Celecoxib solid dispersion and preparation method and application thereof

A technology of solid dispersion and celecoxib, applied in the field of medicine, can solve the problems of difficult to form a uniform mixture, increased bioavailability, poor solubility, etc., and achieve the effects of improving bioavailability, simple preparation method and increasing absorption

Inactive Publication Date: 2014-03-26
BEIJING SUNHO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent 99802185.7 and its divisional application 200410037522.5 record the preparation method of tablets and capsules of celecoxib, and carried out pharmaceutical experiments, but it only uses the method of pulverizing celecoxib to increase its bioavailability
[0006] Celecoxib is poorly soluble in aqueous media, and when administered orally, it is poorly absorbed, and other substances are not easy to form a homogeneous mixture when mixed with celecoxib, and tend to form a crystalline state

Method used

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  • Celecoxib solid dispersion and preparation method and application thereof
  • Celecoxib solid dispersion and preparation method and application thereof
  • Celecoxib solid dispersion and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Preparation of Solid Dispersion A:

[0053] Heat 300g of poloxamer 188 in a water bath to 55°C to melt, and add 15g of celecoxib while stirring. Keep the mixture in a molten state, stir it well, pour it on a steel plate that has been pre-frozen at -25°C, solidify at -25°C for 3 minutes, dry it for 1 day, pulverize it, and then place it in a vacuum drying oven to fully dry to obtain Celecoxib Cloth Solid Dispersion A.

Embodiment 2

[0055] Preparation of Solid Dispersion B:

[0056] Heat 300g of poloxamer 188 in a water bath to 90°C to melt, and add 20g of celecoxib while stirring. Keep the mixture in a molten state, stir it well, pour it on a steel plate that has been pre-frozen at 0°C, solidify at a temperature below 0°C for 8 minutes, dry it for 2 days, crush it, and then place it in a vacuum drying oven to fully dry to obtain celecoxib solid Dispersion B.

Embodiment 3

[0058] Preparation of Solid Dispersion C:

[0059] Add 300g of poloxamer 188 into 30g of celecoxib in 900mL of acetone solution, heat to 55°C to melt, and stir thoroughly. Continue to heat the mixture to fully volatilize the acetone, pour it on a steel plate that has been pre-frozen at -15°C, solidify at -15°C for 3 minutes, dry it for 2 days, pulverize it, and then dry it fully in a vacuum drying oven to obtain celecoxib solid dispersion C.

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Abstract

The invention specifically relates to a celecoxib solid dispersion and a preparation method and application thereof. The celecoxib solid dispersion is prepared from celecoxib and poloxamer 188 at a mass ratio of 1:(1-20) by a melting process and a solvent process. The dispersion provided by the invention has good dispersity and high stability; the solubility and dissolution rate of the medicine are increased; the solubility of the medicine in water is 5-200 times higher than that of the raw medicines; with good dissolution rate in water, the in-vivo absorption of the medicine can be enhanced so as to improve the bioavailability. The solid dispersion also can be made into multiple clinically acceptable dosage forms which are used as new dosage forms of celecoxib.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a solid dispersion of celecoxib and its preparation method and application. technical background [0002] Celecoxib is a drug developed and marketed by Pfizer for the treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. It can also be used to treat acute pain, dysmenorrhea, colorectal polyps and postoperative pain relief. One of the best-selling arthritis treatments right now. The structure of celecoxib is as follows: [0003] [0004] The mechanism of action of celecoxib is to selectively act on cyclooxygenase 2 (COX-2), which is a selective COX-2 inhibitor. Since it does not act on COX-1 and does not affect the synthesis of PGI2, which has a protective effect on the gastrointestinal tract and kidneys, its gastrointestinal side effects and nephrotoxicity are smaller than those of general NSAIDs, and it has no cardiovascular side effects. [0005] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/635A61K47/34A61P29/00A61P19/02A61P19/08A61P1/00
Inventor 林晓洁张明李勇修勇
Owner BEIJING SUNHO PHARMA
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