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Telmisartan tablet composition

A technology of telmisartan and composition, which is applied in the field of telmisartan tablet composition, can solve problems such as poor dissolution rate, inability to obtain shaped solids, strong hygroscopicity, etc.

Active Publication Date: 2010-12-01
BEIJING JINGFENG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Slightly soluble in strong acid, soluble in strong alkali, due to these characteristics, there is often a problem of poor dissolution rate when preparing telmisartan tablets. The prior art uses alkaline reagents such as sodium hydroxide and meglumine in the preparation to make Telmisartan forms a salt under alkaline conditions or further adds surfactants to improve the solubility of the drug. After telmisartan is dissolved with alkaline reagents such as sodium hydroxide and meglumine, it does not dissolve under ordinary heating and drying conditions. No matter the solvent is a mixture of water or ethanol, it is very difficult to dry. In the end, it is only a semi-fluid semi-solid. There is no way to dry it completely, so it needs to be dried under reduced pressure or spray drying.
However, due to the addition of sodium hydroxide and the like in the preparation, the prepared preparation granules still have disadvantages such as high viscosity and strong hygroscopicity, which cause the final obtained plain tablet to absorb moisture and change color easily under normal conditions. Studies have also shown that due to moisture absorption It also further affects the stability of the formulation
The current tablet adopts the method of coating or adding double aluminum blister packaging to solve this problem, but the defects of the granule itself still exist, which puts forward higher requirements for the production process of the preparation. At the same time, coating or Double aluminum blister packaging also increases the cost of the preparation, so it is necessary to improve the moisture resistance of the preparation itself through the improvement of the preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 Telmisartan tablet

[0023] Name of raw material Amount (g)

[0024] Telmisartan 80

[0025] Sodium hydroxide 6.72

[0026] Meglumine 24

[0027] Sorbitol 270

[0028] Calcium hydrogen phosphate 68

[0029] Povidone 20

[0030] Magnesium Stearate 10

[0031]

[0032] A total of 2000 pieces

[0033] Preparation:

[0034] 1) Combine sodium hydroxide and meglumine, add 20ml of water to dissolve, then add telmisartan, and add 120ml of ethanol to dissolve, shake and dissolve telmisartan, dry under reduced pressure at 40°C to obtain a white puffy Solid, pulverized through 200 mesh drying, to obtain telmisartan salt powder;

[0035] 2) Sorbitol, calcium hydrogen phosphate, and povidone are pulverized through 100 mesh, and magnesium stearate is crushed through 40 mesh, weighed according to the prescription amount and mixed with telmisartan salt powder evenly;

[0036] 3) The mixed powder is directly compressed into tabl...

Embodiment 2

[0037] Embodiment 2 Telmisartan tablet

[0038] Name of raw material Amount (g)

[0039] Telmisartan 80

[0040] Sodium hydroxide 6.72

[0041] Meglumine 24

[0042] Sorbitol 250

[0043] Calcium hydrogen phosphate 88

[0044] Povidone 20

[0045] Magnesium Stearate 10

[0046]

[0047] A total of 2000 pieces

[0048] Preparation:

[0049]1) Take sodium hydroxide and meglumine, add 20ml of water to dissolve, then add telmisartan, and add 120ml of ethanol to dissolve, shake and dissolve telmisartan, spray dry to obtain telmisartan salt powder;

[0050] 2) Sorbitol, calcium hydrogen phosphate, and povidone are pulverized through 100 mesh, and magnesium stearate is crushed through 40 mesh, weighed according to the prescription amount and mixed with telmisartan salt powder evenly;

[0051] 3) The mixed powder is directly compressed into tablets to obtain the product.

Embodiment 3

[0052] Embodiment 3 Telmisartan tablet

[0053] Name of raw material Amount (g)

[0054] Telmisartan 80

[0055] Sodium hydroxide 6.72

[0056] Meglumine 24

[0057] Sorbitol 280

[0058] Calcium hydrogen phosphate 58

[0059] Povidone 20

[0060] Magnesium Stearate 10

[0061]

[0062] A total of 2000 pieces

[0063] Preparation method: refer to the method of Example 1.

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Abstract

The invention belongs to the technical field of medicinal preparation, and in particular relates to a telmisartan tablet composition. The telmisartan tablet composition is characterized by being prepared from 80 parts of telmisartan, 6.72 parts of sodium hydroxide, 24 parts of meglumine, 250 to 280 parts of sorbierite, 58 to 88 parts of calcium hydrophosphate, 20 parts of polyvidone and 10 parts of magnesium stearate. By selecting and using the combination of sorbierite and calcium hydrophosphate as filler, the composition can obviously improve the stability of the preparation and is favorable for production and application of the preparation.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a stable telmisartan tablet composition. Background technique [0002] Telmisartan (Telmisartan), chemical name: 4-{[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-yl]methanol Base} biphenyl-2-carboxylic acid, telmisartan is a new type of antihypertensive drug, which belongs to specific angiotensin II receptor (AT type I) antagonist, is a high-efficiency, long-acting, low It can be used alone or in combination with other antihypertensive drugs for the treatment of essential hypertension. It is one of the most ideal antihypertensive drugs because of its slow onset of action, long-lasting effect, and small side effects. one. [0003] Telmisartan is a white, odorless crystalline powder that is almost insoluble in water and aqueous solutions of pH 3-9. Slightly soluble in strong acid and soluble in strong alkali, due to these characteristics, there is often a pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4184A61K47/04A61K47/26A61K47/32A61K47/12A61P9/12
Inventor 陈成龙张洪范辉张信中
Owner BEIJING JINGFENG PHARMA GRP
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