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Celecoxib nanosuspension and preparation method thereof

A nano-suspension, celecoxib technology, applied in anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of low bioavailability of celecoxib, large drug dosage, etc. The effect of increasing solubility and dissolution rate, simple formulation and process, and easy industrialization

Inactive Publication Date: 2015-12-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the marketed variety of celecoxib is celecoxib capsules (Celebrex) developed by Pfizer. Since the capsule dosage form has not improved the defects such as low bioavailability of celecoxib and large drug dosage, there is still a need A celecoxib preparation has been developed, which can significantly improve the bioavailability of the drug on the basis of overcoming the insufficient properties of the raw material drug, and reduce the types and dosage of excipients as much as possible, and celecoxib nanosuspension is exactly such a A new type of preparation with important application value and broad market prospect

Method used

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  • Celecoxib nanosuspension and preparation method thereof
  • Celecoxib nanosuspension and preparation method thereof
  • Celecoxib nanosuspension and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0028] Weigh 0.25g of hypromellose, add 100mL of pure water to dissolve it completely, weigh 0.5g of celecoxib raw material, slowly pour it into the aqueous solution containing hypromellose under stirring, place in ultrasonic Sonicate in a washing machine for 5 minutes to disperse celecoxib in the aqueous stabilizer solution, and shear with a high-speed shear at 10,000 rpm for 5 minutes to obtain an initial suspension. The resulting primary suspension was poured into the feed port of a high-pressure homogenizer, and circulated 5 times at 200 bar and 15 times at 800 bar to obtain a celecoxib nanosuspension. The average particle size of the celecoxib nanosuspension prepared by this method is 382.2nm, the PI is 0.15, and the sedimentation ratio after standing for 48 hours is 95.7%.

Embodiment 2

[0030] Weigh 0.25g of poloxamer 188, add 100mL of pure water to dissolve it completely, weigh 0.5g of celecoxib raw material, slowly pour it into the aqueous solution containing poloxamer 188 under stirring, place in ultrasonic Sonicate in a washing machine for 5 minutes to disperse celecoxib in the aqueous stabilizer solution, and shear with a high-speed shear at 10,000 rpm for 5 minutes to obtain an initial suspension. The resulting primary suspension was poured into the feed port of a high-pressure homogenizer, and circulated 5 times at 200 bar and 15 times at 800 bar to obtain a celecoxib nanosuspension. The average particle size of the celecoxib nanosuspension prepared by this method is 251.3nm, the PI is 0.30, and the sedimentation ratio after standing for 48 hours is 92.5%.

Embodiment 3

[0032] Weigh 0.25g of polyvinylpyrrolidone K30, add 100mL of pure water to dissolve it completely, weigh 0.5g of celecoxib raw material, slowly pour it into the aqueous solution containing polyvinylpyrrolidone K30 under stirring, and place it in an ultrasonic cleaner Sonicate for 5 minutes to disperse celecoxib in the stabilizer aqueous solution, and shear at 10,000 rpm for 5 minutes with a high-speed shear to obtain an initial suspension. The resulting primary suspension was poured into the feed port of a high-pressure homogenizer, and circulated 5 times at 200 bar and 15 times at 800 bar to obtain a celecoxib nanosuspension. The average particle size of the celecoxib nanosuspension prepared by this method is 265.3nm, the PI is 0.29, and the sedimentation ratio after standing for 48 hours is 96.2%.

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Abstract

The invention belongs to the field of pharmaceutical preparations and provides a Celecoxib nanosuspension and a preparation method thereof. Celecoxib is a novel non-steroidal anti-inflammatory drug, inhibits cyclooxygenase -2(COX-2) is through specificity, has anti-inflammatory and pain-easing effects and is clinically used for treating osteoarthritis and rheumatoid arthritis. However, the Celecoxib has very low solubility and in-vivo bioavailability. In order to increase the dissolution and the bioavailability of the drug, a high-speed shearing combined high-pressure homogenizing method is adopted to prepare the Celecoxib nanosuspension, the particle size and the polydispersion index PI are used as indicators for formulation technology optimization, a laser particle analyzer and a transmission electron microscope are adopted to study the particle size and form of the drug, the dissolution of the drug is evaluated through in-vitro dissolution experiments, and rat in-vivo pharmacokinetic study is conducted. Measurement results prove that the drug particle size of the nanosuspension is 50-500 nm, and the dissolution and the in-vivo bioavailability of the drug are increased obviously.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a celecoxib nanosuspension and a preparation method thereof. Background technique [0002] Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) s ), can specifically inhibit cyclooxygenase-2 (COX-2), prevent the production of inflammatory prostaglandins, and then exert anti-inflammatory, analgesic and antipyretic effects. Clinically, it is mainly used for the treatment of osteoarthritis, rheumatoid arthritis and peripheral and central analgesia. [0003] Celecoxib is soluble in methanol, ethanol, dimethyl sulfoxide, acetone and other organic solvents, but hardly soluble in water. The solubility in water is only 3-7μg / mL (pH7, 40℃), and it belongs to the BCSII class of biopharmaceutical classification system . The extremely low solubility of celecoxib in water directly leads to poor gastrointestinal absorption and low oral bioavailability of the drug, which grea...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/635A61K47/26A61P29/00A61K47/20A61K47/32A61K47/34A61K47/38
Inventor 周建平何佳丽丁杨
Owner CHINA PHARM UNIV
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