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Iguratimod crystal form and its composition

A technology of crystal form and composition, which is applied in the field of autoimmune regulation drugs to achieve the effect of high biological activity and easy production

Active Publication Date: 2007-04-11
TIANJIN INSTITUTE OF PHARMA RESEARCH +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Regarding the crystalline form of iguratimod, there has been no literature report on the crystalline form so far

Method used

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  • Iguratimod crystal form and its composition
  • Iguratimod crystal form and its composition
  • Iguratimod crystal form and its composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Example 1. Preparation of Form 1: Take 10 grams of Iguratimod and put it into a 2000 ml round bottom flask, add 1000-1500 ml of analytical pure ethanol and activated carbon, heat, reflux, and filter, and place the filtrate at room temperature for 18 hours, filter, filter The cake was washed and dried under reduced pressure at 50-60°C to obtain 9.8 g of Form 1 with a melting point of 237-238°C.

[0082] The XRD pattern of Form 1 has peaks at about 26.00, about 24.56, about 20.80, about 19.56, about 17.54, about 10.92 and about 6.88, and its DSC endothermic transition is at about 236-240 ° C; the infrared absorption spectrum (IR) (KBr, cm -1 ) at about 3342, 3276, 3123, 3065, 2869, 1687, 1621, 1531, 1489, 1425, 1358, 1264 and 1156 cm -1 There are characteristic bands, see Figure 1-3.

Embodiment 2

[0083] Example 2. Preparation of Form 2: Take 10 grams of Iguratimod and put it into a 1000 ml round bottom flask, add 500-1000 ml of analytically pure acetonitrile and activated carbon, heat, reflux, filter, and place the filtrate at room temperature for 24 hours, filter, filter The cake was washed and dried under reduced pressure at 50-60°C to obtain 9.5 g of Form 2. The melting point is 237-238°C.

[0084] Form 2 has an XRD pattern at about 24.48, about 22.60, about 21.76, about 19.52, about 10.84, about 18.08, about 17.56, about 16.92, about 11.20, about 9.36, about 8.64, about 7.48, about 6.84, about 6.52, and about 5.60 Peak, its DSC endothermic transition is at about 236-240 ° C; the IR (KBr, cm -1 ) at about 3342, 3276, 3123, 3065, 2869, 1687, 1621, 1531, 1489, 1425, 1358, 1264 and 1156 cm -1 There are characteristic bands, differential thermal analysis chart, and infrared spectrum chart are the same as Form 1, see Figure 2-3.

Embodiment 3

[0085] Example 3. Preparation of Form 3: Take 10 grams of Iguratimod and put it into a 100 ml round-bottomed flask, add 20 ml of analytically pure dimethylformamide and activated carbon, heat, reflux, and filter, and place the filtrate in a refrigerator at room temperature for 18 hours. Filter, wash the filter cake, and dry under reduced pressure at 50-60°C to obtain 9.5 g of form 3. The melting point is 237-238°C.

[0086] The XRD pattern of Form 3 has peaks at about 27.28, about 25.68, about 25.24, about 24.40, about 24.04, about 23.08, about 20.16, about 17.52, about 10.56, and about 6.00, and its DSC endothermic transition is at about 236-240°C; IR (KBr, cm -1 ) at about 3342, 3276, 3123, 3065, 2869, 1687, 1621, 1531, 1489, 1425, 1358, 1264 and 1156 cm -1 There are characteristic bands, differential thermal analysis chart, and infrared spectrum chart are the same as Form 1, see Figure 2-3.

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Abstract

The present invention relates to five crystalline forms (Iguratimod) of N-[3-(formamido)-4-oxy-6-phenoxy-4H-1-benzo pyran-7-yl]-methane sulfonamide. The present invention also relates to the application of the crystalline forms (Iguratimod) in preparing medicine for rheumatic arthritis, medicine composition containing the crystalline forms (Iguratimod) and the preparation process of the crystalline forms (Iguratimod).

Description

technical field [0001] The invention belongs to the technical field of autoimmune regulation medicines, and more specifically, the invention relates to the crystal form of iguratimod, its preparation method and its application in the preparation of pharmaceutical preparations. 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 function of NSAIDs is to relieve joint pain, swelling and improve joint function in RA patients, but it does not change the progress of the disease, nor prevent joint destruction, and its severe adverse reactions to the gastrointestinal tract limit its use. Compared with NSAIDs, DMARDs have a slower onset of action and ...

Claims

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Application Information

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IPC IPC(8): C07D311/22A61K31/352A61P29/00A61P19/02
Inventor 梅林雨梁忠信王杏林高晶
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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