# US 8,772,270 B2 · Treatment methods requiring phyto-ingredients

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- Number: US 8,772,270 B2
- Document ID: US8772270B2
- Status: Granted
- Kind: B2
- Application number: 11/673,726
- Filed: 2007-02-12
- Published: 2007-08-23
- Granted: 2014-07-08
- Earliest claimed: 2004-08-10
- Assignees: Enzymotec Ltd.
- Applicants: Avidor Shulman; Dori Pelled; Tzafra Cohen; Orly Farkash
- Inventors: Avidor Shulman; Dori Pelled; Tzafra Cohen; Orly Farkash
- Web page: https://patentgrep.com/patent/US8772270B2

## CPC

- A23D 9/013: Other fatty acid esters, e.g. phosphatides
- A23L 33/11: Plant sterols or derivatives thereof, e.g. phytosterols
- A23L 33/12: Fatty acids or derivatives thereof
- A61K 31/20: having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K 31/23: of acids having a carboxyl group bound to a chain of seven or more carbon atoms
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- A61P 13/08: of the prostate
- A61P 17/00: Drugs for dermatological disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 27/12: for cataracts
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/06: for tuberculosis
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 37/04: Immunostimulants
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A23D: EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS OR COOKING OILS (preservation thereof A23B20/00; production, refinement or preservation of animal or vegetable fats or oils C11B, C11C)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

The invention provides methods for treatment of conditions which require phytosterol therapy without adversely affecting the bioavailability of lipophilic vitamins or lipophilic drugs. The method includes administering a mixture of phytosterol ester(s) (PS-E) and 1,3-diglyceride(s) (DAG) dissolved in an edible oil or fat. The invention also provides a method of improving weight management and a method of treating metabolic conditions that result in overweight. Dietary nutrients, food supplements and food articles containing the mixture are also provided.

## Claims

### Claim 1

A method of increasing or maintaining bioavailability of at least one lipophilic vitamin in a patient receiving phytosterol therapy, wherein the bioavailability of said at least one lipophilic vitamin in said patient is reduced as a result of said phytosterol therapy, said method comprising administering to said patient a therapeutically-effective amount of a mixture of (1) phytosterol ester(s) and/or phytostanol ester(s) (PSE) with (2) 1,3-diglyceride(s) (DAG) dissolved or dispersed in an edible fish oil, wherein fatty acid residues of the PS-E and of the DAG correspond to fatty acid residues of fish oil.

### Claim 2 (depends on 1)

The method of claim 1 wherein said patient receiving phytosterol therapy suffers from deficiencies in fat-soluble vitamins resulting from said therapy.

### Claim 3 (depends on 2)

The method of claim 2, wherein said deficiencies in fat-soluble vitamins result from at least one of a metabolic disorder, malabsorption of fats, drug-vitamin direct or indirect interactions impaired vitamin absorption.

### Claim 4 (depends on 3)

The method of claim 3, wherein said patient also suffers from a condition selected from the group consisting of cancer, benign prostatic hypertrophy, organ transplant, ulcer, prostatitis, cardiovascular disorder (CVD), coronary heart disease (CHD), atherosclerosis, pulmonary tuberculosis, human immunodeficiency virus (HIV), stress-induced immune suppression, rheumatoid arthritis, patients receiving any treatment resulting in immunosuppression, autoimmune patients, radiation-treated patients, chemotherapy-treated patients, and allergic rhinitis/sinusitis.

### Claim 5 (depends on 1)

The method of claim 1, wherein said patient receiving phytosterol therapy is a patient that suffers from an immune deficiency including human immunodeficiency virus (HIV), stress-induced immune suppression, rheumatoid arthritis, patients receiving any treatment resulting in immunosuppression, autoimmune patients, radiation-treated patients, chemotherapy-treated patients, allergic rhinitis/sinusitis, and organ transplant patients.

### Claim 6 (depends on 5)

The method of claim 5, wherein said immune deficiency, is accompanied by an increase in serum cholesterol levels.

### Claim 7 (depends on 1)

The method of claim 1, wherein said patient receiving phytosterol therapy is a child suffering from a vitamin or essential nutrient deficiency, including β-carotene, vitamin A, and vitamin D deficiencies.

### Claim 8 (depends on 1)

The method of claim 1, wherein said at least one lipophilic vitamin is a carotenoid.

### Claim 9 (depends on 8)

The method of claim 8, wherein said at least one lipophilic vitamin is vitamin A or vitamin D.

### Claim 10 (depends on 1)

The method of claim 1, wherein the fatty acid residues of the PS-E and of the DAG are docosahexaenoic (DHA) and eicosapentaenoic acid (EPA) residues.

### Claim 11 (depends on 1)

The method of claim 1, wherein the phytosterol ester(s) are fatty acid ester(s) of a phytosterol selected from the group consisting of stigmasterol, sitosterol, beta-sitosterol, brassicasterol, campesterol, 5-avenasterol, and isomers and derivatives thereof and said phytostanol ester(s) are fatty acid ester(s) of a phytostanol selected from the group consisting of beta-sitostanol, campestanol, stigmastanol, and isomers and derivatives thereof.

### Claim 12 (depends on 1)

The method of claim 1, wherein a weight ratio between phytosterol and/or phytostanol esters and diacylglycerol(s) and phytosterol and/or phytostanol ester(s) in said mixture is from 15:1 to 1:1.

### Claim 13 (depends on 1)

The method of claim 1, wherein an amount of diacylglycerol(s) in said mixture is at least 1 wt %.

### Claim 14 (depends on 1)

The method of claim 1, wherein an amount of phytosterol and/or phytostanol ester(s) in said mixture is at least 1 wt %.

### Claim 15 (depends on 1)

The method of claim 1. wherein an amount of diacylglycerol(s) in said mixture is from 1 to 99 wt %.

### Claim 16

The method of claim wherein said mixture consists of 15 wt % DAG of which more than 50% are 1,3-DAG(s) and 25 wt % total PS-E(s) dissolved or dispersed in fish oil.

### Claim 17

A method of increasing or maintaining bioavailability of at least one lipophilic vitamin in a patient receiving phytosterol therapy, wherein the bioavailability of said at least one lipophilic vitamin in said patient is reduced as a result of said phytosterol therapy, said method comprising administering to said patient a therapeutically-effective amount of a mixture consisting of (1) phytosterol ester(s) and/or phytostanol ester(s) (PS-E) with (2) 1,3-diglyceride(s) (DAG) dissolved or dispersed in fish oil wherein tai acid residues of the PS-E and of the DAG correspond to fatty acid residues of fish oil.

### Claim 18 (depends on 17)

The method of claim 17, wherein the fatty acid residues of the PS-E and of the DAG are docosahexaenoic (DHA) and eicosapentaenoic acid (EPA) residues.

### Claim 19 (depends on 1)

The method of claim 1, wherein said mixture is comprised in a food article.

### Claim 20 (depends on 17)

The method of claim 17, wherein said mixture is comprised in a food article.