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Compositions Comprising Nebivolol

a technology of nebivolol and nebivolol, which is applied in the direction of drug compositions, biocide, cardiovascular disorders, etc., can solve the problems of increasing the risk of developing hypertension, so as to improve the compliance of blood vessels, improve endothelial dysfunction, and increase the level of nitric oxid

Inactive Publication Date: 2009-09-10
MYLAN PHARMA INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012]Even though nebivolol has β-blocking properties, nebivolol is different from other classic β-blockers in that it is highly selective to the β1 adrenergic receptors and also has vasodilating effects related to its effect on endothelial nitric oxide. It is believed that nebivolol increases the levels of nitric oxide within the vascular endothelium through the L-arginine-nitric oxide pathway and has been shown to improve endothelial dysfunction and improve compliance of blood vessels. Nebivolol has also been shown to have antioxidant characteristics which are favorable to the normal functioning of the vascular endothelium. These characteristics make nebivolol an effective antihypertensive agent with favorable effects on the vascular endothelium and cardiovascular system. Nebivolol has been shown to be beneficial in the treatment of cardiovascular diseases such as hypertension, congestive heart failure, arterial stiffness and endothelial dysfunction. In part, the present invention features a composition comprising nebivolol and another cardiovascular agent that is believed to work via a different mechanism.

Problems solved by technology

In addition, individuals with blood pressure of 120 / 80 mmHg or higher are at increased risk of developing hypertension and are considered to be in a “pre-hypertension” state.
The risk of developing hypertension increases more dramatically with increasing age.

Method used

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  • Compositions Comprising Nebivolol
  • Compositions Comprising Nebivolol
  • Compositions Comprising Nebivolol

Examples

Experimental program
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Effect test

example 1

Measurements of NO Release from Human Endothelium

[0155]All measurements presented were recorded in vitro using a sensitive porphyrinic probe, as previously described. Malinski T, Taha Z., Nature. 1992; 358:676-678; Malinski T, Czuchajowski L., Methods in Nitric Oxide Research. 1996:319-339. NO release was measured directly from HUVEC. HUVEC cells from Black and White donors were grown in Ham's F12K medium with 2 mM L-glutamine adjusted to contain 1.5 g / L sodium bicarbonate and supplemented with 0.1 mg / ml heparin and 0.03-0.05 mg / ml endothelial cell growth supplement (ECGS)+10% fetal bovine serum. The HUVEC cells were kept in an atmosphere of elevated CO2 concentration (5%). Nebivolol was obtained from Mylan Laboratories (Morgantown, W. Va.).

[0156]All measurements of endothelial NO release were conducted in Hank's balance solution at 37° C. Cell wells were transferred to a Faraday cage and a porphyrinic sensor (diameter 0.5 mm) was positioned at a distance of 5±2 μm from the surface ...

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PUM

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Abstract

Nebivolol has been shown to be beneficial in the treatment of cardiovascular diseases such hypertension, congestive heart failure, arterial stiffness and endothelial dysfunction. The present invention features a pharmaceutical composition comprising nebivolol and at least one other active agent, wherein the at least one other active agent is a cardiovascular agent.

Description

[0001]This application is a divisional of U.S. Non-Provisional patent application Ser. No. 11 / 141,235, filed May 31, 2005, which is based on and claims priority from U.S. Provisional Patent Application Ser. No. 60 / 577,423, Eric Davis, John O'Donnell, Peter Bottini, filed Jun. 4, 2004; the disclosures of both are hereby incorporated by reference in their entirety.TECHNICAL FIELD[0002]This invention relates to compositions comprising nebivolol and one or more other active agent. More particularly, this invention relates to compositions comprising nebivolol and one or more cardiovascular agents for the treatment and / or prevention of cardiovascular diseases.BACKGROUND OF THE INVENTION[0003]Hypertension is a major health concern in the US. Approximately 50 million Americans have elevated blood pressure defined as a systolic blood pressure (SBP)≧140 mmHg or a diastolic blood pressure (DBP)≧90 mmHg. In addition, individuals with blood pressure of 120 / 80 mmHg or higher are at increased risk...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/41A61P9/00A61K31/35A61K31/353
CPCA61K31/353A61K31/35A61K45/06A61K31/403A61K31/401A61K2300/00A61K31/352A61K31/155
Inventor DAVIS, ERICO'DONNELL, JOHNBOTTINI, PETER
Owner MYLAN PHARMA INC
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