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Polymorphis of valsartan

A technology for valsartan and tan crystal forms, applied in the field of solid-state chemistry of valsartan, can solve problems such as not describing product characteristics

Inactive Publication Date: 2006-06-14
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the Merck Index does not describe the properties of said product

Method used

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  • Polymorphis of valsartan
  • Polymorphis of valsartan
  • Polymorphis of valsartan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0165] from tert-butyl acetate

[0166] 2 g of valsartan was dissolved in 15 ml of refluxing t-BuOAc to form a solution. The solution was cooled to room temperature with slow stirring, cooled to 0 °C and allowed to stand for 2 hours. The precipitate was filtered and left on the filter for 10 minutes. X-ray analysis showed that the sample had Form III crystals. The sample was dried at 50° C. / 10 mmHg for 2 hours, X-ray analysis showed that the dried sample was a purified amorphous form, and an endothermic peak was detectable in DSC.

Embodiment 2

[0168] from methyl tert-butyl ether

[0169] 5 g of valsartan were dissolved in 20 ml of refluxing MTBE, and the resulting solution was cooled to room temperature with slow stirring, then to 0° C. and allowed to stand for 3 hours. The precipitate was filtered, held on the filter for 10 minutes and dried at 50°C / 10 mmHg for 2 hours. X-ray analysis showed the sample to be a purified amorphous form and no endothermic peak was detected in DSC.

Embodiment 3

[0171] from isoethyl ether

[0172] Dissolve 2g valsartan in 35ml i-Pr 2 O, under reflux for 1 hour, most of the valsartan forms a viscous gelatinous residue. The solvent was decanted and the residue was dried at 50°C / 10 mmHg for 2 hours. X-ray analysis showed the sample to be a purified amorphous form and no endothermic peak was detected in DSC.

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Abstract

Provided are crystalline valsartan and amorphous valsartan, and methods for their preparation.

Description

[0001] priority uncle [0002] This application claims the benefit of U.S. Provisional Application Serial No. 60 / 473,640, filed May 28, 2003, and U.S. Provisional Application Serial No. 60 / 455,286, filed March 17, 2003, all of which are incorporated herein by reference . field of invention [0003] The present invention relates to the solid state chemistry of valsartan. Background of the invention [0004] Valsartan, also known as (S)-N-(1-carboxy-2-methyl-propan-1-yl)-N-pentanoyl-N-[2'-(1H-tetrazol-5-yl) ) biphenyl-4-ylmethyl]-amine having the following structure: [0005] [0006] Molecular formula C 24 h 29 N 5 o 3 [0007] Molecular weight 435.52 [0008] Exact mass 435.227040 [0009] Composition C 66.19%H 6.71%N 16.08%O 11.02 [0010] Melting point range 105-110°C [0011] It is also marketed as the free acid under the trade name DIOVAN. DIOVAN is a prescription drug of valsartan in 40mg, 80mg, 160mg and 320mg dosage oral tablets. [0012] Valsartan and...

Claims

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Application Information

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IPC IPC(8): C07D257/04A61K31/41
Inventor I·鲁克曼E·弗尔亚克斯T·科尔泰J·阿伦希姆
Owner TEVA PHARMA IND LTD
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