AU1736299A - Pharmaceutical or veterinary composition for the treatment of skin disorders - Google Patents

Description

P/00/0011 Regulation 3.2

AUSTRALIA

Patents Act 1990 COMPLETE

SPECIFICATION

FOR A STANDARD

PATENT

ORIGINAL

Name of Applicant: Actual Inventor: Address for service in Australia: Invention Title: Riccardo PISATURO Riccardo PISATURO CARTER SMITH BEADLE 2 Railway Parade Camberwell Victoria 3124 Australia PHARMACEUTICAL OR VETERINARY COMPOSITION FOR THE TREATMENT OF SKIN

DISORDERS

Details ofAssociated Provisional Application: PP1953 filed 20 February 1998 The following statement is a full description of this invention, including the best method of performing it known to us

I

PHARMACEUTICAL OR VETERINARY COMPOSITION FOR THE TREATMENT OF SKIN DISORDERS The present invention relates to a pharmaceutical or veterinary composition, in particular a topical pharmaceutical or veterinary composition for use in the treatment of skin disorders.

Most humans and/or animals require some form of treatment for their skin at various stages in their lifetime. As the skin is subjected to much wear and tear, it is important that it is maintained in good condition so that its protective function is not impaired.

Topical compositions for application to the skin for pharmaceutical or veterinary purposes are available in a wide range of types and for treating an equally wide range of conditions and dermatological problems. Modem pharmaceutical and veterinary science, has given rise to a vast range of specific products, many of which ~suffer numerous side effects due to use of highly refined and potent drugs and compounds.

Notwithstanding the effectiveness and efficacious nature of currently available products, the need for a general purpose, multi-efficacy, low-irritant and non toxic skin treatment composition still remains.

According to one aspect of the present invention there is provided a pharmaceutical composition characterised by including an effective amount of garlic or extracts or derivatives thereof in combination with an effective amount of emu oil and a pharmaceutically acceptable carrier.

The present invention also extends to a veterinary composition characterised by including an effective amount of garlic or extracts or derivatives thereof in combination with an effective amount of emu oil and a veterinarily acceptable carrier.

According to another aspect of the present invention there is provided a method for the treatment and/or prophylaxis of skin disorders which includes administering the aforesaid composition to a subject in need thereof.

MAW:IR #27494.CAP 17 February 1999 The present invention also provides the use of a combination of garlic or extracts or derivatives thereof with emu oil in the manufacture of a medicament for the treatment and/or prophylaxis of skin disorders.

The present invention further extends to an extract from the Liliales order, salts thereof, hydrates thereof, solvates thereof, pharmaceutically or veterinarily acceptable derivatives thereof, pro-drugs thereof, tautomers thereof and/or isomers thereof for use in the treatment and/or prophylaxis of skin disorders.

The extract from the Liliales order which is an order of monocot plants growing from rhizomes or bulbs may include extracts from the families liliaceae (lily), Agavaceae (agave), Alliaceae (onion), Amaryllidaceae (daffodil) and Dioscoreaceae (yam). Preferably, the extract is from the Liliaceae family which includes the genera Allium and Colchicum. The Allium genus which includes onions, garlic and leek is particularly preferred. A suitable species of the genus Allium is Allium sativum L. or garlic.

The extract may be isolated from various parts of plants of the Liliales order such as the leaves, bark, stem, flowers or roots. It may be in any form including a solid such as a powder or a liquid such as an oil. It will be appreciated that synthetic versions of the natural product are also included within the scope of the present invention, for example, kyolic which contains an extract of aged garlic having a "reduced odour.

The salts of the Liliales extract are preferably pharmaceutically or veterinarily acceptable, but it will be appreciated that non-pharmaceutically or veterinarily acceptable salts also fall within the scope of the present invention, since these are useful as intermediates in the preparation of pharmaceutically or veterinarily acceptable salts. Examples of pharmaceutically or veterinarily acceptable salts include salts of pharmaceutically or veterinarily acceptable cations such as sodium, potassium, lithium, calcium, magnesium, ammonium and alkylammonium; acid addition salts of pharmaceutically or veterinarily acceptable inorganic acids such as hydrochloric, orthophosphoric, sulphuric, phosphoric, nitric, carbonic, boric, sulfamic and hydrobromic acids; or salts of pharmaceutically or veterinarily acceptable organic MAW:IR #27494.CAP 17 February 1999 acids such as acetic, propionic, butyric, tartaric, maleic, hydroxymaleic, fumaric, citric, lactic, mucic, gluconic, benzoic, succinic, oxalic, phenylacetic, methanesulphonic, trihalomethanesuphonic, toluenesulphonic, benzenesulphonic, salicyclic, sulphanilic, aspartic, glutamic, edetic, stearic, palmitic, oleic, lauric, pantothenic, tannic, ascorbic, veleric acids.

By "pharmaceutically or veterinarily acceptable derivative" is meant any pharmaceutically or veterinarily acceptable salt, hydrate or any other compound which, upon administration to the subject is capable of providing (directly or indirectly) the Liliales extract active metabolite or residue thereof.

The term "pro-drug" is used herein in its broadest sense to include those compounds which can be converted to the Liliales extract.

The term "tautomer" is used herein in its broadest sense to include Liliales extracts which are capable of existing in a state of equilibrium between two isomeric forms. Such forms may differ in the bond connecting two atoms or groups and the position of these atoms or groups in the extract.

The term "isomer" is used herein in its broadest sense and includes structural, geometric and stereo isomers.

One or more pharmaceutically or veterinarily acceptable carriers, diluents adjuvents and/or excipients may be present in the composition. Each carrier, diluent, adjuvant and/or excipient must be pharmaceutically or veterinarily "acceptable" in the sense of being compatible with the other ingredients of the composition and not injurious to the subject.

SThe pharmaceutical or veterinary composition may be prepared by any suitable method known in the art. Preferably, the composition is prepared by combining or mixing the extract from the Liliales order and the pharmaceutically or veterinarily acceptable carrier, diluent, adjuvant and/or excipient together.

The pharmaceutical composition can take the form of a powder, suspension, solution, spray, emulsion, ointment, gel, lotion, hair tonic, shampoo, pessary or cream and can be used for localised application. Such compositions can be prepared by combining, mixing or dissolving the extracts from the Liliales order in the form of a MAW IR #27494.CAP 17 February 1999 free acid or salt with a pharmaceutically acceptable carrier, diluent, adjuvant and/or excipient such as animal, plant and/or mineral extracts; aqueous or non-aqueous solvents, for example, water or alcohol; stabilizers; emulsifiers; detergents; additives, for example, sorbolene; and in addition, where necessary, colorants; flavourings; binders; thickeners; antioxidants; perfumes; and/or preservatives, for example, Unigerm G2.

The consistency, feel or stability of the product can be adjusted by use of the following:- Beeswax at 1-10%, Xanthan Gum at Magnesium Sulphate at 0.1- Polysorbate 60 at 0.25-5%, Sorbitan Stearate at 0.25-5.00%, Lanolin at 1-5.00%, Bis-diglyceryl polyacyladipate-2 at Caprulic/Capric Triglyceride at and Petrolatum (Vaseline) 1-5.0%.

The concentration of ingredients can vary depending on the nature of the treatment and the manner of application. A cream is recommended.

The veterinary composition may include those adapted for: oral administration, external application, for example drenches aqueous or non-aqueous solutions or suspensions); tablets, capsules or boluses; powders, granules or pellets for admixture with feed stuffs; pastes for application to the tongue; topical application, e.g. as a cream, ointment or spray applied to the skin; or intravaginally, e.g. as a pessary, cream or foam.

The term "animal extract" is used herein in its broadest sense and refers to any bodily part extracted from an animal, for example, tissues, organs, fluids, keratinous material, feathers, scales, oil, fat, bone, wax, skin, hair, etc. The animal may be a lower invertebrate, higher invertebrate or vertebrate. Examples of lower invertebrates include protozoa, sponges, coelenterates, flatworms and nemertea or proboscis worms. The higher invertebrates may be selected from molluscs, annelida, echinoderms and arthropods, for example, crustaceans, spiders, centipedes, millipedes and insects, such as, bees. Examples of vertebrates include sea squirts or tunicates, MAW:IR #27494 CAP 17 February 1999 cephalochordata, jawless fish, cartilaginous fish, bony fish, amphibians, reptiles, birds or mammals, such as, marsupials.

Preferably the animal extract is selected from wool fat, seal fat, emu oil, goanna oil or fish oil. The animal extract is most preferably emu oil.

The term "plant extract" is used herein in its broadest sense and refers to any anatomical part extracted from a plant, for example, seeds, oil, leaves, bark, stems, flowers or roots. Suitable plant extracts include vegetable extracts, for example, Aloe vera; tree extracts, for example, tee tree oil or eucalyptus oil; fruit extracts, for example, olive oil; and herbal extracts, for example, canola or lavender oil.

The term "mineral extract" is used herein in its broadest sense and refers to any element, compound or composition extracted from the earths crust such as, for example, inorganic materials, micronutrients, fossil fuels, clays, cement, glass, rocks, .0 sulphur and sand. Preferred mineral extracts include mineral oil such as liquid petroleum derivatives; mineral spirits, mineral water or mineral wax.

0'"0 According to a further aspect of the present invention there is provided a topical pharmaceutical or veterinary composition including an effective amount of garlic or extracts or derivatives thereof in combination with an effective amount of emu oil and a pharmaceutically or veterinarily acceptable carrier, diluent, adjuvant and/or excipient.

According to a still further aspect of the present invention there is provided a method for the treatment and/or prophylaxis of skin disorders which includes topically :*000* applying a therapeutically effective amount of such a composition to the skin of a *so* subject in need thereof.

A preferred composition contains up to about 20% by weight garlic extract in combination with up to about 50% by weight emu oil with the balance by weight being the pharmaceutically or veterinarily acceptable carrier, diluent, adjuvant and/or excipient.

The term "skin disorder" is used herein in its broadest sense and refers to any disorder which effects the appearance and/or structure of the skin. Skin disorders which may be treated by the method of the invention include dermatitis, eczema, MAW:IR #27494.CAP 17 Februimy 1999 psoriasis, acne, heat rash, skin blemishes, hyperkeratosis, ichthyosis, viral skin disorders, such as, warts or herpes, for example, cold sores, chickenpox and shingles, and fungal skin disorders, such as, dermatophyte infections, for example, ringworm and tinea or yeast infections, for example, candidiasis or thrush. The method is particularly useful in treating fungal skin disorders. It will be appreciated that the method of the invention may also be used to improve the appearance of dry, flaky, wrinkled, aged or photodamaged skin. It will also sooth or alleviate the associated effects of the skin disorder such as pain, itching, swelling, etc.

The method of treatment and/or prophylaxis involves the administration of .o effective amounts of the extract from the Liliales order for a time and under conditions sufficient for the skin disorder to be inhibited, reduced or otherwise ameliorated. The extract may be administered in a single dose or a series of doses.

The subject may be a human, livestock animal sheep, cow or horse), S laboratory test animal mouse, rabbit or guinea pig) or companion animal (e.g.

dog or cat). The present invention however, is particularly directed to human therapy.

The composition of the invention is preferably applied in the form of a topical formulation 1 to 3 times a day to the area of skin suffering from the disorder. This treatment regime may be continued until the skin disorder is alleviated, typically 1 week.

The invention will now be described with reference to the following examples.

These examples are not to be construed as limiting the invention in any way.

Example 1 The following ingredients were combined in the amounts specified: Ingredient Amount (by weight) Emu Oil 92% Kyolic Unigerm G2 3% MAW:IR #27494.CAP 17 Februaiy 1999 The emu oil used in Example 1 had the following composition: o *°oo* FAME ANALYSIS Carbon Content Fatty Acid Name Amount C14 Myristic 0.6 C16:0 Palmitic 20.4 C16:1 Palimitoleic C18:0 Stearic 8.6 C18:1 Oleic 50.1 C18:2 Linoleic 13.3 C18:3 Linolenic 0.9 C20:0 Arachinic 0.1 C20:1 Gadoleic 0.4 MICROBIOLOGICAL ANALYSIS Total Viable Aerobic Count (CFU/g) Incubation Period Result 30°C/72 hrs 25°C/5 days PEROXIDE VALUE Number of mg Active Oxygen contained in 1000g of the sample Example 2 The following ingredients were combined in the amounts specified: Ingredient Sorbolene Kyolic Unigerm G2 Amount (by weight) 92% s3% The sorbolene used in Example 2 had the following composition.

Ingredient Cetomacrogol Emulsifying Wax Liquid paraffin Amount (by weight) MAW:IR #27494.CAP 17 February 1999 White soft paraffin Chlorocresol 0.1% Propylene glycol Purified water, freshly boiled and cooled 59.9% Example 3 The composition of Example 1 was applied topically to the nose, ears, eye area, neck and rest of the body of stud beef cattle suffering from ringworm. After the first application the redness of the ringworm was alleviated and often the problem was cured. In some cases, a second application was required.

The composition was found to not cause any problems very close to the eye no tears or irritation. The cattle ceased rubbing the ringworm affected area immediately.

Example 4 The composition of Example 1 was applied to the skin of cattle that were affected with ringworm, ranging from extremely severe cases to moderate cases.

Within a few days there was a marked improvement. The cattle who had severe cases of ringworm were treated with the composition 1 week later. In each case the ringworm affected areas were healing and the hair was growing back within 1 to 2 S. weeks.

Example The composition of Example 1 was applied to the skin of cattle suffering from warts and bald patches. The healing process commenced immediately and the hair grew back very quickly.

Example 6 An elderly woman had been suffering with tinea for many years and in recent months it had spread from her toes to her feet and half way up her knees. The composition of Example 2 was applied to the tinea twice a day. The tinea stopped itching almost immediately. After 2-3 days it started healing and within 10 days the MAW:IR #27494.CAP 17 February 1999 tinea had completely disappeared.

Example7 Water phase Ingredients: Purified Water Thickening Agents Garlic Powder Preservative Oil Phase Ingredients Emu Oil Polyglyceryl-2 Sesqui-isostearate Polyglycerol Polyrincinoleate Triethanolamine Example 8 Ingredient Purified Water Magnesium Aluminium Silicate Garlic Powder Phenoxyethanol/Methylparaben/ EthylparabeniPropylparabenJ Butylparaben (Uniphen) Emu Oil Polyglyceryl-2 Sesqul-isostearate Polyglycerol Polyrincinoleate Example 9 Ingredient Purified Water Carbomer Garlic Powder Percentage w/w to make 100.00 0.10- 5.00 1.00 -20.00 0.10- 1.00 1.00-50.00 0.50 -5.00 0.50 5.00 0.10- 5.00 Percentage w/w 63.80 %w/w 0.50 10.00 0.70 20.00 2.00 3.00 Percentage w/w 63.30 %w/w 0.50 10.00 M4AW:IR #27494.CAP 1 eray19 17 February 1999 Phenoxyethanol/Methylparabeiij EthylparabeniPropylparaben/ Butylparaben (Uniphen) Emu Oil Polyglyceryl-2 Sesqui-isostearate Polyglycerol Polyrincinoleate Triethanolamine 0.70 20.00 2.00 3.00 0.50 MAW:IR #27494.CAP 17 February 1999

Claims (6)

1. A pharmaceutical composition characterised by including an effective amount of garlic or extracts or derivatives thereof in combination with an effective amount of emu oil and a pharmaceutically acceptable carrier.

2. A veterinary composition characterised by including an effective amount of garlic or extracts or derivatives thereof in combination with an effective amount of emu oil and a veterinarily acceptable carrier.

3. A method for the treatment and/or prophylaxis of skin disorders including the therapeutic administration of a composition according to claim 1 or 2.

4. The use of a combination of garlic or extracts or derivatives thereof with emu oil in the manufacture of a medicament for the treatment and/or prophylaxis of skin disorders. A composition according to claim 1 or 2 being w/w a a Purified Water Thickening Agent Garlic Powder Preservative Emu Oil Polyglyceryl-2 Sesqui-isostearate Polyglycerol Polyrincinoleate Triethanolamine

6. A composition according to claim Purified Water Magnesium Aluminium Silicate Garlic Powder Phenoxyethanol/Methylparaben/ Ethylparaben/Propylparaben/ Butylparaben (Uniphen) Make up to 100 0.10- 5.00 1.00 20.00 0.10- 1.00 1.00- 50.00 0.50- 5.00 0.50- 5.00 0.10- 5.00 5 being:- %w/w

63.80 0.50 10.00 0.70 MAW:IR #27494.CAP 17 February 1999 Emu Oil 20.00 Polyglycerol-2Sesqui-isostearate 2.00 Polyglycerol Polyrincinoleate 3.00 7. A composition according to claim 5 being: w/w- Purified Water 63.30% Magnesium Aluminium Silicate Carbomer 0.50 Garlic Powder 10.00 Phenoxyethanol/Methylparaben/ Ethylparaben/Propylparaben/ Butylparaben (Uniphen) 0.70 Emu Oil 20.00 Polyglyceryl-2 Sesqui-isostearate 2.00 Polyglycerol Polyrincinoleate 3.00 Triethanolamine 0.50 8. A composition according to any one of claims 5 to 7 being a cream adapted for topical application. 9. A method according to claim 3 wherein said therapeutic administration is the topical application of said composition to the area of skin suffering from the disorder. A method according to claim 3 for the treatment of any one or a combination of dermatitis, eczema, psoriasis, acne, heat rash, skin blemishes, hyperkeratosis, ichthyosis, viral skin disorders, such as warts or herpes, for example, cold sores, chickenpox and shingles, and fungal skin disorders, such as, dermatophyte infections, for example, ringworm and tinea or yeast infections, for example, candidiasis or thrush. 11. A method according to claim 3 for the treatment of ringworm. 12. A method according to claim 3 for the treatment of warts. 13. A method according to claim 3 for the treatment of baldness. MAW:IR #27494.CAP 17 February 1999 14. A method according to claim 3 for the treatment of tinea. A composition according to any one of claims 1, 2, 5, 6, 7 or 8 substantially as hereinbefore described with particular reference to the examples. 16. A method according to any one of claims 3 or 9 to 14 substantially as hereinbefore described with particular reference to the examples. Dated: 17 February 1999 CARTER SMITH BEADLE Patent Attorneys for the Applicant: Riccardo PISATURO oo a :%oo MAW:IR #27494.CAP 17 February 1999