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Tilmisartan salt and its prepn

A technology of telmisartan and sodium salt, which is applied in the field of telmisartan salt and its preparation, can solve the problems of low solubility, low dissolution rate and strong water absorption of telmisartan raw materials, and achieve high promotion and application prospects , High dissolution rate, easy preparation

Inactive Publication Date: 2004-11-24
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Telmisartan crude drug solubility is less, after making preparation, its stripping rate is lower, and patent CN1336920A once reported that telmisartan is dissolved in 0.1mol / L NaOH, is transformed into a kind of homogeneous and completely free by spray drying. Qualitative particles, but samples prepared by this method are more hygroscopic

Method used

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  • Tilmisartan salt and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 4'-[(1,4'-dimethyl-2'-n-propyl[2,6'-di-1hydro-benzimidazol]-1'-yl)methyl]-[1,1' -Biphenyl]-2-carboxylic acid sodium salt

[0027] In a 250ml reaction flask, add 10g (0.0195mol) Telmisartan (0.0195mol), 0.75g (0.0189mol) NaOH and 100ml water, stir for 1 hour (30°C), filter, remove insoluble matter, concentrate to a small volume, add ethanol 30ml, concentrated, added 30ml of n-hexane to wash, poured off, added 30ml of ethanol, concentrated, repeated again, concentrated to dryness to obtain 9.9g of telmisartan sodium salt, yield 95.2%. Melting point: 223-225°C.

[0028] Elemental Analysis: C 33 h 29 N 4 o 2 Na·H 2 O calculated value: C71.48 H5.10 N10.11

[0029] Experimental value: C71.42 H5.08 N10.22

Embodiment 2

[0031] 4'-[(1,4'-dimethyl-2'-n-propyl[2,6'-di-1hydro-benzimidazol]-1'-yl)methyl]-[1,1' -Biphenyl]-2-carboxylate potassium salt

[0032] In a 250ml reaction bottle, add 10g (0.0195mol) Telmisartan (0.0195mol), 1.06g (0.0188mol) KOH and 100ml water, stir for 1 hour (30°C), filter, remove insoluble matter, concentrate to a small volume, add ethanol 30ml, concentrated, added 30ml of n-hexane to wash, poured off, added 30ml of ethanol, concentrated, repeated again, concentrated to dryness to obtain 10.6g of telmisartan potassium salt with a yield of 95.6%. Melting point: 203-205°C.

[0033] Elemental Analysis: C 33 h 29 N 4 o 2 K·H 2 O Calculated value: C69.04 H5.40 N9.76 Experimental value: C69.01 H5.28 N9.88

Embodiment 3

[0035] The fine powder of raw materials and auxiliary materials is evenly mixed and sieved, and 5% polyvinylpyrrolidone solution is added to make granules and dried. After the dry granules are sized, magnesium stearate is added, mixed evenly, and then compressed into tablets.

[0036] mg / tablet

[0037] Telmisartan sodium salt 20

[0038] Lactose 170

[0039] Sodium carboxymethyl starch 10

[0040] Meglumine 8

[0041] Magnesium Stearate 2

[0042] 5% polyvinylpyrrolidone solution appropriate amount

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Abstract

The Tilmisartan salt of the present invention is salt formed with Tilmisartan and alkali metal, alkali earth metal, pharmaceutically acceptable amine, amino acid. It may be sodium salt, potassium salt, calcium salt, magnesium salt and amine salt, preferably sodium salt, potassium salt or tert-butyl amine salt. The preparation of Tilmisartan salt includes the following steps: reaction between Tilmisartan and organic alkali, inorganic alkali, arginine or lysine in organic solvent or water to produce target product, and collecting Tilmisartan salt. The Tilmisartan salt may be used to replace available Tilmisartan.

Description

technical field [0001] The invention relates to a telmisartan salt and a preparation method thereof. Background technique [0002] European patent EP502314B1 discloses a compound, telmisartan, and discloses a general structural formula, as follows: [0003] [0004] Telmisartan and its physiologically acceptable salts have valuable pharmacological properties. It is an angiotensin II antagonist, which due to its pharmacological properties can be used in the treatment of hypertension and myocardial insufficiency, in the treatment of ischemic peripheral circulation diseases, myocardial ischemia (angina). [0005] Telmisartan crude drug solubility is less, after making preparation, its dissolution rate is lower, and patent CN1336920A once reported that telmisartan is dissolved in 0.1mol / L NaOH, is transformed into a kind of homogeneous and completely free by spray drying. Qualitative particles, but the samples prepared by this method are more hygroscopic. Contents of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P9/10A61P9/12C07D209/14
Inventor 钟静芬孟小弟郭晔堃陈国梁时惠麟
Owner SHANGHAI INST OF PHARMA IND
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