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Olmesartan medoxomil crystal and preparation method thereof

A technology for olmesartan medoxomil and crystal, which is applied in the field of new olmesartan medoxomil and its preparation, can solve the problems of poor solubility, difficult absorption, low bioavailability and the like of olmesartan medoxomil, and achieves good crystallinity and stability , low toxicity and simple preparation method

Inactive Publication Date: 2013-01-02
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Olmesartan medoxomil has poor solubility and is difficult to absorb after entering the human body, resulting in low bioavailability

Method used

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  • Olmesartan medoxomil crystal and preparation method thereof
  • Olmesartan medoxomil crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 1.0 g of olmesartan medoxomil in a three-necked bottle, add 20 mL of acetone, heat and reflux until completely dissolved, add 1 mL of water dropwise into the above solution, cool to 0-5°C while stirring, keep stirring at this temperature for 2 hours, and precipitate a solid , suction filtration, the resulting white powdery solid was washed twice with 2 mL of cold acetone, and dried at low temperature to obtain 0.871 g of olmesartan medoxomil crystals, with a yield of 87.1% and a purity of 99.8%. The prepared olmesartan medoxomil crystals had the following properties: X-ray powder diffraction pattern:

[0037] 2θ(°) d（?） Relative Strength 11.62 7.61 30 12.70 6.96 47 14.50 6.10 33 14.88 5.95 29 16.52 5.36 94 19.60 4.52 49 20.58 4.31 38 21.86 4.06 100 22.08 4.02 64 22.52 3.95 26 23.30 3.82 32 24.60 3.62 47 25.24 3.53 35

Embodiment 2

[0039] Take 1.0g of olmesartan medoxomil in a three-necked bottle, add 10mL of isopropanol, heat to reflux until completely dissolved, add 0.5mL of water to the above solution, cool to 0-5°C while stirring, and keep stirring at this temperature for 2h , precipitated solid, suction filtered, the white powdery solid obtained was washed twice with 2mL of cold isopropanol, and dried at low temperature to obtain 0.834g of olmesartan medoxomil crystals, with a yield of 83.4% and a purity of 99.7%. 1 is the same.

Embodiment 3

[0040] Embodiment 3 Acetone and water mixed solvent ratio experiment

[0041] According to the method of Example 1, two solvents, acetone and water, are used for recrystallization. The solvent ratios are 20:1, 20:2, 20:3, 20:4, 20:5, and 20:6. As above, the results are shown in Table 1, and the crystal form of the product obtained is the same as in Example 1.

[0042] Table 1 Experimental results of acetone and water mixed solvent ratio

[0043] serial number 1 2 3 4 5 6 Acetone:water (V:V) 20：1 20：2 20：3 20：4 20：5 20：6 Yield(%) 87.1 87.3 87.8 87.9 88.2 88.5 purity(%) 99.8 99.8 99.7 99.7 99.6 99.5

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PUM

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Abstract

The invention provides a new olmesartan medoxomil crystal and a preparation method thereof; the crystal has good crystallinity and stability; the preparation method is realized by recrystallization of olmesartan medoxomil in a mixed solvent. The olmesartan medoxomil crystal prepared by the method has good crystallinity and stability; the method is simple; the used organic solvent is a Class III solvent, which has low toxicity, and is beneficial to environmental protection; and the method is suitable for large-scale production.

Description

[0001] technical field [0002] The invention relates to a new crystal of olmesartan medoxomil and a preparation method thereof, a pharmaceutical composition containing the crystal of olmesartan medoxomil and the application of the pharmaceutical composition in the preparation of drugs for preventing or treating hypertension. Background technique [0003] Olmesartan medoxomil, chemical name is (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl-4-(1-hydroxy-1-methylethyl )-2-Propyl-1-{4-[2-(tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate, a prodrug, is absorbed during It is hydrolyzed, and blocks the vasoconstrictive effect of angiotensin II by selectively blocking the combination of angiotensin II and the AT1 receptor of vascular smooth muscle. It is used for the prevention or treatment of hypertension and other diseases. Its structural formula is: [0004] [0005] Those skilled in the art can prepare olmesartan medoxomil through the methods disclosed in US5616599, WO2004...

Claims

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Application Information

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IPC IPC(8): C07D405/14A61K31/4178A61P9/12
Inventor 邱传亮姜玉岗耿玉先马贵红黄玉锋
Owner BEIJING WINSUNNY PHARMA CO LTD
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