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Preparation method of candesartan cilexetil tablets

A technology for candesartan medoxomil and sartan medoxomil tablets, which are applied in directions such as medical preparations without active ingredients, medical preparations containing active ingredients, and pill delivery, etc., can solve the problem of decreased drug stability and unfavorable commercial production. , affecting the appearance of the product, etc., to achieve a good dissolution effect, avoid the decline of drug stability, and avoid the effect of reducing the dissolution rate

Active Publication Date: 2019-10-22
HINYE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in actual production, when the particle size of candesartan cilexetil is reduced below 20 μm, the stability of the drug will be greatly reduced. In order to ensure its stability, it is necessary to add more low-melting oily substances, although The melted oily substance reduces the friction between the fine crystals and improves the stability of the product, but it will also lead to a decrease in the dissolution rate of the product, and it will also cause sticking problems in the subsequent tablet production process, which will lead to unsatisfactory one-sidedness. Smooth, affects the appearance of the product, and is not conducive to commercial production

Method used

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  • Preparation method of candesartan cilexetil tablets
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  • Preparation method of candesartan cilexetil tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] A preparation method of candesartan cilexetil tablet, comprising the following steps;

[0032] (1) Weighing and preparing materials: weighing and preparing materials according to the prescription ratio in the table below;

[0033]

[0034] (2) Preparation method;

[0035] The candesartan cilexetil, lactose, cornstarch, hydroxypropyl cellulose, and carmellose calcium that were taken by weighing the prescription amount were passed through a 50-mesh sieve three times using a swinging granulator, and were used for subsequent use; the polyethylene glycol 6000 dissolved in the prescription amount In 95% ethanol, stir and control the temperature in a water bath of 50-60°C, heat and dissolve to prepare a wetting agent for later use; place the sieved and mixed raw and auxiliary materials in a granulator for dry mixing for 5 minutes, and set the stirring speed of the granulator to 160rpm, the shear rate is 1500rpm. Then add a 95% ethanol solution of polyethylene glycol 6000 ...

Embodiment 2

[0037] The candesartan cilexetil tablets prepared by different prescriptions in Example 1 were placed at 60°C for 10 days, and a high temperature experiment was carried out to investigate the related substances of the product. The experimental results are as follows:

[0038]

[0039] According to the measurement results, it can be known that the product produced by the preparation method of the present invention, when the ratio of the dosage of candesartan cilexetil and polyethylene glycol 6000 in the prescription is 2:1, the related substances in the product are relatively higher than the related substances in other prescriptions. is the most stable.

Embodiment 3

[0041]Press 2015 version " Chinese Pharmacopoeia " four general rules 0931 dissolution rate and release rate determination method second method, measure the dissolution rate of different prescription products in embodiment 1, wherein dissolution medium: 1% polysorbate 20 aqueous solution 900ml, rotating speed: 50rpm, The measurement results are as follows;

[0042]

[0043] In the prior art, on the one hand, the addition of polyethylene glycol 6000 can improve the stability of the medicinal ingredients in the solid preparation, but on the other hand, it will also lead to a decrease in the disintegration of the solid preparation, so that the drug can be released from the solid preparation. Dissolution properties were significantly reduced. According to the above measurement results, it can be known that the addition of polyethylene glycol 6000 has little effect on the dissolution rate of the product by adopting the preparation method of the present invention, and does not ca...

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Abstract

The invention relates to a preparation method of candesartan cilexetil tablets. The preparation method comprises the steps that candesartan cilexetil, lactose, corn starch, hydroxypropyl cellulose andcarboxymethyl cellulose calcium are weighed, pass through a 50-mesh sieve by using a shaking-type granulator and then are mixed for use, wherein the weight ratio of the candesartan cilexetil to polyethylene glycol 6000 is 4:1-4:2, and the weight ratio of the hydroxypropyl cellulose to the carboxymethyl cellulose calcium is 7:0.4-7:1; the polyethylene glycol 6000 is weighed and added to 95% ethanol, stirring is conducted, water-bath heating and dissolution are conducted by controlling the temperature at 50-60 DEG C, and a wetting agent is prepared for use, wherein the weight ratio of the polyethylene glycol 6000 to the 95% ethanol is 1:6.5-1:13; the sieved and mixed materials are placed in a horizontal wet mixing granulator for dry mixing, the prepared wetting agent is added at the liquidadding speed of 7-8 kg / min, granulation is conducted, discharging is conducted after wet mixing is conducted for 4-6 minutes, and wet granules are finished by a 24-mesh stainless steel sieve on the shaking-type granulator; the working procedures of drying, tabletting and the like are conducted.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a preparation method of candesartan cilexetil tablets. [0002] technical background [0003] Candesartan cilexetil is rapidly hydrolyzed into the active metabolite candesartan in the body. Candesartan is a selective angiotensin II receptor (AT1) antagonist that antagonizes vascular tension by binding to vascular smooth muscle AT1 receptors The vasoconstriction effect of factor Ⅱ, thereby reducing the resistance of peripheral blood vessels, helps to lower blood pressure. It is also believed 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. [0004] US Patent No. 5,196,444 discloses the curative effect of candesartan cilexetil in treating hypertension, and discloses a crystal form of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/10A61K47/38A61K31/4184A61P9/12
CPCA61K9/2031A61K9/2054A61K9/2095A61K31/4184A61P9/12
Inventor 丁强曾清泉金波宋志林高玉贺程雪清王衡新
Owner HINYE PHARM CO LTD
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