Combination of fenofibrate and coenzyme q10 for the treatment of endothelial dysfunction

• US 20040022778A1
• Filed: 04/17/2003
• Published: 02/05/2004
• Est. Priority Date: 10/26/2000
• Status: Active Grant

• Current Assignee: Fournier Laboratories Ireland Limited (Abbvie Incorporated)
• Original Assignee: Fournier Laboratories Ireland Limited (Abbvie Incorporated)
• Inventors: Watts, Gerald Franus, Playford, David Alan
• Granted Patent: US 7,410,983 B2
• Time in Patent Office: Days
• US Class Current: 424/94.1
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/12 Ketones
• CPC Class Codes: A61K 31/215 of carboxylic acids
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 39/06 Free radical scavengers or antioxidants
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/08 Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock artificial tears A61P27/04
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/04 Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• CPC Class Codes: A61P 9/06 Antiarrhythmics
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives
• CPC Class Codes: A61P 9/14 Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Abstract

The present invention relates to a combination of a peroxisome proliferator activated receptor (PPAR) activator and a benzoquinone and their use in treating and/or preventing disorders characterized by endothelial dysfunction, such as cardiovascular disease, strokes and myocardial infarction. According to a preferred embodiment of the invention the benzoquinone or precursor thereof is a ubiquinone or precursor thereof, more preferably, coenzyme Q₁₀ or a precursor thereof, and the PPAR activator is a librate or a thiazolidinedionc, more preferably fenolibrate.

Claims

1. A composition comprising:

a peroxisome proliferator activated receptor (PPAR) activator selected from a fibrate, a thiazolidinedione, and a pharmaceutically acceptable salt thereof;

a benzoquinone selected from a ubiquinone, a precursor thereof capable of being metabolized In the human or animal body to said ubiquinone and a pharmaceutically acceptable salt thereof.

2. A composition according to claim 1 wherein the above mentioned ubiquinone or precursor thereof is coenzyme Q₁₀ or a precursor thereof.

3. A composition according to claim 1 or 2 wherein the above mentioned PPAR activator is fenofibrate.

4. A composition according to claim 3 wherein the above mentioned fenofibrate is co-micronlsed with a solid surfactant.

5. A composition according to claim 4 wherein the above mentioned solid surfactant is sodium lauryl sulphate.

6. A pharmaceutical composition comprising a composition according to any one of claims 1 to 5, together with a pharmaceutically acceptable carrier or diluent.

7. A method for producing a pharmaceutical composition as claimed in claim 6, which comprises admixing said PPAR activator and benzoquinone with a pharmaceutically acceptable carrier or diluent.

8. A composition comprising a peroxisome proliferator activated receptor (PPAR) activator and a benzoquinone as defined in any of claims 1 to 5 for use in therapy.

9. The use of a composition as claimed in any of claims 1 to 5 for the manufacture of a medicament for use in treating a disorder characterized by endothelial dysfunction.

10. The use according to claim 9 wherein the above mentioned disorder is selected from the group consisting of cardiovascular disease, hypertension, stroke, myocardial infarction, peripheral vascular disease, angina pectoris, cardiac failure, diastolic and/or systolic ventricular dysfunction, macro and microangiopathy in patients with diabetes, and tissue damage related to ischemica or reperfusion.

11. The use according to claim 9 or 10 wherein the above mentioned medicament is in a form adapted for an administration of said peroxisome pro liferator activated receptor (PPAR) activator and benzoquinone in a separate, sequential or concomitant manner.