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Title:
PHARMACEUTICAL COMPOSITION CONTAINING BLACK CUMIN OIL, FLAX OIL AND BORAGO OIL
Document Type and Number:
WIPO Patent Application WO/2004/012753
Kind Code:
A1
Abstract:
This invention relates to an enteral pharmaceutical composition for the treatment of multiple sclerosis. The pharmaceutical composition includes black cumin oil (nigella sativa, flax oil (oleium lini), borage oil (borago officinalis), vitamins and minerals. When taken enterally, the composition has been shown to treat multiple sclerosis successfully. The dosage of the composition depends on the severity of the multiple sclerosis and the patient, but a usual dosage is 20ml to 40ml per day.

Inventors:
CREDE HELFRIED HANS RUDOLF (ZA)
Application Number:
PCT/IB2003/003054
Publication Date:
February 12, 2004
Filing Date:
July 31, 2003
Export Citation:
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Assignee:
CREDE HELFRIED HANS RUDOLF (ZA)
International Classes:
A61K31/202; A61K36/23; A61K36/30; A61K36/55; A61P25/00; A61P39/06; (IPC1-7): A61K35/78; A61K31/202; A61P25/00; A61P39/06
Domestic Patent References:
WO2000032211A12000-06-08
Foreign References:
US4058594A1977-11-15
EP0520624A11992-12-30
EP0347056A11989-12-20
Other References:
HARBIGE L S ET AL: "The protective effects of omega-6 fatty acids in experimental autoimmune encephalomyelitis (EAE) in relation to transforming growth factor-beta 1 (TGF-beta1) up-regulation and increased prostaglandin E2 (PGE2) production", CLINICAL AND EXPERIMENTAL IMMUNOLOGY, vol. 122, no. 3, December 2000 (2000-12-01), &, pages 445 - 452, XP002263545, ISSN: 0009-9104
TREMLETT H L ET AL: "Nonprescription medicine use in a multiple sclerosis clinic population", BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, vol. 50, no. 1, July 2000 (2000-07-01), &, pages 55 - 60, XP002263546, ISSN: 0306-5251
Attorney, Agent or Firm:
Donald, Heather June (PO Box, 2024 Craighall, ZA)
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Claims:
CLAIMS
1. An enteral pharmaceutical composition containing black cumin oil (nigelle sativa), flax oil (oleium lini) and borage oil (borago officinalis) for the treatment of multiple sclerosis.
2. The composition according to claim 1 containing 70 to 80% by mass, flax oil ; 10% to 20% by mass, black cumin oil ; and 5% to 15% by mass borage oil.
3. The composition according to claim 2 containing 75% by mass, flax oil ; 15% by mass, black cumin oil ; and 10% by mass borage oil.
4. The use of black cumin oil (nigella sativa), flax oil (oleium lini) and borage oil (borago officinalis) in a method of making a medicament for use in a method of treating multiple sclerosis.
5. The use according to claim 4, wherein the medicament contains 70 to 80% by mass, flax oil ; 10% to 20% by mass, black cumin oil ; and 5% to 15% by mass borage oil.
6. The use according to claim 5, wherein the medicament contains 75% by mass, flax oil ; 15% by mass, black cumin oil ; and 10% by mass borage oil.
7. An enteral pharmaceutical composition for treating multiple sclerosis, the composition containing 65% to 75% by mass polyunsaturated fatty acids wherein one of the polyunsaturated fatty acids is gammalinolenic acid.
8. The composition according to claim 7, wherein the polyunsaturated fatty acids are selected from alphalinolenic acid and linoleic acid.
9. The composition according to claim 7, containing 1% to 10 % by mass gammalinolenic acid.
10. The composition according to claim 7, containing in percentage by mass of the composition: AlphaLinolenic Acid 40% to 50% Linoleic Acid 22% to 26% Oleic Acid 16% to 20% GammaLinolenic Acid 1 % to 5% Palmitic Acid 4% to 7% StearicAcid 2% to 5% Other fatty Acids 2% Aromatic Oils 0.3%.
11. The composition according to claim 10, containing in percentage by mass of the composition: AlphaLinolenic Acid 45% Linoleic Acid 24% Oleic Acid 18% GammaLinolenic Acid 2% Palmitic Acid 6% StearicAcid 4% Other fatty Acids 2% Aromatic Oils 0.3%.
12. The composition according to claim 7, containing desaturase enzymes.
13. The composition according to claim 12, containing delta6desaturase.
14. The composition according to claim 1 or claim 7 ; containing vitamins B3, B6 and C, zinc and magnesium.
15. A method of treating multiple sclerosis, the method including the step of administering an enteral pharmaceutical composition containing black cumin oil (nigella sativa), flax oil (oleium lini) and borage oil (borago officinalis) to a patient in need thereof.
16. The method according to claim 15, the composition containing 70 to 80% by mass, flax oil ; 10% to 20% by mass, black cumin oil ; and 5% to 15% by mass borage oil.
17. The method according to claim 16, the composition containing 75% by mass, flax oil ; 15% by mass, black cumin oil ; and 10% by mass borage oil.
18. The method according to claim 15, wherein the composition is administered to the patient at a dosage of 20ml40ml per day.
19. The method according to claim 18, wherein the composition is administered to the patient at a dosage of 20ml per day.
Description:
PHARMACEUTICAL COMPOSITION CONTAINING BLACK CUMIN OIL, FLAX OIL AND BORAGO OIL BACKGROUND TO THE INVENTION This invention relates to an enteral pharmaceutical composition for the treatment of multiple sclerosis.

Multiple sclerosis is caused by damage to the myelin sheath which covers the axons of neurons. Nerve signals travel from neuron to neuron via axons. The myelin sheath serves as an insulation against signal loss to neighbouring tissue. A damaged myelin sheath leads to a distortion or complete disappearance of signals.

In addition, the myelin sheath is sub-divided into distinct sections which are separated from each other by nodes, which are called"Nodes of Ranvier". The latter's function is to speed up the transmission of nerve signals.

Damage to the myelin sheath therefore not only distorts or leads to the complete loss of nerve signals, but also slows down their transmission from neuron to neuron.

This, in essence, is the nature of the phenomenon known as multiple sclerosis.

As the damage to the myelin sheaths progresses, the patient affected by the disease loses control of essential body functions: loss of balance, slow and shaky walking patterns, speech impediment, even loss of bladder control and other symptoms.

Myelin is a very complex substance, consisting of various fats, fatty acids, phospho-lipids, proteins and even cholesterol.

The vast majority of these substances are either fat or fat derivatives. It is therefore clear that the formation and periodic regeneration of myelin depends on dietary intake and a well-functioning metabolic system.

It is believed that if a treatment could be found which repairs the damage to the myelin sheath and which would prevent the damage from re-occurring, it would either cure the sufferer or at least reduce the symptoms to bearable levels.

It is an object of the invention to provide a pharmaceutical composition, which will assist in curing the causes of multiple sclerosis SUMMARY OF THE INVENTION According to the invention there is provided an enteral pharmaceutical composition containing black cumin oil (nigella sativa), flax oil (oleium lini) and borage oil (borago officinalis) for the treatment of multiple sclerosis.

The invention also relates to a method of treating multiple sclerosis using the aforementioned pharmaceutical composition, and to the use of black cumin oil, flax oil and borage oil in a method of making a medicament for use in a method of treating multiple sclerosis.

The composition typically contains 70 to 80% by mass, preferably 75% by mass flax oil ; 10% to 20% by mass, preferably 15% by mass black cumin oil ; and 5% to 15% by mass, preferably 10% by mass borage oil.

According to a preferred embodiment of the invention there is provided an enteral pharmaceutical composition for treating multiple sclerosis, the composition containing 65% to 75% by mass polyunsaturated fatty acids wherein one of the polyunsaturated fatty acids is gamma-linolenic acid. The other polyunsaturated fatty acids may be selected from alpha-linolenic acid and linoleic acid.

Advantageously, the composition contains 1% to 10 % by mass gamma- linolenic acid.

In a preferred embodiment of the invention, the pharmaceutical composition contains, by mass of the composition: Alpha-Linolenic Acid 40% to 50%, preferably 45% Linoleic Acid 22% to 26%, preferably 24% Oleic Acid 16% to 20%, preferably 18% Gamma-Linolenic Acid 1 % to 5%, preferably 2% Palmitic Acid 4% to 7%, preferably 6% Stearic-Acid 2% to 5%, preferably 4% Other fatty Acids 2% Aromatic Oils 0.3% Preferably, the composition also contains enzymes, preferably desaturase enzymes such as delta-6-desaturase.

Advantageously, the composition also contains vitamins, preferably vitamins B3, B6 and C, and minerals, preferably zinc and magnesium.

DETAILED DESCRIPTION OF THE INVENTION This invention relates to an enteral pharmaceutical composition for the treatment of multiple sclerosis.

The pharmaceutical composition includes black cumin oil (nigella sativa), flax oil (oleium lini), borage oil (borago officinalis) and vitamins and minerals.

Black cumin oil is composed of the following fatty acids by mass: Myristic 0.2% Palmitic 12. 4% Palmitoleic 0.2% Stearic 2.7% Oleic 23.7% Omega 6 (Linoleic) 57.2% Omega 3 (Linolenic) 0.2% Arachidic 0.4% Gadoleic 0.4% Other 0.6% Flax oil is composed of the following fatty acids by mass: Omega 3 (Linolenic) 60. 1% Omega 6 (Linoleic) 15.2% Oleic 16. 4% Palmitic 3.9% Stearic 3.6% Other 0.8% Borage oil is composed of the following fatty acids by mass: Gamma-Linolenic acid 22% Linoleic acid 38% Oleic acid 16% Palmitic 9% Gadoleic acid 4% Stearic acid 3% Other total 8% (palmitoleic, linolenic, arachidic, erucic, behenic, nervonic).

The flax oil, borage oil and black cumin oil are mixed at a percentage 75%, 10% and 15% by mass respectively to provide a medicinal composition according to the invention. These percentages may vary, depending on the individual's requirements.

When taken enterally the composition has been shown to treat multiple sclerosis successfully. The dosage of the composition depends on the severity of the multiple sclerosis and the patient, but a usual dosage is 20mi to 40ml per day, typically 20mi per day.

The composition of the invention provides an abundance of polyunsaturated fatty acids which are believed to be the building materials for the formation of myelin, the breakdown of which is believed to be the root cause of multiple sclerosis. This abundance of fatty acids is provided by the flax oil, the black cumin oil and the borage oil.

The conversion of essential fatty acids to substances required for the formation of myelin is a slow and inefficient process. It is assumed that only about 2 to 3 % of essential fatty acids entering the metabolic pathways are eventually converted to the substances needed, even if all factors perform normally. The process is further slowed down by various aspects, either acquired or genetically programmed, such as malfunction of the small intestine (inhibiting absorption of co-factors), liver damage (leading to, for instance, inadequate formation of enzymes) or inadequate supply and/or absorption of essential fatty acids.

The enzymes required for essential fatty acids metabolism are delta-6, delta-5 and delta-4-desaturase, of which delta-6-desaturase is the most important because if its function is impaired for whatever reasons, the other two enzymes have nothing to work with. It may also be that delta-6-desaturase is not produced by the body in sufficient quantities, which leads to the same malfunction. The borage oil contains gamma-linolenic acids, a substance normally produced in the human body by the enzyme delta-6-desaturase acting on dietary linoleic acid through a process known as desaturation and elongation. In the composition of the invention, gamma-linolenic acid is therefore available for subsequent metabolic conversions even if no or to little delta-6-desaturase is present. Borage seeds are also a source of delta-6- desaturase, thus making a basic supply of delta-6-desaturase available for the relevant conversions of fatty acids, not only into gamma-linolenic acid but also dihomo-gamma-linolenic acid, from which arachidonic acid and other essential fatty acid derivatives are formed.

Enzymes require so-called co-factors in order to properly perform their functions. In the case of delta-6, delta-5 and delta-4-Desaturase, the co- factors are the vitamins B3, B6, and C and the minerals zinc and magnesium.

Even an abundance of enzymes will not be able to effect the proper essential- fatty-acid metabolisms even if only one of the co-factors is not available in sufficient quantities. As a consequence, the complex end products of said metabolism, arachidonic acid with 4 double bonds, and docosahexaenoic acid, with 6 double bonds, will not be available in sufficient quantities. These two fatty acids are"brain fatty acids", meaning that they are incorporated into various brain structures, playing a vital role in the formation of myelin, and the transmission of nerve signals. Multiple sclerosis sufferers are therefore not only affected by a lack of available essential fatty acids, but also by a lack of available enzymes and/or a lack of available co-factors. Borage seeds contain the enzyme delta-6-desaturase, which is therefore made available through the oil, as an oil-soluble substance and/or through seed particles which are purposely left in the oil after cold-pressing. Therefore, even if a patient is lacking the enzyme delta-6-desaturase, it is made available through the borage oil and seed component of the present invention.

Example 1 In a typical example of the invention, 750moi flax oil is mixed with 100mut of borage oil and 150ml of black cumin oil to provide a preparation which is made up by the following by mass of the composition: Alpha-Linolenic Acid 45.5% Linoleic Acid 23.6% Oleic Acid 17.9% Gamma-Linolenic A 2.2% Palmitic Acid 5.6% Stearic Acid 3.5% Other fatty Acids 2. 1% Aromatic Oils 0.3% The composition also comprised 0, 1g vitamin B6, 0, 1g vitamin B3,5g vitamin C, 14g magnesium and 0,6g zinc.

Example 2 A lady in her early fifties had multiple sclerosis for"more than 10 years". Her condition had gradually worsened over time, from plateau to plateau, until she had developed the usual spectrum of MS symptoms: impaired eyesight, <BR> <BR> speech impediments, incontinence, "tight-chest"phenomena, numbness in various limbs, walking impediments, and more.

She began using the composition described in Example 1 at a dosage of 20ml per day. Her condition improved after 4 to 6 weeks. Approximately 3 months after beginning to use the composition of the invention she was practically symptom free and after 15 months she was still practically symptom free.

Example 3 A young man in his mid-20s was diagnosed to have multiple sclerosis in December 2001. His condition deteriorated rapidly, to the point where he could no longer reach out for an object in front of him without missing it. He had also, by May 2002, developed a strong speech impediment.

In May 2002, the patient started using the composition of Example 1 at a dosage of 20moi per day. Within 4 months, his condition had improved to such an extent that he was practically symptom-free.