appropriate amount of lubricant is added, compressed into tablets, and lupagliflozin tablets are obtained .

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Description & Claims & Application Information

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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

AI-Extracted Technical Summary

Problems solved by technology

Abstract

Examples

Example Embodiment

Example Embodiment

Example Embodiment

PUM

Description & Claims & Application Information

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