Compositions containing omega-3 oil and uses thereof

Abstract

The invention provides pharmaceutical compositions containing omega-3 oil and a non-hydrophilic co-solvent that have an increased absorption rate. The pharmaceutical compositions may further contain one or more pharmaceutical organic molecules. The invention further provides kits containing these pharmaceutical compositions, methods for formulating pharmaceutical compositions containing omega-3 oil, and methods for decreasing the likelihood of developing cardiovascular disease, decreasing triglyceride or LDL cholesterol levels, decreasing pain or inflammation, treating diabetes, chronic pulmonary diseases, or irritable bowel syndrome, decreasing symptoms of an autoimmune disease or allergic conditions.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a Continuation of U.S. application Ser. No. 13 / 822,517, filed Apr. 12, 2013, which is the U.S. National Stage of International Application No. PCT / US2011 / 51698, filed Sep. 15, 2011, which claims benefit of U.S. Provisional Application No. 61 / 383,972, filed Sep. 17, 2010, each of which is hereby incorporated by reference.FIELD OF THE INVENTION[0002]The present invention relates to the field of pharmacology and molecular medicine. More specifically, the invention relates to pharmaceutical compositions containing omega-3 oil in co-solvents that are useful for treating, e.g., cardiovascular conditions, and / or as vehicles for delivering other therapeutic agents.BACKGROUND OF THE INVENTION[0003]Omega-3 oil is widely regarded as having certain therapeutic benefits primarily associated with cardiovascular disease. As the scientific community has become more comfortable with the safety and efficacy of omega-3 oils, the recommen...

AI Technical Summary

Benefits of technology

[0025]Desirably, these methods result in at least a 2-fold decrease in the time to optimal therapeutic effect or result in less gastric lesions than administration of a NSAID or a DMARD alone.

[0030]By the term “herbal-based oil” is meant an oil extracted from a herb plant (e.g., rosemary, basil, turmeric, and ginger). The herbal-based oil may inhibit cyclooxgenase COX-1 or COX-2 activity (e.g., mediate at least a 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 60%, 70%, 80%, 90%, or 95% decrease in COX-1 and / or COX-2 activity). These herbal oils contain mixtures of low potency cyclooxygenase (COX-1 and / or COX-2) inhibitors. These multi-component mixtures are additive in their effects. They are also synergistic because the various molecular inhibitors act / bind to different molecular sites on the enzyme (i.e., COX-1 and / or COX-2) surface and change the intrinsic ability of these enzymes to function. Multiple site inhibitors make these oils effective as therapeutic agents. Final concentrations of herbal extract in pharmaceutical compositions between 1% and 10% (by weight) are optimal. Combinations of multiple (e.g., two, three, four, or five) herbals oils are useful and provide greater efficacy.

[0036]By the term “therapeutic organic molecule” is meant a molecule that may be used to reduce the likelihood (e.g., at least a 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 60%, 70%, 80%, 90%, or 95% reduction) of developing a disease or to treat or ameliorate one or more symptoms of a disease in a subject (e.g., reduce the severity of one, two, three, four, or five symptoms by at least 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 60%, 70%, 80%, 90%, or 95%). A therapeutic organic molecule may have a molecular weight between 100 g / mole and 800 g / mole, a log P value greater than 2, or a melting point of below 200° C. In addition, therapeutic organic molecules may be soluble in a hydrophobic environment (e.g., a solvent). Non-limiting examples of therapeutic organic molecules include NSAIDs (e.g., ketoprofen), DMARDs (e.g., methotrexate), fenofibrate, a statin, and niacin.

[0037]By the phrase “decreasing the likelihood of developing” is meant a reduction (e.g., at least 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 50%, 60%, 70%, 80%, 90%, or 95%) for a subject or a patient population in the chance or rate of developing a specific disease (e.g., cardiovascular disease) by administering one or more pharmaceutical compositions compared to a subject or patient population not receiving the one or more pharmaceutical compositions. The methods of the invention may also reduce the likelihood of developing one or more (e.g., one, two, three, four, or five) symptoms of a disease (e.g., cardiovascular disease or diabetes) in a patient population or a subject receiving one or more of the provided pharmaceutical compositions.

[0038]By “treating” a disease in a subject is meant reducing the severity or duration of at least one symptom (e.g., one, two, three, four, or five symptoms) of the disease by administrating one or more pharmaceutical composition(s) to the subject.

[0040]By the phrase “one or more symptoms of diabetes” is meant one or more symptoms clinically observed for patients having diabetes (e.g., type I diabetes, type II diabetes, or pre-diabetes). Non-limiting examples of symptoms of diabetes include: frequent urination, unusual thirst, extreme hunger, unusual weight loss, extreme fatigue and irritability, frequent infections, blurred vision, tingling / numbness in extremities, recurring infections (e.g., skin, gum, and bladder infections), decreased insulin absorption or sensitivity (e.g., decrease by at least 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, or 60%), elevated blood glucose levels (e.g., one or more blood glucose readings of greater than 104 mg / dL), and increased glycated hemoglobin levels (e.g., HbA1C greater than 7.0%).

Problems solved by technology

It is difficult to ingest enough gel capsules to achieve this dosage.

Compliance and swallowing difficulties limit the ability of many patients from consistently taking an amount of omega-3 oil sufficient to elicit a therapeutic effect.

High grade liquid oils are available that allow patients to take these quantities of oils, but the dose volume, taste, and costs are negative factors.

Costs become prohibitive when chemically-altered or refined omega-3 oils from the natural state are used.

The weakness in the available oil products is that these compositions have not been optimized for absorption.

Despite the high quality of omega-3 oil contained within these products, the absorption efficiencies (time to maximum plasma concentration, t1 / 2 for absorption) of the products are not optimal.

The other marketed omega-3 products are also not optimized for absorption.

The conditions for dissolution and absorption are not optimal for these products, and thus, the efficiency of integration into cell membranes and triglyceride storage forms is not optimal.

The gel caps are inferior to Lovaza / Omacor (described above) and also suffer from a reduced efficiency of absorption.