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Eutectic drug for treating heart failure

A technology of co-crystals and drugs, applied in the field of medicine, can solve the problems of long synthesis steps and the like

Active Publication Date: 2017-05-17
顾国明 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This route has long synthesis steps and uses precious Pd catalyst for high-pressure hydrogenation reduction reaction

Method used

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  • Eutectic drug for treating heart failure
  • Eutectic drug for treating heart failure
  • Eutectic drug for treating heart failure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Sacubitra Calcium Synthesis:

[0059] Control the temperature at 10-20°C, add 518g of dichloromethane, 39g of SV-A and 12.3g of succinic anhydride to a 1L dry reaction kettle in sequence, add 17.4g of N,N-diisopropylacetic acid dropwise at a temperature of 10-20°C Amine (DIPEA), after dripping, continue to control the temperature and stir for 3 to 4 hours; TLC monitors the reaction (developing solvent: ethyl acetate: acetic acid = 100: 1, Rf sv-1 = 0.2, Rf sv-2 =0.6, UV 254nm ), when SV-A disappears, the reaction is considered complete.

[0060] After the reaction is complete, add 40kg of water, evaporate the solvent under reduced pressure at 25-35°C, with a vacuum degree of ≤-0.08MPa, add 350g of isopropyl acetate to the residue, and wash the organic phase twice with water (100g / time), 0.2 % sodium bicarbonate washing 2 times (100g / time), 1.5N hydrochloric acid washing 2 times (100g / time), water washing 2 times (100g / time) and saturated sodium chloride washing 2 tim...

Embodiment 3

[0074] The HPLC detection method of Sacubi Trifemasartan Potassium:

[0075] Take Example 2 to prepare 5 mg of sacubi, trifemasartan potassium, dissolve it in a mixed solution (70 ml of mobile phase A: 30 ml of mobile phase), ultrasonicate for 10 minutes, filter, and take the filtrate.

[0076] Chromatographic column: octadecylsilane bonded silica gel as filler (recommended chromatographic column is Waters SunFire C18, 150×4.6mm, 3.5μm, or equivalent)

[0077] Mobile phase: 0.05% trifluoroacetic acid solution is mobile phase A, acetonitrile is mobile phase B, and elution is carried out according to the following gradient:

[0078] time (minutes) Mobile phase A(%) Mobile phase B(%) 0 70 30 50 35 65 50.01 70 30 60 70 30

[0079] Detection wavelength: 254nm

[0080] Flow rate: 1.0ml / min

[0081] Injection volume: 10 μl.

Embodiment 4

[0083] Sacubi Trifemasartan Potassium Tablets are formulated from the following components:

[0084]

[0085]

[0086] Its preparation method comprises the following steps:

[0087] 1) Grind and sieve sacubi, trifemasartan potassium and pharmaceutical excipients respectively, set aside,

[0088] 2) physically mix the raw materials and pharmaceutical excipients in parts by weight of the prescription amount,

[0089] 3) Wet granulation,

[0090] 4) dried, granulated,

[0091] 5) Convert the additional auxiliary materials, mix evenly, and press into tablets

[0092] 6) The Opadry is dissolved in a certain solvent and used as a coating solution for coating.

[0093] test results

[0094] Drug content: qualified

[0095] Disintegration time limit: meet the regulations

[0096] Sacubi Trifemasartan Potassium Dissolution in 45 minutes: 95.27%

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Abstract

The invention discloses a eutectic drug for treating heart failure and relates to a eutectic formed by sacubitril and an angiotensin-receptor blocker, wherein the angiotensin-receptor blocker is selected from: drugs such as fimasartan and the like.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a co-crystal medicine for treating heart failure. Background technique [0002] Background Technology of Shakubi [0003] The chemical name of Sacubitril is: 4-(((2S,4R)-1-(1,1′-biphenyl-4-yl)-5-ethoxy-4-methyl-5 -Oxopentan-2-yl)amino)-4-oxobutanoic acid (I), its structural formula is: [0004] [0005] Sacubitril is an inhibitor of neprilysin, which was first reported in EP0555175 patent. In July 2015, the U.S. Food and Drug Administration (FDA) approved the first angiotensin receptor (angiotensinreceptor) and neprilysin (neprilysin) dual inhibitor sacubitril valsartan sodium ( LCZ696) is marketed for patients with heart failure with reduced ejection fraction, which can reduce the risk of cardiovascular death and hospitalization for heart failure, and is the first clinical use of sacubitril as a drug. Sacubitril is a prodrug, which is cleaved into the neprilysin inhibitor LBQ657 u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10C07C233/47A61K31/216A61K31/513A61P9/04A61P9/10
CPCA61K31/216A61K31/513C07B2200/13C07C233/47C07D403/10A61K2300/00
Inventor 顾国明熊金武
Owner 顾国明
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