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Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base

A technology of escitalopram, dispersible tablets, applied in the form of precipitation from solvents, to prepare the orodispersible tablets, 18] It has been found that escitalopram base is suitable for preparing the oral part, [0004] [0005 ] It is a selective medium field that can solve the problems of low friability, poor tablet strength of fast disintegrating tablets, and hindering the application of conventional packaging materials.

Inactive Publication Date: 2010-12-29
H LUNDBECK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many of these methods result in rapidly disintegrating tablets with poor tablet strength and low friability
This may prevent the application of conventional packaging materials as well as conventional packaging methods

Method used

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  • Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
  • Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
  • Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Embodiment 1, free release escitalopram free base from escitalopram oxalate

[0105] 704 g of escitalopram oxalate were placed in a 6 L three-necked flask equipped with a mechanical stirrer and a pressure compensating funnel. 3 L of water was added, followed by 600 mL of diethyl ether. The pH was adjusted to 9-9.5 by adding 27% w / w ammonia and the mixture was stirred for 1 / 2 hour. The phases were separated and the aqueous phase was re-extracted with 300 mL diethyl ether. The combined organic phases were washed twice with 300 mL of water and washed with MgSO 4 Drying, filtration and evaporation under vacuum at 40°C gave a light brown oil.

[0106] Yield: 542.5 g (98.4%)

Embodiment 2

[0107] Embodiment 2, the precipitation of escitalopram hydrobromide, the release of free base and the crystallization of base

[0108] Precipitation of escitalopram hydrobromide:

[0109] 3 kg of escitalopram free base (purified by HPLC: 99.16% (area %)) as a light brown oil dissolved in 12 kg of 2-propanol was added to 20 L with mechanical stirring, reflux condenser, scrubber , gas inlet and thermometer for thermostatic control of the reactor. The solution was heated to 40° C., and then HBr gas was injected into the solution until the pH was 3-4. The reaction is exothermic and the temperature in the reactor is maintained between 40-43°C. A small amount of seed crystals (escitalopram hydrobromide, 100-200 mg) was added and crystallization started within 10 minutes. The mixture was then cooled to 10° C. over 5 hours and kept at this temperature for a further 12 hours. The crystals were filtered off, rinsed on the filter with 3x1 L2-propanol, and dried to constant weight at...

Embodiment 3

[0120] Embodiment 3, the crystallization of escitalopram free base

[0121] 520 escitalopram free base (purity: 99.25%; HPLC) of light brown oily state was placed in 2 L equipped with mechanical stirrer, reflux condenser, N 2 Inlet / outlet and thermometer for thermostatic control of the reactor. 50 mL of ethyl acetate was added, and the mixture was heated to 35° C., followed by the addition of 1.3 L of heptane. When the solution was homogeneous, slow cooling to -5°C was initiated over 12 hours. When the temperature was 20°C, a small amount of seed crystals (escitalopram base) (10-20 mg) was added. Crystallization begins at about 10°C. The mixture was stirred at -5°C for another 5-7 hours, then the crystals were filtered off by filtration. The crystals were rinsed with 2 x 150 mL of heptane on the filter and dried under vacuum at 25°C to constant weight.

[0122] Yield: 485 g (93.3%)

[0123] HPLC purity of product: 99.58% (area %)

[0124] Melting point (DSC, onset): 45....

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Abstract

The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22N and an oral-disintegration time of less than 120s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100 DEG C, as well as a method for making such an orodispersible tablet.

Description

[0001] This application is a divisional application with application number 200680020039.3. [0002] The first aspect of the present invention relates to the known antidepressant escitalopram (escitalopram), namely S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-di The crystalline base of hydro-5-isobenzofurancarbonitrile, the formula of the base, the method of preparing and purifying escitalopram free base and its salts using the crystalline base or hydrobromide of escitalopram, through the Salt obtained by the method and formulation containing said salt. A second aspect of the present invention relates to orodispersible tablets comprising an active pharmaceutical ingredient absorbed in a water-soluble filler, wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., and a method for preparing the orodispersible tablet method. Background of the invention [0003] Escitalopram is a well known antidepressant that has been on the market ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/87A61K31/343A61K9/20A61P25/24
CPCC07D307/87A61K31/343A61P25/24A61P43/00A61K31/216C07B63/00A61K9/20
Inventor R·丹瑟H·彼得森O·尼尔森M·H·罗克H·伊莱亚森K·利杰格伦
Owner H LUNDBECK AS
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