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Celecoxib solid dispersion using metal organic framework object as carrier and preparation method thereof

A technology of metal-organic framework and solid dispersion, which is applied in the field of medicine to achieve good dispersion performance, reduce particle size, and improve dissolution rate

Inactive Publication Date: 2018-12-14
SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the high melting point of lactose in this method, in order to reduce the melting temperature, it needs to be heated to melt under high pressure of 8-10 atmospheres, and the preparation process involves the limitation of high temperature and high pressure conditions.

Method used

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  • Celecoxib solid dispersion using metal organic framework object as carrier and preparation method thereof
  • Celecoxib solid dispersion using metal organic framework object as carrier and preparation method thereof
  • Celecoxib solid dispersion using metal organic framework object as carrier and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Take by weighing α-cyclodextrin 3.9g (4mmol), potassium hydroxide 1.8g (32mmol) is dissolved in 30ml water, filter with 0.45um polytetrafluoroethylene filter membrane, filtrate is placed in the 50ml beaker, put this beaker into Put it in a container containing methanol for 5 days, use the methanol diffusion method to crystallize, centrifuge filter, wash the solid with methanol twice, soak it in dichloromethane for 12 hours, filter, and dry the solid in vacuum at 40°C for 24 hours. A blank metal organic framework carrier MOF-1 was obtained.

[0027] After weighing 1.0 g of celecoxib and adding 2.5 ml of methanol to dissolve it, add 0.5 g of blank metal organic framework carrier. After standing at room temperature for 3 days, centrifugal filtration, the solid was washed 3 times with methanol to remove free celecoxib on the solid surface, and vacuum-dried at 40°C for 12 hours to obtain the MOFs as a carrier celecoxib solid dispersion.

Embodiment 2

[0029] Weigh 3.9g (4mmol) of α-cyclodextrin, dissolve 1.28g (32mmol) of sodium hydroxide in 30ml water, filter with a 0.45um polytetrafluoroethylene filter membrane, place the filtrate in a 100ml beaker, and put it into a container containing Store in a methanol container sealed for 5 days, use the methanol diffusion method to crystallize, centrifuge filter, wash the solid with methanol twice, soak in dichloromethane for 12 hours, filter, and dry the solid in vacuum at 40°C for 24 hours. A blank metal organic framework carrier MOF-2 was obtained.

[0030] After weighing 1.0 g of celecoxib and dissolving it in 2.5 ml of methanol, add 0.5 g of blank metal organic framework carrier. After standing at room temperature for 3 days, centrifugal filtration, the solid was washed with methanol three times to remove free celecoxib on the surface, and vacuum-dried at 40°C for 12 hours to obtain the MOFs as a carrier celecoxib solid dispersion.

Embodiment 3

[0032] After weighing 1.2 g of celecoxib and dissolving it in 4 ml of ethanol, add 0.5 g of MOF-2 carrier. After standing at room temperature for 3 days, centrifugal filtration, the solid was washed with ethanol three times to remove free celecoxib on the surface, and vacuum-dried at 40°C for 12 hours to obtain the MOFs as a carrier celecoxib solid dispersion.

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Abstract

The invention relates to a celecoxib solid dispersion using a metal organic framework object as a carrier and a preparation method thereof, which belong to the technical field of medicine. A poorly soluble drug celecoxib is loaded on the metal organic framework object by an impregnation method or a co-crystallization method, the mass percentage of celecoxib in the solid dispersion exceeds more than 10%, the solid dispersion can significantly improve the solubility of celecoxib, and the celecoxib solid dispersion has a good application prospect in the field of medicine.

Description

technical field [0001] The invention relates to a celecoxib solid dispersion with a metal organic framework as a carrier and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Celecoxib (Celecoxib) is a new generation of non-steroidal anti-inflammatory analgesics, which inhibits prostaglandin production by selectively inhibiting cyclooxygenase-2 (COX-2) to achieve anti-inflammatory and analgesic effects. It does not inhibit cyclooxygenase-1 (COX-1), which has a protective effect on the gastrointestinal tract, and its risk of gastrointestinal adverse reactions is significantly lower than that of traditional non-steroidal anti-inflammatory analgesics, so it is widely used clinically Treatment of osteoarthritis and rheumatoid arthritis. [0003] Celecoxib is almost insoluble in water and dissolves slowly in commonly used dissolution media. For example, patent CN99802185.7 discloses that the compound is almost insoluble in...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/40A61K47/02A61K31/635A61P29/00
CPCA61K31/635A61K47/02A61K47/6951A61P29/00
Inventor 林振广渠广民李兆明李尚斌
Owner SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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