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Novel celecoxib composition and preparation process thereof

A technology of celecoxib and composition, applied in the field of new celecoxib composition, can solve the problems of restricting development, increasing degradation products, difficulty in swallowing and the like

Inactive Publication Date: 2013-07-24
北京博爱旺康医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are two problems in the soft capsule dosage form: 1. The content is liquid, and the raw material drug is dissolved in the liquid, which is easy to decompose and increase the generation of degradation products, which is unstable
2. There is a limit to the total amount of the solution, if it exceeds 1.0ml, it will be difficult to swallow
[0011] Celecoxib can also be used to treat various solid tumors such as tumor pain, colitis and lung cancer, and patients with rheumatoid arthritis and cancer are in urgent need of a celecoxib preparation that can be used for injection. Lecoxib is almost insoluble in water, and its water insolubility limits the development of its liquid preparations such as injections. The above solid dispersions, β-cyclodextrin inclusion complexes, and micronization technologies cannot solve the problem of celecoxib injection dosage forms. , and also have their own shortcomings in the preparation of solid preparations

Method used

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  • Novel celecoxib composition and preparation process thereof
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of celecoxib glucosyl-β-cyclodextrin composition by saturated aqueous solution method

[0039] Weigh 307g (0.237mol) of glucosyl-β-cyclodextrin, put it in a 500ml three-necked bottle with an electric stirring device, add 230ml of phosphate buffer solution with pH 9.0, and put it in a water bath at 40°C to dissolve it; weigh Take 30g (0.079mol) of celecoxib, dissolve it in 30ml of ethanol, drop it into the saturated solution of glucosyl-β-cyclodextrin, stir at constant temperature for 4 hours, let the reaction solution stand for precipitation, suction filter, and the precipitate Wash with an appropriate amount of ethanol, and vacuum-dry at 50°C to obtain it.

[0040] Take celecoxib glucosyl-β-cyclodextrin composition obtained by this method 0.337g (containing celecoxib 30mg) and celecoxib 30mg, respectively add 10ml of water, fully shake to dissolve and then filter, the composition Take 1ml of the continued filtrate from the bottle, put it in a 100...

Embodiment 2

[0043] Example 2 Preparation of celecoxib glucosyl-β-cyclodextrin composition by solution stirring method

[0044] Weigh 6.83g (5.23mol) of glucosyl-β-cyclodextrin, put it in a beaker, add 800ml of pH 9.0 phosphate buffer, stir to dissolve, and weigh 1g (2.62mmol) of celecoxib, add In the above glucosyl-β-cyclodextrin solution. The mixed solution was stirred for 20 minutes by means of magnetic stirring, the solution was gradually clarified, filtered, and the filtrate was the celecoxib glucosyl-β-cyclodextrin composition solution. The solution prepared by the above method is freeze-dried to obtain a solid celecoxib glucosyl-β-cyclodextrin composition.

[0045] As determined by an ultraviolet-visible spectrophotometer, the solubility of the celecoxib glucosyl-β-cyclodextrin composition is 2.0556 mg / ml.

[0046]

Embodiment 3

[0047] Example 3 Preparation of celecoxib diglucosyl-β-cyclodextrin composition by saturated aqueous solution method

[0048] Weigh 532g (0.395mol) of diglucosyl-β-cyclodextrin, put it in a 500ml three-neck bottle with an electric stirring device, add 380ml of phosphate buffer solution with pH 9.0, and put it in a water bath at 40°C to dissolve it; Weigh 30g (0.079mol) of celecoxib, dissolve it in 30ml of ethanol, drop it into the saturated solution of diglucosyl-β-cyclodextrin, stir at constant temperature for 4 hours, let the reaction solution stand for precipitation, and suction filter. The precipitate was washed with an appropriate amount of ethanol, and dried under vacuum at 50°C to obtain the obtained product.

[0049]

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Abstract

The invention relates to a novel composition of celecoxib and glucosyl-cyclodextrin or sulfobutyl-beta-cyclodextrin as well as a preparation method of the composition and application in medicine preparations. According to the invention, the prepared composition of celecoxib and glucosyl-cyclodextrin or sulfobutyl-beta-cyclodextrin has the advantages of improving the water solubility and the stability and has no adverse effect of hemolysis, so that the composition can serve as a starting material or a constituent for preparing intestinal-administration preparations or non-intestinal-administration preparations for treating tumors or rheumatoid arthritis; and the solid preparations have high bioavailability and the freeze-dried powder injections meet the requirements on the aspect of pH value and have no adverse effect of hemolysis.

Description

technical field [0001] The present invention relates to a new celecoxib composition, as well as the preparation process and medical application of the composition. Background technique [0002] Arthritis is a disabling disease characterized clinically by pain, joint deformation, and limited mobility. Osteoarthritis is a restrictive joint disease leading to severe disability due to progressive joint destruction; rheumatoid arthritis is a chronic inflammatory disease involving multiple systems caused by an autoimmune disorder. [0003] NSAIDs are widely used in the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It inhibits the formation of prostaglandins and thromboxanes by inhibiting the activity of cyclooxygenase (COX). COX has two isozymes: the essential enzyme COX-1 and the inducible enzyme COX-2. The enzymatic products of COX-1 are involved in physiological functions such as protection of gastrointestinal mucosa, platelet function, regul...

Claims

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Application Information

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IPC IPC(8): A61K31/635A61K47/40A61P35/00A61P29/00A61P19/02
Inventor 黄华其他发明人请求不公开姓名
Owner 北京博爱旺康医药科技有限公司
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