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Celecoxib lyophilized orally disintegrating tablets with high bioavailability and preparation method thereof

A celecoxib, utilization technology, applied in the field of celecoxib freeze-dried orally disintegrating tablets and its preparation, can solve the difficult problems of solvent residue, low bioavailability, low oral compliance, etc., to reduce adverse reactions Risk of reactions, reduction of local irritation, effect of low doses

Active Publication Date: 2020-02-28
烟台药物研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN201310659807.1 adopts microsphere technology to prepare celecoxib immediate-release microspheres, but a large amount of organic solvents are used in the preparation process, and it is difficult to solve the problem of solvent residue; Preparation of diols as solid dispersions
[0004] At present, the commercially available formulation of celecoxib in China is the capsule formulation produced by Pfizer Pharmaceutical Co., Ltd., which has low bioavailability, large dosage, slow absorption, low oral compliance, and cardiovascular and gastrointestinal adverse effects. reaction and other defects

Method used

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  • Celecoxib lyophilized orally disintegrating tablets with high bioavailability and preparation method thereof
  • Celecoxib lyophilized orally disintegrating tablets with high bioavailability and preparation method thereof
  • Celecoxib lyophilized orally disintegrating tablets with high bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Recipe composition:

[0029]

[0030] The specific preparation method is: adding polyvinylpyrrolidone and sodium lauryl sulfate into 200mL of pure water and stirring to dissolve. Slowly pour the celecoxib raw material into the dispersion medium and stir for 5 minutes, so that the celecoxib is fully wetted and dispersed in the dispersion medium to obtain an initial suspension. Add the above primary suspension into a nano grinder, adjust the rotation speed to 3000 rpm, and wet grind for 30 minutes to obtain a nanoscale drug suspension. Add the prescribed amount of mannitol and aspartame into the suspension, stir and mix until fully dissolved, and obtain a suspension for freeze-drying. After vacuum degassing the above suspension, inject it into the mold accurately. Freeze-dry the mold filled with the liquid medicine according to the freeze-drying curve: Pre-freeze at -100°C for 2 hours - vacuumize - maintain at -40°C for 3 hours - maintain at -20°C for 8 hours - maint...

Embodiment 2

[0032] Recipe composition:

[0033]

[0034]

[0035] Add polyvinylpyrrolidone and sodium lauryl sulfate into 200 mL of pure water and stir to dissolve. Slowly pour the celecoxib raw material into the dispersion medium and stir for 5 minutes, so that the celecoxib is fully wetted and dispersed in the dispersion medium to obtain an initial suspension. Add the above primary suspension into a nano grinder, adjust the rotation speed to 1000 rpm, and wet grind for 120 min to obtain a nanoscale drug suspension. Add the prescribed amount of glycine and aspartame into the suspension, stir and mix until fully dissolved, and obtain a suspension for freeze-drying. After vacuum degassing the above suspension, inject it into the mold accurately. Freeze-dry the mold filled with the liquid medicine according to the freeze-drying curve: Pre-freeze at -40°C for 4 hours—vacuumize——15°C for 10 hours—0°C for 5 hours—15°C for 6 hours—30°C for 2 hours— Return to atmospheric pressure. Afte...

Embodiment 3

[0037] Recipe composition:

[0038]

[0039] Add hydroxypropyl cellulose and sodium lauryl sulfate into 150mL of pure water and stir to dissolve, add microcrystalline cellulose-sodium carboxymethyl cellulose slowly, and stir at high speed until uniformly dispersed. Slowly pour the celecoxib raw material into the dispersion medium and stir for 15 minutes, so that the celecoxib is fully wetted and dispersed in the dispersion medium to obtain an initial suspension. Add the above primary suspension into a nano grinder, adjust the rotation speed to 3500 rpm, and wet grind for 45 minutes to obtain a nanoscale drug suspension. Add the prescribed amount of sucrose and aspartame into the suspension, stir and mix until fully dissolved, and obtain a suspension for freeze-drying. After vacuum degassing the above suspension, inject it into the mold precisely. Freeze-dry the mold filled with the liquid medicine according to the freeze-drying curve: pre-freeze at -80°C for 2 hours—vacuu...

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Abstract

The invention relates to celecoxib lyophilized orally disintegrating tablets with high bioavailability and a preparation method thereof. The celecoxib lyophilized orally disintegrating tablets comprise, by weight, 30-75% of celecoxib, 10-50% of a filler, 10-50% of a stabilizer, and 0.01-10% of a flavoring agent, adding up to 100% by weight, wherein the drug particle size of celecoxib is 10-1000 nm. The drug in the orally disintegrating tablets is subjected to nano-micronization treatment to prepare a nano drug delivery system with the particle size of 10-1000 nm, so that the solubility and dissolution speed of the drug can be obviously increased, the gastrointestinal absorption speed and the bioavailability can be increased, the same treatment effect can be achieved with lower dosage, andthe risk of adverse reactions can be reduced.

Description

technical field [0001] The invention relates to a celecoxib freeze-dried orally disintegrating tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Celecoxib is the world's first selective non-steroidal anti-inflammatory analgesic, which can prevent the production of inflammatory prostaglandins by specifically inhibiting COX-2, and achieve anti-inflammatory, analgesic and antipyretic effects. Compared with traditional non-steroidal anti-inflammatory analgesics, celecoxib does not inhibit COX-1, which has a protective effect on the gastrointestinal tract, which greatly reduces the risk of adverse reactions in the gastrointestinal tract while anti-inflammatory and analgesic. Clinically, it is mainly used to relieve the symptoms and signs of osteoarthritis (OA), adult rheumatoid arthritis (RA) and ankylosing spondylitis. At the same time, it is also widely used in the analgesic treatment of acut...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/32A61K47/20A61K47/38A61K47/36A61K47/42A61K47/26A61K47/10A61K31/635A61P29/00
CPCA61K9/2031A61K9/2013A61K9/2054A61K9/2027A61K9/205A61K9/2063A61K9/0056A61K31/635A61P29/00
Inventor 孔淑萌李亚平孙帅王琳程东方牛宝华李祥平
Owner 烟台药物研究所
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