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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  • Abstract
  • Description
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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

Method used

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  • Legemiddel inneholdende vardenafilhydrokloridtrihydrat
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  • Legemiddel inneholdende vardenafilhydrokloridtrihydrat

Examples

Experimental program
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Effect test

Example

[0053] Comparative Example 1 and Example 2 : The improved disintegration of tablets prepared by the conventional preparation method of tumbler granulation and coating method and the tablet of the present invention

[0054] 216 g of micronized vardenafil HCl was mixed with 605 g of microcrystalline cellulose and 43.2 g of crospovidone. 2101 g of microcrystalline cellulose and 132 g of crospovidone were added thereto and mixed, and then mixed with 350 g of microcrystalline cellulose, 17.5 g of highly dispersed silica, and 35 g of magnesium stearate. The mixture was compressed into tablets having a diameter of 6 mm and a tablet weight of 87 mg (corresponding to 5 mg of vardenafil base) using a rotary tablet press. In the coating device, 43.5 mg of a coating mixture containing 4.5% hypromellose, 1.5% polyethylene glycol 400, 1.23% titanium dioxide, 0.25% yellow iron oxide and 0.02% red iron oxide was sprayed to each tablet. Suspension.

Example

[0055] Comparative Example 1

[0056] Vardenafil hydrochloride present in the tablet is partly trihydrate and partly dehydrated form (1 to 4 modified form). The disintegration time of the tablet is 2 minutes.

Example Embodiment

[0057] Example 2

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

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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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