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Azilsartan alkali salt A crystal form, preparation method and application thereof

A technology of choline salt and crystal form, applied in the field of Azisartan choline salt crystal form A and its preparation, and achieves remarkable effects of stability and bioavailability

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

AI Technical Summary

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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  • Azilsartan alkali salt A crystal form, preparation method and application thereof
  • Azilsartan alkali salt A crystal form, preparation method and application thereof
  • Azilsartan alkali salt A crystal form, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 500 mg of azilsartan choline salt raw material powder in a container, add 100 ml of organic solvent, suspend at a temperature of 37°C for 48 hours, then filter and vacuum dry to obtain a white powder that is azilsartan choline salt A Crystal form, wherein, the ratio of azilsartan and choline in the raw material of azilsartan choline salt is 2:1.

[0034] The purity grades of the organic solvents used in the above method are all analytically pure grades, which can be ethanol, n-propanol, n-butanol, isopropanol, isopropyl ether, methyl tert-butyl ether, acetone, ethyl acetate, Any one of isopropyl acetate, 4-methyl-2-pentanone, 2-butanone, sec-butanol, n-heptane, acetonitrile, toluene, dichloromethane and tetrahydrofuran, or any two or two of the above Mix more than one in any proportion.

Embodiment 2

[0036] Dissolve 500 mg of azilsartan choline salt raw material powder in 10 ml of methanol, add n-propanol, isopropanol, diethyl ether, isopropyl ether, 4-methyl-2-pentanone, methyl tert-butyl ether Or any single solvent in acetonitrile until a small amount of solid precipitation stops, leave it for 12 hours to obtain a white solid, filter and vacuum-dry the white powder obtained by the white solid, which is the Azilsartan choline salt A crystal form, wherein , the ratio of azilsartan and choline in the raw material of azilsartan choline salt is 2:1.

[0037] In this example, the purity grades of methanol, n-propanol, isopropanol, diethyl ether, isopropyl ether, 4-methyl-2-pentanone, methyl tert-butyl ether or acetonitrile are analytical grades.

[0038] The ratio selection of azilsartan and choline in the azilsartan choline salt raw material is the same as in Example 1.

Embodiment 3

[0040] 500 mg of azilsartan choline salt raw material powder is dissolved in 20 milliliters of dimethylformamide, any single solvent is added in isopropyl ether, methyl tert-butyl ether or acetonitrile until a small amount of solids are separated out and stopped, static Set aside for 12 hours to obtain a white solid, filter and vacuum-dry the white solid to obtain a white powder that is the Azilsartan choline salt A crystal form, wherein the azilsartan choline salt raw material is azilsartan and choline The ratio is 2:1.

[0041] In this example, the purity grades of dimethylformamide, isopropyl ether, methyl tert-butyl ether or acetonitrile are all analytical grades.

[0042] The ratio selection of azilsartan and choline in the azilsartan choline salt raw material is the same as in Example 1.

[0043] The above crystal form A of azilsartan choline salt provided by the present invention can be used to prepare medicines for treating hypertension.

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Abstract

The invention discloses an Azilsartan alkali salt A crystal form, a preparation method and application thereof. Specifically, the XRPD atlas of the Azilsartan alkali salt A crystal form has diffraction peaks at places with 2theta=9.521, 11.02, 11.76, 13.26, 13.72, 14.279, 15.961, 17.28, 18.24, 19.12, 19.781, 20.423 20.999, 21.86, 22.6, 24.679, 25.919, 26.98, 28.501, 29.521, 30.82, and 33.901, wherein the error range of the 2theta value is 0.2. The Azilsartan alkali salt A crystal form provided by the invention has good high temperature and high humidity illumination stability, can be applied in drugs for treatment of high blood pressure diseases, and has significant stability and bioavailability.

Description

technical field [0001] The invention relates to a medicine for treating hypertension, in particular to azilsartan choline salt A crystal form 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 ab...

Claims

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Application Information

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