Solid oral preparation containing telmisartan and preparation method thereof

A technology for telmisartan and oral preparations, which is applied in the direction of medical preparations containing active ingredients, pill delivery, pharmaceutical formulations, etc., and can solve the problem of losing time and labor for fluidized bed granulation, prolonging the time of fluidized bed granulation, Increased problems such as explosions

Active Publication Date: 2011-07-06
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent CN200710041363.X can indeed improve the dissolution of telmisartan by dissolving telmisartan, alkaline reagent and povidone together in aqueous solution or alcohol aqueous solution as a binder granulation method, but this method also has two problems. Insufficiency: at first more alkaline reagents are used in this method, and the phenomenon that gastric juice partial alkali causes indigestion unavoidably can take place after patient takes; Secondly inventor finds in practice that the aqueous solution of telmisartan and alkaline reagent is relatively Viscous, adding povidone will increase the viscosity of the solution, and it is very difficult to use this viscous solution for fluidized bed granulation, and a little carelessness in the process will ca

Method used

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  • Solid oral preparation containing telmisartan and preparation method thereof
  • Solid oral preparation containing telmisartan and preparation method thereof
  • Solid oral preparation containing telmisartan and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]

[0032] 200g of telmisartan, 15.5g of sodium hydroxide and 8.5g of meglumine were dissolved in 200g of water to obtain a homogeneous solution; 60g of hypromellose, 681.8g of mannitol, 180g of corn starch, 36.0g of Mix povidone through a φ2.0mm rotary sieve to obtain a granule mixture; place the granule mixture in a fluidized bed and spray the above homogeneous solution to obtain wet granules; dry the wet granules at 60°C and pass through a φ2.0mm rotary sieve for granulation to obtain Dry granules; the dry granules are mixed with magnesium stearate and compressed into tablets.

[0033] According to dissolution assay method (Chinese Pharmacopoeia 2005 edition appendix XC second method), with the pH1.0 hydrochloric acid solution of 900ml as dissolution medium, rotating speed is 75rpm, to embodiment 1 sheet and import telmisartan sheet (mecasu , manufacturer: Boehringer Ingelheim, Germany) for dissolution testing, and the results are shown in Table 1 and figure 1 .

...

Embodiment 2

[0042]

[0043] 200g of telmisartan and 14.0g of sodium hydroxide were dissolved in about 400g of water to obtain a homogeneous solution; Sodium is mixed together through a φ2.0mm rotary sieve to obtain a granule mixture; the granule mixture is placed in a fluidized bed, and the above homogeneous solution is sprayed to obtain wet granules; the wet granules are dried at 60°C and passed through a φ2.0mm rotary sieve for granulation to obtain dry Granules; add the above-mentioned magnesium stearate to the dry granules, mix well and compress into tablets.

Embodiment 3

[0045]

[0046] The telmisartan of 200g, 16.0g sodium hydroxide and 24.0g meglumine are jointly dissolved in about 400g water to obtain a homogeneous solution; 2048g mannitol, 1600g microcrystalline cellulose and 40.0g crospovidone Mix with a φ2.0mm rotary sieve to obtain a granule mixture; place the granule mixture in a fluidized bed and spray the above-mentioned homogeneous solution to obtain wet granules; dry the wet granules at 60°C and pass through a φ2.0mm rotary sieve for granulation to obtain dry granules; The granules are added with the above-mentioned magnesium stearate, mixed evenly, and then compressed into tablets.

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Abstract

The invention provides a solid oral preparation without a surfactant. The solid oral preparation comprises the following components in percentage by weight: 5-25% of telmisartan, an alkaline reagent and the balance of pharmaceutically acceptable vectors, wherein the weight of the alkaline reagent is equal to 7-20% of that of telmisartan. The invention also provides a method for preparing the solid oral preparation. The preparation prepared by the method can be quickly and sufficiently released in the psychophysical pH range of gastrointestinal tracts; and compared with the prior art, the preparation method has the advantages that the process is simpler, the quality of the soli oral preparation is more stable, the cost is greatly saved, and the efficiency is improved.

Description

technical field [0001] The present invention relates to a solid oral preparation containing telmisartan, more specifically to a tablet containing telmisartan. The invention also provides a tablet preparation method suitable for industrial production. Background technique [0002] Telmisartan is an angiotensin II receptor antagonist developed for the treatment of hypertension and other medical conditions. Its chemical name is 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid common chemical name. The CAS registry number is 144701-48-4. Molecular formula is C 33 h 30 N 4 o 2 , and its molecular weight is 514.63. has the following structure. [0003] [0004] Telmisartan tablets are products developed by Boehringer Ingelheim, Germany, and the trade name is Mecasu The preparation specification is 20mg / 40mg / 80mg tablet. Mecaso It was first listed in the United States in 1999, listed in the UK in 2000, and li...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61K9/20A61P9/12
Inventor 陈浩彭俊清李巧霞胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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