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Amorphous Azilsartan choline salt, preparation method and use thereof

A choline salt, amorphous technology, applied in the field of amorphous azilsartan choline salt and its preparation, to achieve the effects of remarkable stability and bioavailability, and good high-temperature light stability

Inactive Publication Date: 2016-07-20
SHANGHAI SUNTRONG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the solid prepared by the above-mentioned patent method is semi-crystalline, and no specific crystal form is involved. Therefore, it is of great significance to develop a new crystal form of azilsartan organic amine salt to improve the bioavailability of azilsartan

Method used

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  • Amorphous Azilsartan choline salt, preparation method and use thereof
  • Amorphous Azilsartan choline salt, preparation method and use thereof
  • Amorphous Azilsartan choline salt, preparation method and use thereof

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Embodiment Construction

[0019] The invention discloses an amorphous azilsartan choline salt and its preparation method and application, wherein the amorphous azilsartan choline salt has good high temperature and light stability, and is used in medicines for treating hypertension. Stability and bioavailability are remarkable. The present invention will be described in detail below in conjunction with the accompanying drawings.

[0020] The amorphous azilsartan choline salt provided by the invention, its XRPD collection of patterns is as follows figure 1 shown.

[0021] In the aforementioned amorphous azilsartan choline salt, the ratio of azilsartan to choline is 2:1, and the azilsartan choline salt exists in the form of a single molecule or a complex. Among them, the complex form is a molecular existence state understood by those skilled in the art, usually but not limited to a binding state formed by the interaction force between molecules, such as hydrogen bond type, ion type, charge transfer The...

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Abstract

The invention discloses an amorphous Azilsartan choline salt, a preparation method and use thereof. Specifically, the preparation method comprises the steps of: adding 1000mg of Azilsartan choline salt raw material powder into 50ml of methanol, performing heating to 50DEG C, and then utilizing ultrasound to dissolve all the Azilsartan choline salt raw material, and finally performing vacuum flash rotary evaporation to obtain white solid, i.e. the amorphous Azilsartan choline salt. Specifically, the ratio of Azilsartan to choline in the Azilsartan choline salt raw material is 2:1. The amorphous Azilsartan choline salt provided by the invention has good high temperature and illumination stability, can be applied to drugs for treatment of high blood pressure diseases and has significant stability and bioavailability.

Description

technical field [0001] The invention relates to medicine for treating hypertension, in particular to amorphous azilsartan choline salt and its preparation method and application. Background technique [0002] Azilsartan (also known as Azilsartan Medoxomil, English: Azilsartan) (INN) is an angiotensin II receptor antagonist drug for the treatment of hypertension. Receptor antagonist (sartan) drugs. As a prodrug, azilsartan is rapidly hydrolyzed into azilsartan acid in the gastrointestinal tract and exerts its pharmacological effect by selectively blocking the binding of angiotensin II to the ATI receptor in vascular smooth muscle And block the vasoconstrictive effect of angiotensin II, thereby lowering blood pressure. The drug is taken orally and can be used alone or in combination with other antihypertensive drugs for the treatment of hypertension and related complications. [0003] Because the molecular structure of azilsartan has a carboxyl group, it is poorly absorbed ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/10C07C215/40A61P9/12
Inventor 于迎渌陈金瑶弋东旭
Owner SHANGHAI SUNTRONG BIOTECH