Telmisartan amorphous crystal and preparation method thereof

A technology of telmisartan and crystal form, which is applied in the field of pharmaceutical engineering and cardiovascular disease treatment drugs, can solve the problems of difficulty in obtaining telmisartan amorphous crystal form, small amount of drying, long cycle, etc., and achieve easy industrialization The effect of production, good dissolution rate and safe preparation method
CN104557724AActive Publication Date: 2015-04-29JIANGSU ZHONGBANG PHARMA

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JIANGSU ZHONGBANG PHARMA
Publication Date
2015-04-29

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Abstract

The invention discloses a telmisartan amorphous crystal and a preparation method thereof. An X-ray powder diffraction spectrum of the telmisartan amorphous crystal is as shown in figure 1, and no peak exists on a specific 2 theta characteristic peak position. The preparation method of the telmisartan amorphous crystal comprises the following steps of: a, mixing a crude telmisartan product and an organic solvent, wherein the organic solvent is alcohol; b, adding an alkali, and salifying and dissolving telmisartan under heating; c evaporating out the solvent, selectively metering and adding water at the same time, and adding acid at a temperature below 40 DEG C till no precipitate is separated out; d carrying out centrifugal separation on the precipitate product, and drying a detergent. The telmisartan amorphous crystal is provided by adopting the organic solvent with very low toxicity. The preparation method disclosed by the invention is safe, simple and high in operability; in addition, the obtained product is single in crystal form and can be used for preparing a medicament which contains amorphous telmisartan due to good dissolvability.
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Description

technical field

[0001] The invention belongs to medical engineering and drugs for treating cardiovascular diseases, in particular to a crystal form of telmisartan and a preparation method thereof. technical background

[0002] Telmisartan is a new type of AT antagonist with long-acting, high-efficiency and low-toxicity. It was developed by German Bellinger-Ingelheim Pharmaceutical Company and launched in 1997. It is also a non-peptide angiotensin II receptor antagonist that selectively and irreversibly blocks the AT1 receptor without affecting other receptor systems, especially those involved in the cardiovascular system. The structural formula is as follows:

[0003]

[0004] Those skilled in the art can prepare telmisartan through the methods disclosed in WO2004 / 87676, US2004 / 236113, WO2006 / 44648, WO2012 / 28925, WO2011 / 102645, EP2305650, US2006 / 211866, WO2006 / 136916, WO2010 / 4385.

[0005] When a substance is crystallized, due to the influence of various factors, the bo...

Claims

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