Crystalline form I of celecoxib, preparation method and purpose thereof

A technology of celecoxib and crystal form, applied in the field of autoimmune regulation drugs, can solve problems such as restricted use, and achieve the effects of easy production and high biological activity

Inactive Publication Date: 2012-12-26
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main role of NSAIDs is to reduce joint pain, swelling and improve joint function in RA patients, but its severe adverse reactions to the gastrointestinal tract limit its use

Method used

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  • Crystalline form I of celecoxib, preparation method and purpose thereof
  • Crystalline form I of celecoxib, preparation method and purpose thereof
  • Crystalline form I of celecoxib, preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Preparation of celecoxib crystal form I: Take 10 grams of celecoxib and put it into a 250 ml round bottom flask, add 10-15 ml analytically pure ethyl acetate and activated carbon, heat, reflux, filter, and place the filtrate at room temperature for 1 hour , filtered, the filter cake was washed, and dried under reduced pressure at 50-60°C to obtain 9.8 g of Celecoxib Form I, with a melting point of 160-164°C.

[0080] The XRD pattern of Celecoxib Form I has peaks at 5.38, 10.74, 14.86, 16.12, 19.66 and 21.54. Infrared absorption spectrum at 3338.48, 3232.05, 3098.55, 1347.58 and 1164.19cm -1 There are characteristic bands, and its DSC endothermic transition is at 160-164°C. See Figure 1a , Figure 1b , figure 2 , image 3 .

Embodiment 2

[0082] Preparation of Celecoxib Form I 100mg Capsules

[0083] Capsules are prepared with the following composition:

[0084]

[0085]

Embodiment 3

[0087] Preparation of Celecoxib Form I 200mg Capsules

[0088] Capsules are prepared with the following composition:

[0089]

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Abstract

The invention relates to a crystalline form I of celecoxib and a preparation method thereof, and further relates to a pharmaceutical composition prepared by using the crystalline form I of celecoxib obtained by the invention, and an application of the pharmaceutical composition. The crystalline form I of celecoxib is characterized by an x-ray powder diffraction pattern spectrum, a differential thermal analysis spectrum and an infra-red spectrogram thereof.

Description

technical field [0001] The invention belongs to the technical field of autoimmune regulation drugs, more specifically, the invention relates to celecoxib crystal form I and its preparation method and its application in the preparation of antipyretic, analgesic and anti-arthritis drugs. Background technique [0002] Rheumatoid arthritis (RA) is a highly disabling systemic autoimmune disease. If it is not actively and effectively treated, joint erosions will generally occur within 1 to 2 years. Currently, RA treatment is divided into two categories of drugs, non-steroidal anti-inflammatory analgesics (NSAIDs) and disease-modifying antirheumatic drugs (DMARDs). The main role of NSAIDs is to relieve joint pain, swelling and improve joint function in RA patients, but their severe adverse reactions to the gastrointestinal tract limit their use. Recombinant enzymatic studies showed that its IC for COX-2 and COX-1 50 0.04μmol / L and 15μmol / L respectively, the selective inhibitory e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/12A61K31/635A61P19/02A61P29/00
Inventor 梅林雨罗振福梁忠信郑志超高晶靳朝东张宗鹏
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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