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Angiotensin receptor antagonist as well as NEP inhibitor drug crystal form and preparation thereof

A crystal form and solvent technology, applied in the field of angiotensin receptor antagonists and NEP inhibitor drug crystal forms and their preparation, can solve the problems of low solubility and low bioavailability of preparations, and achieve the effect of good stability

Inactive Publication Date: 2017-01-11
JIANGSU CAREFREE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In general, for oral solid water-insoluble drugs, the higher the melting point of the product crystal form, the better the stability, but the solubility of the corresponding product and the bioavailability of the preparation are relatively low

Method used

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  • Angiotensin receptor antagonist as well as NEP inhibitor drug crystal form and preparation thereof
  • Angiotensin receptor antagonist as well as NEP inhibitor drug crystal form and preparation thereof
  • Angiotensin receptor antagonist as well as NEP inhibitor drug crystal form and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Preparation of Amorphous Crystal Form of Trisodium Valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-valeric acid ethyl ester)

[0018] Add 60mL methanol to a 100 mL three-necked flask, stir magnetically, add 15.0 g valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl -Ethyl valerate) trisodium, (control the temperature throughout the process to T<35°C), stir to dissolve the solid, continue to stir for 30 minutes, evaporate the solvent under negative pressure (<-0.1 Mpa) below 35°C, and obtain the target The crystalline product is 15.0 g, yield: 100%.

Embodiment 2

[0020] Preparation of Amorphous Crystal Form of Trisodium Valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-valeric acid ethyl ester)

[0021] Add 50 mL of isopropanol to a 100 mL three-necked flask, stir magnetically, add 10 g of valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2 -Methyl-valeric acid ethyl ester) trisodium, (control temperature throughout the process to T<35°C), stir to dissolve the solid, continue to stir for 30min, evaporate the solvent under negative pressure (<-0.1 Mpa) below 35°C , to obtain 10 g of the target crystal form product, yield: 100%.

Embodiment 3

[0023] Preparation of Amorphous Crystal Form of Trisodium Valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-valeric acid ethyl ester)

[0024] Add 25 mL tetrahydrofuran into a 50 mL three-necked flask, stir magnetically, and add 2 g valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl Base-ethyl pentanoate) trisodium, (the temperature is controlled to T<35°C during the whole process), stir to dissolve the solid, continue to stir for 30 minutes, and evaporate the solvent under negative pressure (<-0.1 Mpa) below 35°C. Add 20 mL of acetonitrile to the obtained solid, stir to disperse, filter, and dry under negative pressure (<-0.1 Mpa) at 35±2°C for 24 hours to obtain 1.9 g of the target crystal form product with a yield of 95%.

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Abstract

The invention relates to an amorphous crystal form of a latest-generation cardiotonic agent valsartan ((2R, 4S)-5-biphenyl-4-group-5-(3-carboxyl-propionyl-amino)-2-methyl-ethyl valerate) trisodium and a preparation method of the cardiotonic agent.

Description

technical field [0001] The present invention relates to a new generation anti-heart failure drug valsartan ((2R, 4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl Amorphous crystal form of trisodium ester and preparation method thereof. Background technique [0002] Valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-valeric acid ethyl ester) trisodium, the structural formula is as formula [I] shown. [0003] [0004] [I] [0005] Valsartan ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-valeric acid ethyl ester) trisodium was developed by Novartis Pharmaceuticals as an anti- The heart failure drug was granted fast-track review by the FDA. It is the first angiotensin receptor-neprilysin dual inhibitor. Blocking the degradation of natriuretic peptides by the neprilysin inhibitor sacubitril benefits cardiovascular and renal function in patients with heart failure, while valsartan targets angiotensin recep...

Claims

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Application Information

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IPC IPC(8): C07D257/04
CPCC07D257/04
Inventor 秦引林
Owner JIANGSU CAREFREE PHARM CO LTD
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