Legemiddel inneholdende vardenafilhydrokloridtrihydrat

A technology of vardenafil hydrochloride and trihydrate, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, sugar-coated pills, etc., can solve problems such as inability to separate vardenafil HCl, and achieve rapid disintegration and clear definition , the effect of fast dissolution rate

Active Publication Date: 2005-10-12
BAYER IP GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, however, Vardenafil HCl cannot be prepared or isolated in pure form because the polymorphic forms of Vardenafil HCl each absorb a small amount of water and thus exist as a mixture of polymorphic forms and hydrates. Non-HCl polymorphic forms

Method used

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  • Legemiddel inneholdende vardenafilhydrokloridtrihydrat
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  • Legemiddel inneholdende vardenafilhydrokloridtrihydrat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0058] The tablet has a 150m 3 / h Rehydration for 4 hours in a fluidized bed granulator with inlet air at a temperature of 30° C. and a water content of 19 g / kg (corresponds to a relative air humidity of 70%). Therefore, the modified form of vardenafil HCl in the tablet of the present invention is equivalent to the trihydrate. Tablets now disintegrate in just 1 / 2 minute.

Embodiment 3

[0059] Example 3: The stability of the prepared tablet of the present invention

[0060] 28.4 kg of micronized vardenafil HCl trihydrate were mixed with 69.6 kg of microcrystalline cellulose and 5.16 kg of sieved crospovidone in a mechanical mixer. This mixture was mixed with 182 kg microcrystalline cellulose and 9.84 kg crospovidone in a tank mixer and granulated by drum dry granulation. After mixing 1.50 kg of highly disperse silicon dioxide and 3.00 kg of magnesium stearate, tablets with a mass of 125 mg and a diameter of 7 mm were prepared with a rotary tablet press. The uncoated tablet was coated with 5.74 kg hypromellose, 1.91 kg polyethylene glycol 400, 1.57 kg titanium dioxide, 319 g yellow iron oxide, 25.5 g red iron oxide in a commercially available coating system And the suspension of 118kg purified water carries out coating. The modified form of vardenafil HCl in this coated tablet does not correspond to the trihydrate form, therefore, it represents an undefine...

Embodiment 4

[0062] Example 4: Release of Active Ingredient from Tablets Prepared According to the Invention

[0063] 336g vardenafil HCl was mixed with 2216g microcrystalline cellulose and 134g crospovidone and it was dry granulated. The granules were transferred, then mixed with 283 g microcrystalline cellulose, 16 g crospovidone and 15 g magnesium stearate and compressed to a diameter of 5 mm and a mass of 48 mg (equivalent to 5 mg vardenafil base per tablet ) tablets. The tablet was provided with a white coating of 57.4 g hypromellose, 19.1 g macrogol 4000 and 19.1 g titanium dioxide and stored in an oven at 25° C. and a relative air humidity of 80% for 4 sky. The modification of vardenafil HCl in the tablet corresponds to the trihydrate form.

[0064] As shown by the release data in Table 1, the tablets of the invention prepared in this way released the active very rapidly, although all of the vardenafil HCl in the final tablet reverted to the trihydrate form. Element.

[0065]...

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Abstract

Production of solid medicaments (A) containing vardenafil hydrochoride (I) in the form of the trihydrate involves using (I) of any water content in the production of (A) and converting (I) into the trihydrate form at an intermediate processing stage or in the final product. An independent claim is included for the medicaments (A) (specifically in coated tablet form) obtained by the process. - ACTIVITY : Vasotropic. - MECHANISM OF ACTION : None given in the source material.

Description

technical field [0001] The present application relates to a medicament comprising vardenafil hydrochloride in solid form, substantially in trihydrate form, and a process for its preparation. Background technique [0002] The pharmaceutical active ingredient vardenafil (IUPAC-name: 2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl) in the form of Examples 19, 20 and 336 in WO99 / 24433 acyl]phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one), vardenafil hydrochloride and valdenafil hydrochloride Denafil trihydrate and its use for the treatment of erectile dysfunction are described. [0003] Vardenafil hydrochloride has been found to exist in four different polymorphic forms (anhydrous modified form I with a melting point of 217°C, modified form II with a melting point of 190°C, modified form III with a melting point of 183-186°C , modified form IV) with a transformation point of 166° C. and preferably does not form any of these polymorphs at room temperature. Furtherm...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/28A61K31/53A61P15/10
CPCA61K9/2893C07D487/04A61K31/53A61K9/2095A61K9/28A61K9/2866A61P15/00A61P15/10Y02A50/30
Inventor P·谢尔诺A·格鲁嫩伯格A·奥姆R·贝林豪森E·福勒斯J·-O·亨克
Owner BAYER IP GMBH
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