Drugs with improved pharmacokinetic properties

A technology of pharmaceutical preparation and trihydrate, which is applied in the field of new vardenafil pharmaceutical preparations, and can solve the problems of the decrease of vardenafil plasma concentration and the like

Active Publication Date: 2016-06-08
BAYER IP GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The increase in plasma concentration especially after a few hours of administration of a pharmaceutical preparation that disintegrates and releases particularly rapidly is unexpected, since a rapid increase and plasma concentration of vardenafil may occur through accelerated disintegration of the active ingredient faster fall in concentration

Method used

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  • Drugs with improved pharmacokinetic properties
  • Drugs with improved pharmacokinetic properties

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Experimental program
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Effect test

Embodiment 6

[0028] Demonstration of increased bioavailability in rapidly disintegrating tablets in the oral cavity according to the invention

[0029] Each of the 12 probands was administered oral rapidly disintegrating tablets consisting of the following: 11.85 mg of vardenafil hydrochloride trihydrate, 0.55 mg of yellow iron oxide, 0.075 mg of red iron oxide Iron, 0.75mg of apricot flavor, 0.125mg of neohesperidin dihydrochalcone, 2.50mg of aspartame, 0.625mg of highly dispersible silicon dioxide, 3.125mg of magnesium stearate and 105.4mg of At 25° C., about 10.4 mg of the active ingredient used is dissolved in 10 ml of physiological saline (corresponding to 8.8 mg of vardenafil), which is about 88% of the dose. At 37° C., in 900 ml of physiological saline, in a USP paddle stirring device with a rotating speed of 50 rpm, the release rate of the active ingredient within 5 minutes was 73%. Thereby, the solubility and dissolution rate criteria of the present invention are met. Compared ...

Embodiment 7

[0031] Demonstration of increased bioavailability in rapidly disintegrating tablets in the oral cavity according to the invention

[0032] Each of the 11 probands was administered oral rapidly disintegrating tablets consisting of 5.93 mg of vardenafil hydrochloride trihydrate, 0.352 mg of yellow iron oxide, 0.048 mg of red iron oxide Iron, 0.48mg of apricot flavor, 0.08mg of neohesperidin dihydrochalcone, 1.60mg of aspartame, 0.40mg of highly dispersible silicon dioxide, 2mg of magnesium stearate and 69.11mg of The active ingredient used is approximately 91% soluble in 10 ml of physiological saline at 25°C. The release rate of the active ingredient was 78% in 900 ml of physiological saline at 37° C. and in a USP paddle stirring apparatus at a speed of 50 rpm within 5 minutes. Thereby the solubility standard and dissolution rate standard of the present invention are realized. As a comparison, in the crossover approach, a conventional tablet swallowed with water, consisting o...

Embodiment 8

[0034] Demonstration of increased bioavailability in rapidly disintegrating tablets in the oral cavity according to the invention

[0035] The following ingredients were mixed in a plow mixer: 697 g of micronized vardenafil hydrochloride trihydrate, 500 g of a coloring material composed of 4.4% yellow iron oxide, 0.6% red iron oxide and 95% A premix consisting of 30g of apricot flavor, 5g of neohesperidin dihydrochalcone, 100g of aspartame and 3518g of The powder mixture was mixed with 25 g of highly disperse silicon dioxide in a drum mixer (Freifallmischer) and sieved through a 0.5 mm sieve. This mixture was then blended with 125 g of magnesium stearate in a tumbler mixer for 5 minutes. The final powder mixture was compressed on a tablet machine into round tablets weighing 170 mg, 8 mm in diameter and about 35N breaking strength. As a comparison, in the crossover approach, conventional tablets swallowed with water were administered, consisting of the following components:...

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Abstract

The application relates to a novel vardenafil pharmaceutical preparation, which disintegrates rapidly in the oral cavity, improves bioavailability, and causes a plateau-like plasma concentration change process, and a preparation method thereof.

Description

[0001] This case is a divisional application of application number 200680006596.X. technical field [0002] The application relates to a novel vardenafil pharmaceutical preparation, which disintegrates rapidly in the oral cavity, improves bioavailability, and causes a plateau-like plasma concentration change process, and a preparation method thereof. Background technique [0003] Imidazotriazine derivatives, such as vardenafil, and their use as phosphodiesterase inhibitors of cGMP, and their spectrum of activity are known (eg WO99 / 24433) and can be Trademark purchased. However, its therapeutic use is compromised by the low bioavailability of vardenafil, approximately 14%, and its sharp drop in plasma concentration one hour after administration of vardenafil. In principle, low bioavailability will cause high plasma concentration variation among different individuals. In addition, the dose must be increased to achieve a certain exposure (Exiposition). The sharp decrease in ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/53A61K9/20
CPCA61K9/006A61K31/53A61K9/0056A61P15/00A61P15/10A61P43/00A61K9/20A61K9/2013A61K9/2018
Inventor P·瑟诺R·黑尼格K·波利早内丰
Owner BAYER IP GMBH
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