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Preparation method of C-type candesartan cilexetil crystal

A candesartan cilexetil and crystallization technology, which is applied in the field of preparation of candesartan cilexetil cilexetil C-type crystal, can solve problems such as candesartan cilexetil cilexetil crystal form and crystal grain processing difficulties, and achieve the effect of ensuring the particle size range

Inactive Publication Date: 2013-08-28
EMEISHAN HONGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a kind of preparation method of candesartan cilexetil crystal form C, solve the existing difficult problem of candesartan cilexetil crystal form and crystal grain processing

Method used

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  • Preparation method of C-type candesartan cilexetil crystal
  • Preparation method of C-type candesartan cilexetil crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A preparation method of candesartan cilexetil C-type crystal, comprising the following steps:

[0023] (1) Add the crude candesartan cilexetil K6 to an ethanol solution whose mass is 7 times the mass of the crude candesartan cilexetil K6, stir and heat until dissolved;

[0024] (2) Cool down the dissolved solution to 30-35°C, and stir at this temperature until crystals are precipitated, then add dropwise water whose mass is twice the mass of the dissolved solution, and filter after the crystallization is complete. Get K6 boutique;

[0025] (3) Add anhydrous ethanol with a mass 4 times the quality of K6 fine product to K6 fine product, then use emulsifier for beating, transport with peristaltic pump, and spray dry to obtain candesartan type C with a particle size of micron Esters crystallize.

Embodiment 2

[0027] A preparation method of candesartan cilexetil C-type crystal, comprising the following steps:

[0028] (1) Add the crude candesartan cilexetil K6 to an ethanol solution whose mass is 10 times the mass of the crude candesartan cilexetil K6, stir and heat until dissolved;

[0029] (2) Cool down the dissolved solution to 30-35°C, and stir at this temperature until crystals are precipitated, then add dropwise water whose mass is twice that of the dissolved solution, and filter after the crystallization is complete. Get K6 boutique;

[0030] (3) Add anhydrous ethanol with a quality 5 times that of K6 fine product to the K6 fine product, then use an emulsifier for beating, transport it with a peristaltic pump, and carry out spray drying to obtain candesartan type C with a particle size of micron Esters crystallize.

Embodiment 3

[0032] A preparation method of candesartan cilexetil C-type crystal, comprising the following steps:

[0033] (1) Add the crude candesartan cilexetil K6 into an ethanol solution whose mass is 3 times the mass of the crude candesartan cilexetil K6, stir and heat until dissolved;

[0034] (2) Cool down the dissolved solution to 30-35°C, and stir at this temperature until crystals are precipitated, then add dropwise water whose mass is 0.5 times the mass of the dissolved liquid, and filter after the crystallization is complete. Get K6 boutique;

[0035] (3) Add absolute ethanol twice the quality of K6 fine product to K6 fine product, then use emulsifier for beating, transport with peristaltic pump, and spray dry to obtain candesartan type C with a particle size of micron Esters crystallize.

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Abstract

The invention discloses a preparation method of a C-type candesartan cilexetil crystal to solve the problem that an existing candesartan cilexetil crystal form and crystal grains are difficult to process. The preparation method comprises the following steps of: (1) adding a candesartan cilexetil crude product K6 into an ethanol solution, and stirring and heating until completely dissolving; (2) reducing the temperature of the completely dissolved solution to 30-35 DEG C, stirring at the temperature until a crystal is separated out, dropwise adding water, and filtering after complete crystallization to obtain a K6 fine product; and (3) adding absolute ethyl alcohol into the K6 fine product, pulping by adopting an emulsifying agent, conveying by using a peristaltic pump, and performing spray drying to obtain the C-type candesartan cilexetil crystal of which the particle size is of nano-scale. According to the preparation method, a spray drying method is adopted, so that the problem of product agglomeration in the conventional drying is solved, and then a dried product meets requirements on the crystal form and particle size once.

Description

technical field [0001] The invention specifically relates to a method for preparing candesartan cilexetil C-type crystal. Background technique [0002] Candesartan cilexetil is rapidly hydrolyzed into the active metabolite candesartan in the body. Candesartan is a selective angiotensin II receptor (AT1) antagonist, which antagonizes vascular tension by binding to vascular smooth muscle AT1 receptors The vasoconstriction effect of factor II reduces the peripheral vascular resistance. Others believe that candesartan can exert a certain antihypertensive effect by inhibiting the secretion of aldosterone by the adrenal gland. Candesartan does not inhibit kininase II and does not affect the degradation of bradykinin. [0003] There are many crystal forms of candesartan cilexetil, and at present, the crystal form C with better stability. The remaining crystalline forms are either not stable or have poor drug efficacy. Therefore, the control of crystalline forms needs to be studi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10
Inventor 葛绍勇涂亮陈立扬谯在银何海兵邓鹏洪健季健雷雨
Owner EMEISHAN HONGSHENG PHARMA
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