New Crystal Forms of Supramolecular Complexes of Angiotensin Receptor Antagonist and Neutral Endopeptidase Inhibitor

A receptor antagonist, neutral endopeptidase technology, applied in the field of new crystal forms of angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex, can solve the problem of stability and fluidity. Different compressibility and other problems, to achieve the effect of good stability and high water solubility

Active Publication Date: 2017-08-22
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, its stability, fluidity, and compressibility may also be different. These physical and chemical properties have a certain impact on the application of drugs.

Method used

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  • New Crystal Forms of Supramolecular Complexes of Angiotensin Receptor Antagonist and Neutral Endopeptidase Inhibitor
  • New Crystal Forms of Supramolecular Complexes of Angiotensin Receptor Antagonist and Neutral Endopeptidase Inhibitor
  • New Crystal Forms of Supramolecular Complexes of Angiotensin Receptor Antagonist and Neutral Endopeptidase Inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 1g of LCZ696 crystal form I in a container, add 6ml of tetrahydrofuran to dissolve it, slowly add this solution into 60ml of cyclohexane at room temperature, stir slowly for 24h, filter and vacuum dry to obtain a white powder, which is LCZ696 of the present invention Crystal form II.

[0021] X-ray powder diffraction (XRPD)

[0022] The XRPD pattern of LCZ696 crystal form II was obtained by using a Rigaku Ultima IV powder diffractometer, which was irradiated with Cu-Kα and carried out at room temperature using a D / tex Ultra detector. The scanning range is from 5° to 45° in the 2θ interval, and the scanning speed is 20° / min. The XRPD crystal form characterization data of LCZ696 crystal form II are shown in Table 1:

[0023] Table 1

[0024]

[0025] Infrared spectrum of LCZ696 crystal form II

[0026] Using Fourier transform attenuated total reflection infrared spectroscopy (ATR-FTIR) spectrometer (Agilent Cary630) to obtain infrared absorption spectrum, the ...

Embodiment 2

[0037] Weigh 1g of LCZ696 crystal form I in a container, add 6ml of tetrahydrofuran to dissolve it, slowly add this solution into 60ml of methyl tert-butyl ether at room temperature, stir slowly for 24h, filter and vacuum dry to obtain a white powder, XRPD detection shows The product obtained was the same as in Example 1.

Embodiment 3

[0039] Weigh 1g of LCZ696 crystal form I in a container, add 6ml of isobutanol to dissolve, slowly add this solution into 60ml of methyl tert-butyl ether at room temperature, stir slowly for 24h, filter and vacuum dry to obtain a white powder, XRPD Detection showed that the obtained product was the same as in Example 1.

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Abstract

The present invention discloses a novel crystalline form of an angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex. The novel crystalline form of the supramolecular complex has high water solubility and good stability. Experiments show that the moisture absorption and intrinsic dissolution extent and speed are superior to those of a conventional crystalline supramolecular complex.

Description

technical field [0001] The invention relates to a new crystal form of a supramolecular complex of an angiotensin receptor antagonist (ARB) and a neutral endopeptidase (NEP) inhibitor and a preparation method thereof. Background technique [0002] Angiotensin receptor antagonist (ARB) and neutral endopeptidase (NEP) inhibitor supramolecular complex provided by the present invention: [3-((1S,3R)-1-biphenyl-4-ylmethyl -3-Ethoxycarbonyl-1-butylcarbamoyl)propanoic acid-(S)-3'-methyl-2'-(pentanoyl{2"-(tetrazol-5-yl anion)biphenyl -4'-ylmethyl}amino)butyric acid]trisodium hemipentahydrate (or abbreviated as "LCZ696"). LCZ696 was developed by Novartis in Switzerland and can be used for the treatment of hypertension and heart failure (acute and Chronic), its structure is as shown in formula A: [0003] [0004] WO 2007056546 discloses a crystal form of LCZ696, which is characterized in that the X-ray powder diffraction pattern measured by the Scintag XDS2000 powder diffractomete...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D257/04C07C233/47C07C231/24
CPCC07B2200/13C07C231/24C07C233/47C07D257/04
Inventor 任国宾齐明辉洪鸣凰刘岩陈景艳
Owner EAST CHINA UNIV OF SCI & TECH
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