Thromboxane Receptor Antagonists in AERD/Asthma

a thromboxane receptor and asthma technology, applied in the field of thromboxane receptor antagonists, can solve the problems of inability to respond to conventional treatments, inability to help many patients with aerd, so as to reduce the need for rescue medications and reduce the symptoms of aspirin desensitization

Inactive Publication Date: 2017-01-05
CUMBERLAND PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0014]It is an object of the invention to reduce rescue medications needed as a result of an aspirin-induced reaction in a human patient suffering from AERD.
[0015]It is another object of the invention to reduce the symptoms of aspirin desensitization in AERD patients.

Problems solved by technology

Such patients often do not respond to conventional treatments.
However, aspirin desensitization does not help many AERD patients.

Method used

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  • Thromboxane Receptor Antagonists in AERD/Asthma

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0082]In this example, ifetroban sodium tablets are prepared with the following ingredients listed in Table 1:

TABLE 1IngredientsPercent by weightNa salt of Ifetroban35Mannitol50Microcrystalline Cellulose8Crospovidone3.0Magnesium Oxide2.0Magnesium Stearate1.5Colloidal Silica0.3

[0083]The sodium salt of ifetroban, magnesium oxide, mannitol, microcrystalline cellulose, and crospovidone is mixed together for about 2 to about 10 minutes employing a suitable mixer. The resulting mixture is passed through a #12 to #40 mesh size screen. Thereafter, magnesium stearate and colloidal silica are added and mixing is continued for about 1 to about 3 minutes.

[0084]The resulting homogeneous mixture is then compressed into tablets each containing 35 mg, ifetroban sodium salt.

example ii

[0085]In this example, 1000 tablets each containing 400 mg of Ifetroban sodium are produced from the following ingredients listed in Table 2:

TABLE 2IngredientsAmountNa salt of Ifetroban400gmCorn Starch50gGelatin7.5gMicrocrystalline Cellulose (Avicel)25gMagnesium Stearate2.5g

example iii

[0086]In this example. An injectable solution of ifetroban sodium is prepared for intravenous use with the following ingredients listed in Table 3:

TABLE 3IngredientsAmountIfetroban Sodium2500mgMethyl Paraben5mgPropyl Paraben1mgSodium Chloride25,000mgWater for injection q.s.5liter

[0087]The sodium salt of ifetroban, preservatives and sodium chloride are dissolved in 3 liters of water for injection and then the volume is brought up to 5 liters. The solution is filtered through a sterile filter and aseptically filled into pre-sterilized vials which are then closed with pre-sterilized rubber closures. Each vial contains a concentration of 75 mg of active ingredient per 150 ml of solution.

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Abstract

The present invention is directed to methods of treating AERD (aspirin exacerbated respiratory disease) and/or asthma via the administration of a thromboxane receptor antagonist to a patient in need thereof.

Description

FIELD OF THE INVENTION[0001]The present invention is related to the use of thromboxane receptor antagonists (e.g., Ifetroban) in the treatment of AERD (aspirin exacerbated respiratory disease) and asthma; and pharmaceutical compositions for the treatment of the same.BACKGROUND OF THE INVENTION[0002]Aspirin Exacerbated Respiratory Disease (AERD) is a chronic medical condition that consists of asthma, recurrent sinus disease with nasal polyps, as well as a sensitivity to aspirin and other non-steroidal anti-inflammatory drugs (NSAIDs). Patients suffering from typically develop reactions triggered by aspirin or other NSAIDs. These reactions include, but are not limited to increased nasal congestion or stuffiness; eye watering or redness; cough, wheezing, or chest tightness; frontal headache or sensation of sinus pain; flushing and / or a rash; nausea and / or abdominal cramping; and a general feeling of malaise, sometimes accompanied by dizziness.[0003]From a scientific perspective, AERD i...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/422
CPCA61K31/422A61P11/06A61P43/00A61P11/00A61K31/616
Inventor PAVLIV, LEO
Owner CUMBERLAND PHARM INC
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