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Eutecticum of azilsartan and 4,4'-dipyridyl and preparation method of eutecticum

A bipyridine and co-crystal technology, applied in the co-crystal of azilsartan and 4,4'-bipyridine and the field of preparation thereof, achieves the effects of easy industrial production, good thermodynamic stability and simple operation

Inactive Publication Date: 2018-08-03
WUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no literature and patent reports about azilsartan co-crystals. The present invention provides the first preparation method and crystal structure of azilsartan co-crystals. The experimental method is simple and easy for industrial production. Sartan cocrystal provides experimental basis

Method used

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  • Eutecticum of azilsartan and 4,4'-dipyridyl and preparation method of eutecticum
  • Eutecticum of azilsartan and 4,4'-dipyridyl and preparation method of eutecticum
  • Eutecticum of azilsartan and 4,4'-dipyridyl and preparation method of eutecticum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Dissolve 50.00 mg of azilsartan and 9.00 mg of 4,4'-bipyridine in 20 mL of acetone.

[0029] (2) Stir for 0.5 h under airtight conditions to completely dissolve the solid drug.

[0030] (3) Transfer the clarified liquid in the reaction vessel to a glass test tube, seal the test tube mouth with a parafilm, pierce 1-3 small holes on the parafilm with a needle, let it stand, evaporate at room temperature, and start to precipitate colorless after 7 days Transparent flaky crystals.

[0031] (4) The precipitated crystals were collected by single crystal diffraction and analyzed by Shelxtl software to determine that they were azilsartan-4,4'-bipyridine co-crystals, consisting of 8 azilsartan molecules and 4 4,4'- The structural units of bipyridine molecules are formed by O-H···N hydrogen bonds. Its space group is monoclinic C2 / c space group, its melting point is 164±2°C, and its unit cell structure is as follows: figure 1 As shown, its crystallographic data are as fig...

Embodiment 2

[0033] (1) Dissolve 50.00 mg of azilsartan and 9.00 mg of 4,4'-bipyridine in 50 mL of acetonitrile.

[0034] (2) Stir for 0.5 h under airtight conditions to completely dissolve the solid drug.

[0035] (3) Transfer the clarified liquid in the reaction vessel to a glass test tube, seal the test tube mouth with a parafilm, pierce 1-3 small holes on the parafilm with a needle, let it stand, evaporate at room temperature, and start to precipitate colorless after 20 days Transparent flaky crystals.

[0036](4) The precipitated crystal was determined to be azilsartan-4,4'-bipyridine co-crystal by single crystal diffraction unit cell, and its unit cell structure and crystallographic data were the same as those in Example 1.

Embodiment 3

[0038] (1) Dissolve 50.00 mg of azilsartan and 9.00 mg of 4,4'-bipyridine in 20 mL of methanol.

[0039] (2) Stir for 0.5 h under airtight conditions to completely dissolve the solid drug.

[0040] (3) Transfer the clarified liquid in the reaction vessel to a glass test tube, seal the test tube mouth with a parafilm, pierce 1-3 small holes on the parafilm with a needle, let it stand, evaporate at room temperature, and start to precipitate colorless after 15 days Transparent flaky crystals.

[0041] (4) The precipitated crystal was determined to be azilsartan-4,4'-bipyridine co-crystal by single crystal diffraction unit cell, and its unit cell structure and crystallographic data were the same as those in Example 1.

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Abstract

The invention discloses eutecticum of azilsartan and 4,4'-dipyridyl and a preparation method of the eutecticum, which relates to the technical field of medicine eutecticum. The invention aims at providing eutecticum of azilsartan and 4,4'-dipyridyl which is good in application prospect and thermal mechanical stability. The azilsartan-4,4'-dipyridyl eutecticum is formed by structural units consisting of eight azilsartan molecules and four 4,4'-dipyridyl molecules by virtue of O-H...N hydrogen bonds, and a space group is a monoclinic system C2 / c space group; and the eutecticum is characterized in that: bond length: a is equal to 28.9266(17), b is equal to 7.8175(5), c is equal to 24.9867(16); and bond angle: alpha is equal to 90 degrees, beta is equal to 110.254(7), gamma is equal to 90 degrees, Z is equal to 8, and V is equal to 5301.0(6).

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to a co-crystal of azilsartan and 4,4'-bipyridine and a preparation method thereof. Background technique [0002] Drug co-crystal is a hot field of drug research at present, the reason is that it can improve the physical and chemical properties of drugs, and can improve the solubility, dissolution rate and bioavailability of drugs. More importantly, co-crystals usually have excellent stability, which can overcome the problem of poor stability of drugs after salt formation. [0003] Azilsartan is the active ingredient of the new antihypertensive drug Azilsartan Medoxomil developed by Japan's Takeda Pharmaceutical Company (Takeda). On February 25, 2011, it was approved by the U.S. FDA under the product name Edarbi; and Azilsartan was launched in Japan in April 2012 under the product name Azilva. At present, there are no literature and patent reports about azilsartan co-crys...

Claims

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Application Information

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IPC IPC(8): C07D413/10C07D213/22C07D213/127
CPCC07B2200/13C07D213/127C07D213/22C07D413/10
Inventor 张宪瑞高蕾黎春兰刘娟娟杨韶平
Owner WUZHOU UNIV
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