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Telmisartan tablets and preparation method thereof

A technology of telmisartan and sodium salt, applied in the field of telmisartan tablets and preparation thereof, can solve the problems of large difference, long time consumption, manpower and material resources, etc., and achieves good product stability, simple process operation, and improved similarity. sexual effect

Inactive Publication Date: 2020-06-09
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This method requires the use of micronization equipment, the conditions are relatively harsh, and high-performance jet mill performance is required, as well as a large amount of energy and manpower consumption.
The Chinese invention patent application with the patent publication number CN107982232A provides a method for preparing telmisartan tablets. It is found that when the process is implemented, the solution is very viscous, and the whole process takes a long time and consumes a lot of manpower and material resources.
The patent application with the patent publication number CN107137370A discloses a preparation method of telmisartan tablet. The product prepared according to the prescription process needs to be coated. After comparing a number of dissolution curves, it is found that it is different from the reference preparation. Larger, poor bioequivalence

Method used

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  • Telmisartan tablets and preparation method thereof
  • Telmisartan tablets and preparation method thereof
  • Telmisartan tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] A kind of preparation method of telmisartan tablet comprises the steps:

[0055] 1. 40g telmisartan, 3.3g sodium hydroxide, and 12g meglumine were prepared into 90g ethanol aqueous solution (2:1);

[0056] 2. The prepared solution was distilled under reduced pressure at 80°C, and the precipitated particles were dissolved in 90 g of ethanol, and then evaporated to dryness for recrystallization, finally obtaining an amorphous sodium salt particle;

[0057] 3. Add the prepared sodium salt granules, 160g sorbitol, and 20g povidone K30 into a wet mixing granulator, stir and shear for 20min, add 4.8g purified water to make a soft material, granulate, and fluidize the bed at 60°C For drying, the parameters of the fluidized bed are: the inlet air temperature is 50°C, the fan frequency is 30Hz, and the material temperature is controlled at about 40°C. The moisture content is controlled not to be higher than 3.5% to obtain dry granules; the dried granules are sized and passed th...

Embodiment 2

[0061] A kind of preparation method of telmisartan tablet comprises the steps:

[0062] 1. 80g telmisartan, 7.0g sodium hydroxide, and 30g meglumine were prepared into 180g ethanol aqueous solution (2:1);

[0063] 2. The prepared solution was distilled under reduced pressure at 90°C, and the precipitated particles were dissolved in 180 g of acetone, and then evaporated to dryness again for recrystallization, finally obtaining a crystal form of amorphous sodium salt particles.

[0064] 3. Add the prepared sodium salt granules, 300g sorbitol, and 40g povidone K30 into a wet mixing granulator, stir and shear for 20 minutes, add 14.4g purified water to make a soft material, granulate, and fluidize the bed at 60°C For drying, the parameters of the fluidized bed are: spraying speed 10r / min, air inlet temperature 50°C, fan frequency 30Hz, material temperature controlled at about 40°C. The moisture content is controlled not to be higher than 3.5% to obtain dry granules; the dried gra...

Embodiment 3

[0068] Preparation method I (control group 1) of prior art telmisartan tablet:

[0069] The sodium hydroxide 3.36g that weighed recipe quantity (in 1000 pieces) joins 150mL purified water, after stirring and dissolving, add meglumine 12g, after stirring and dissolving completely, add telmisartan raw material 40g, after stirring and dissolving completely, Finally, 12g of povidone was added, stirred and dissolved, and ultrasonically degassed to obtain a slurry. Weighed 122.24g of mannitol as a substrate and added it to a fluidized bed for granulation, plus 31.92g of mannitol, 12g of hydroxypropyl cellulose, and stearin Magnesium acid 1.68g, talcum powder 4.8g are mixed and compressed into tablets to obtain Telmisartan tablets. Among them, the parameters of the fluidized bed are: the spraying speed is 10r / min, the air inlet temperature is 50°C, the fan frequency is 30Hz, and the material temperature is controlled at about 40°C.

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Abstract

The invention relates to a preparation method of telmisartan tablets. The preparation method comprises steps as follows: telmisartan, sodium hydroxide and meglumine are subjected to salinization and recrystallization treatment, dry particles are obtained, the particles and auxiliary materials are granulated in a wet type granulator and dried in a fluidized bed, a lubricating agent is added after granulation for tabletting, and the telmisartan tablets with digestion performance which is highly similar to digestion performance of an original reference preparation are prepared. Telmisartan is adopted as a raw material, amorphous sodium salt is prepared from the telmisartan raw material by synthetic test equipment, the sodium salt has stable characters and can be stored for a long time, with the adoption of an optimized wet granulation technology, micronization equipment with harsh conditions is not needed, the technological operation is simple, meanwhile, similarity of multiple strippingcurves of an own product and a reference preparation is improved, the product has good stability and compressibility, and similarity of multiple stripping curves of a main drug and the reference preparation is improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a telmisartan tablet with good compressibility, improved similarity of dissolution curves of the main drug and a reference preparation, and very stable product and a preparation method thereof. Background technique [0002] The chemical name of telmisartan is 4'-[(1,4'-dimethyl-2'-propyl[2,6'-di-1H-benzimidazole]-1'-yl)methyl Base]-[1,1'-diphenyl]-2-carboxylic acid, English aliases: Telmisartan; TELMISARTAN, white or off-white crystalline powder. INN Telmisartan (telmisartan) is an angiotensin II receptor antagonist developed for the treatment of hypertension and other medical conditions, as disclosed in EP-A-502314 patent. Its chemical name is 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-ylmethyl]-biphenyl- 2-Carboxylic acid, has the following structure: [0003] [0004] Telmisartan is a new antihypertensive drug and a specific angiotensin II rece...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4184A61K47/18A61K47/32A61P9/12
CPCA61K9/2013A61K9/2027A61K31/4184A61P9/12
Inventor 陈用芳胡延贵杨绪凤樊竟洁
Owner CHONGQING CONQUER PHARML
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