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Endothelin antagonist and beta receptor blocking agent as comblined preparation

A technology of endothelin antagonists and receptor blockers, which is applied in the field of new drug combination preparations and can solve problems such as unsatisfactory activity

Inactive Publication Date: 2004-05-12
ABBVIE DEUTSHLAND GMBH & CO KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the activity of the combination of these active compounds is not satisfactory

Method used

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  • Endothelin antagonist and beta receptor blocking agent as comblined preparation
  • Endothelin antagonist and beta receptor blocking agent as comblined preparation
  • Endothelin antagonist and beta receptor blocking agent as comblined preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Coated tablets were prepared with the following composition:

[0035] Compound A 100.0mg

[0036] Bucinolol 10.0mg

[0037] Anhydrous Lactose 30.0mg

[0038] Microcrystalline Cellulose 30.0mg

[0039] Polyvinylpyrrolidone 20.0mg

[0040] Magnesium Stearate 5.0mg

[0041] Macrogol 6000 0.8mg

[0042] Iron Oxide Yellow 1.2mg

[0043] Titanium dioxide 0.3mg

[0044] Talc powder 0.7mg

[0045] Compound A, bucinolol, lactose, cellulose and polyvinylpyrrolidone were wet granulated and dried. The granules are sieved, blended with magnesium stearate, and the tablet-ready mixture is compressed into oval tablet cores each weighing 190.0 mg. The tablet cores are then coated until the final weight of the coated tablet reaches 200 mg.

Embodiment 2

[0047] Hard gelatin capsules were prepared having the following composition:

[0048] Compound A 100.0mg

[0049] Bucinolol 30.0mg

[0050] Lactose crystals 18.0mg

[0051] Polyvinylpyrrolidone 15.0mg

[0052] Microcrystalline Cellulose 17.5mg

[0053] Sodium carboxymethyl starch 10.0mg

[0054] Talc powder 9.0mg

[0055]Magnesium Stearate 3.0mg

[0056] The first 5 components were wet granulated and dried. The granules are mixed with sodium carboxymethyl starch, talc and magnesium stearate and the resulting mixture filled into size 1 hard gelatin capsules.

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Abstract

The invention relates to a combination consisting of endothelin-antagonists and beta receptor blocking agents. Said combination is suitable for the treatment of diseases.

Description

technical field [0001] The present invention relates to novel pharmaceutical combination preparations suitable for the treatment of diseases based on vasoconstriction, comprising beta-blockers and endothelin antagonists. Background technique [0002] Combination preparations comprising a beta-blocker and an endothelin antagonist suitable for the treatment of diseases based on vasoconstriction have been disclosed (WO 92 / 13545). However, the activity of combinations of these active compounds is not satisfactory. [0003] Combinations with improved properties have now been found. Contents of the invention [0004] The present invention provides a combination of an endothelin antagonist of formula I and a beta-blocker: [0005] [0006] Wherein the substituents are defined as follows: [0007] R 1 is C 1 -C 4 -Alkyl, C 1 -C 4 - alkoxy; [0008] R 2 is C 1 -C 4 -Alkyl, C 1 -C 4 - alkoxy; [0009] R 3 is a C that can be substituted by phenyl 1 -C 8 -Alkyl, w...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/4045A61K31/505A61K45/06A61P9/00A61P9/04A61P9/10A61P9/12A61P13/12
CPCA61K45/06A61P13/12A61P9/00A61P9/04A61P9/10A61P9/12A61K31/505
Inventor M·基申加斯特K·明特尔
Owner ABBVIE DEUTSHLAND GMBH & CO KG
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