Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/01—Hydrocarbons
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
  • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
  • A61K31/202—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
  • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
  • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
  • A61K31/355—Tocopherols, e.g. vitamin E
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/30—Boraginaceae (Borage family), e.g. comfrey, lungwort or forget-me-not
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
  • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
  • A61P17/08—Antiseborrheics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/10—Antimycotics

Definitions

• the present invention relates to a composition for the treatment of Dermatitis, such as Diaper Dermatitis (DD) and Seborrheic Dermatitis (SD), such as Infantile Seborrhoeic Dermatitis (ISD).
• Dermatitis such as Diaper Dermatitis (DD) and Seborrheic Dermatitis (SD), such as Infantile Seborrhoeic Dermatitis (ISD).
• DD Diaper Dermatitis
• SD Seborrheic Dermatitis
• ISD Infantile Seborrhoeic Dermatitis
• Diaper Dermatitis represents the most common dermatologic disease that affects infants (Ward DB, Fleischer AB Jr, Feldman SR et al. Characterization of diaper dermatitis in the United States. Arch Pediatr Adolesc Med 2000;154:943-946). The incidence of DD is highest in those between 8 and 12 months of age (Wolf R, Wolf D, Tuzun E, et al. Diaper Dermatitis. Clin Dermatol 2001; 18: 657-60). There are no differences in the prevalence between genders or race, although breastfed babies may have a reduced risk (Singleton JK. Pediatric dermatoses: three common skin disruptions in infancy. Nurse Pract 1997; 22: 32-50 and Levy M.
• feces proteose
• the enzymes in feces may irritate baby's tender skin.
• feces contain organisms that can cause skin infection.
• Urine further irritates the diaper area. As urine breaks down, it releases ammonia. This causes the pH of the skin to rise (in other words, to become increasingly basic, or alkaline) and the enzymes from baby's stool to become more active. This may result in tissue/skin damage and lead to diaper rash.
• Contributing factors to the acute inflammatory condition include skin occlusion and friction , lipolytic and proteolytic activity of fecal enzymes, and excessive moisture as well as increased pH related to the prolonged exposure to urine.
• the combined action of these factors may compromise the skin barrier and increase susceptibility to further attack by enzymatic activity and chemical irritants as well as to secondary bacterial or fungal infections, frequently involving Candida spp. and Staphylococcus aureus.
• the incidence of Diaper Dermatitis correlates with the occurrence of diarrhea and frequency of diaper changes (Stamatas GN, Zerweck C, Grove G, Martin KM. Documentation of Impaired Epidermal Barrier in Mild and Moderate Diaper Dermatitis In Vivo Using Noninvasive Methods. Pediatr Dermatol 2011; 28: 99-107).
• Diaper Dermatitis is characterized by compromised stratum corneum (SC) barrier function as indicated by increased transepidermal water loss (TEWL) and also by increased skin hydration.
• SC stratum corneum
• Diaper Dermatitis causes emotional stress for infants, as indicated in a study on infant behavior during and after an episode of DD. Parents reported an increase in the frequency of crying as the first symptom of pain together with agitation. Other behavioral indicators of distress, such as facial expressions (eyes squeezed shut, deepening of the nasolabial furrow), were more prevalent, normal eating habits and sleeping patterns were disrupted, and the frequency of urination and defecation diminished. Levels of salivary Cortisol, a molecular indicator of stress, also increased in some infants during the period with DD (Stamatas GN, Tierney NK. Diaper Dermatitis: Etiology, Manifestations, Prevention, and Management. Pediatr Dermatol 2014; 31: 1-7).
• Diaper Dermatitis Although not the most practical, is to discontinue use of diapers, allowing the affected skin to air out. Thorough drying of the skin before diapering is a good preventive measure because it is the excess moisture, either from urine and feces or from sweating, that sets the conditions for a diaper rash to occur.
• Various moisture-absorbing powders such as talcum or starch, reduce moisture but may introduce other complications. Airborne powders of any sort can irritate lung tissue, and powders made from starchy plants (corn, arrowroot) provide food for fungi and are not recommended by the American Academy of Dermatology.
• Zinc oxide-based ointments may be effective in certain cases, especially in prevention of diaper dermatitis, because they have both a drying and an astringent effect on the skin, being mildly antiseptic without necessarily causing irritation.
• Treatment with zinc oxide-based ointments introduces a risk of drying out the skin and thus does not provide an optimal treatment of diaper dermatitis.
• Zinc oxide-based sprays suffer from the drawback of having a thick viscosity, requiring subsequent distribution by rubbing in on the sensitive skin. Further, such existing sprays require shaking of the spray container before use, and the spray leaves a white residual after use.
• Seborrheic Dermatitis is a chronic inflammatory skin disorder characterized in immunocompetent adult patients by periods of exacerbation and remission.
• the reported prevalence of SD in the overall adult population ranges from 1 to 5 percent, and the disorder can affect any ethnicity.
• Infantile SD may be limited to scalp involvement ("cradle cap") or may be more diffuse.
• the adult form of SD which is far more common than infantile SD and appears to affect men more than women, may present first around puberty, correlating with the increase in cutaneous lipids resulting from androgen-driven sebaceous gland development and sebum secretion.
• the course of adult SD in affected individuals is variable throughout adulthood with some noting only occasional periods of exacerbation and others experiencing greater chronicity with more frequent recurrences.
• Seborrheic dermatitis is a common complaint brought to pediatricians. Also known as “cradle cap” in infants and “dandruff” in adolescents, the condition is believed to be triggered by Malassezia yeasts ("Use of Olive Oil for the Treatment of Seborrheic Dermatitis in Children” by Elaine Siegfried and Erica Glenn, Arch Pediatr Adolesc Med. 2012;166(10):967, citing "The role of sebaceous gland activity and scalp microfloral metabolism in the etiology of seborrheic dermatitis and dandruff" by o Bl, Dawson TL, J Investig Dermatol Symp Proc. 2005;10(3):194-197).
• borage seed oil is derived from the seeds of the Borago officinalis (borage). Borage seed oil has one of the highest amounts of gamma-linolenic acid (GLA) of seed oils— higher than blackcurrant seed oil or evening primrose oil, to which it is considered similar. The oil comprises around 24% of GLA typically. GLA is converted to dihomo-gamma-linolenic acid, a precursor to a variety of the 1-series prostaglandins and the 3-series leukotrienes.
• GLA gamma-linolenic acid
• the present invention concerns a composition comprising ethyl lactate, for use in the treatment, prophylaxis or alleviation of symptoms of dermatitis. Without being bound by theory, it is speculated that ethyl lactate may stabilize the pH of the skin, thereby alleviating symptoms of dermatitis, in particular DD.
• ethyl lactate provides a number of advantages as compared to existing treatments.
• the skin does not become dry; rather, ethyl lactate provides a natural level of moisture. Further, ethyl lactate provides a barrier against contaminants leading to DD. In addition, the application of ethyl lactate does not leave a visible residual after use.
• compositions according to the present invention provide improved penetration, as well as a less greasy texture of the composition as compared to borage oil. This leads to improved ease of application as well as improved patient compliance. It has further surprisingly been discovered that compositions according to the present invention reduces, inhibits and/or does not allow proliferation of strains of Malassezia. It appears that Squalane dissolves glue formed by dry sebum. Squalane has similar properties as liquid sebum, meaning it dissolves dry sebum at the scalp so it can be washed away.
• borage oil has not been used successfully for the oral treatment of ISD. It is not known whether this is due to lack of clinical experimentation, or because GLA administered orally is broken down or accompanied by side effects, or its metabolism is too fast to provide effective treatment.
• compositions of the present invention may act as depot formulations, slowly releasing any actives from the skin.
• the present invention concerns a composition
• a composition comprising Squalane and gamma-linolenic acid (GLA).
• GLA gamma-linolenic acid
• the present invention concerns a method of manufacture of a composition, comprising mixing Squalane, gamma-linolenic acid (GLA) and vitamin E.
• GLA gamma-linolenic acid
• the addition of vitamin E surprisingly appears to prevent precipitate in forming upon mixing Squalane and borage oil.
• the present invention concerns a use of Squalane and GLA for the manufacture of a medicament for the treatment, prophylaxis or alleviation of symptoms of
• Dermatitis such as Diaper Dermatitis (DD) and Seborrheic Dermatitis (SD).
• the present invention concerns the treatment, prophylaxis or alleviation of symptoms of DD and SD comprising application of a composition according to the invention.
• the invention concerns a composition comprising ethyl lactate, for use in the treatment, prophylaxis or alleviation of symptoms of dermatitis.
• ethyl lactate may stabilize the pH of the skin, thereby alleviating symptoms of dermatitis.
• the invention concerns the composition, wherein said use is for treatment, prophylaxis or alleviation of symptoms of an indication selected among Diaper Dermatitis (DD), Atopic Dermatitis and Seborrheic Dermatitis (SD).
• DD Diaper Dermatitis
• SD Seborrheic Dermatitis
• the invention concerns the composition for use in the treatment, prophylaxis or alleviation of symptoms of Diaper Dermatitis (DD).
• DD Diaper Dermatitis
• the invention concerns the composition for use in the treatment, prophylaxis or alleviation of symptoms of Seborrheic Dermatitis (SD).
• SD Seborrheic Dermatitis
• the invention concerns the composition for use in the treatment, prophylaxis or alleviation of symptoms of Infantile Seborrheic Dermatitis (ISD).
• ISD Infantile Seborrheic Dermatitis
• the invention concerns the composition for use in the treatment, prophylaxis or alleviation of symptoms of an indication selected among the group consisting of dandruff and cradle cap.
• the invention concerns the composition comprising 1% - 50%, preferably 2% - 40%, more preferred 3% - 30%, preferably 4% - 25%, more preferred 5% - 20%, preferably 7% - 15%, more preferred about 10% ethyl lactate.
• the invention concerns the composition further comprising kigelia.
• the invention concerns the composition further comprising kigelia oil.
• the invention concerns the composition comprising 1% - 50%, preferably 2% - 40%, more preferred 3% - 35%, preferably 5% - 30%, more preferred 7% - 25%, preferably 10% - 20%, more preferred about 15% kigelia oil.
• the invention concerns the composition comprising 0.5% - 15%, preferably 1% - 10%, more preferred 2% - 5%, preferably 2.5% - 4%, more preferred about 3% kigelia.
• the invention concerns ethyl lactate for use in the treatment, prophylaxis or alleviation of symptoms of dermatitis.
• the invention concerns the ethyl lactate, wherein said use is for treatment, prophylaxis or alleviation of symptoms of an indication selected among Diaper Dermatitis (DD), Atopic Dermatitis and Seborrheic Dermatitis (SD).
• DD Diaper Dermatitis
• SD Seborrheic Dermatitis
• the invention concerns the ethyl lactate for use in the treatment, prophylaxis or alleviation of symptoms of Diaper Dermatitis (DD).
• DD Diaper Dermatitis
• the invention concerns a composition comprising Squalane and gamma-linolenic acid (GLA).
• GLA gamma-linolenic acid
• GLA may be obtained from vegetable oils such as GLA safflower oil (Carthamus tinctorius), evening primrose (Oenothera biennis) oil, blackcurrant seed oil, borage oil, and hemp seed oil. GLA is also found in edible hemp seeds, oats, barley, and spirulina. Each contains varying amounts of the fatty acid, with GLA safflower oil at 40% GLA being a concentrated form. This is a genetically modified oil. It should be noted that conventional safflower oils have zero GLA. Borage oil ranges from 15% to 20% and evening primrose oil ranges from 8% to 10% GLA.
• the invention concerns a composition, further comprising at least one fat-soluble ingredient.
• the invention concerns a composition, further comprising vitamin E.
• Vitamin E refers to a group of eight fat-soluble compounds that include both tocopherols and tocotrienols.
• the eight compounds are alpha-tocopherol, beta-tocopherol, gamma- tocopherol, delta-tocopherol, alpha-tocotrienol, beta-tocotrienol, gamma-tocotrienol, and delta- tocotrienol.
• the invention concerns a composition, further comprising Rosemary Extract.
• Rosemary Extract is also known as rosmarinus officinalis I. extract, with CAS Number: 84604- 14-8.
• the invention concerns a composition, further comprising vitamin E and Rosemary Extract. Using vitamin E and Rosemary Extract appears to provide a synergy effect on the stability of the composition.
• the invention concerns a composition comprising gamma-linolenic acid (GLA), vitamin E and Rosemary Extract, and optionally at least one fat-soluble ingredient. Vitamin E and Rosemary Extract appear to stabilize GLA.
• GLA gamma-linolenic acid
• Vitamin E and Rosemary Extract appear to stabilize GLA.
• the invention concerns a composition, further comprising Sunflower oil.
• the invention concerns a composition, further comprising Rosemary Extract and Sunflower Oil.
• Sunflower oil is a suitable carrier for Rosemary Extract.
• the invention concerns a composition, comprising at least one compound selected among a tocopherol and a tocotrienol, or a pharmaceutically acceptable salt thereof.
• the invention concerns a composition, comprising at least one compound selected among the group consisting of alpha-tocopherol, beta-tocopherol, gamma- tocopherol, delta-tocopherol, alpha-tocotrienol, beta-tocotrienol, gamma-tocotrienol, and delta- tocotrienol, or a pharmaceutically acceptable salt thereof.
• the invention concerns a composition, comprising at least one tocopherol selected among a natural tocopherol and a synthetic form of tocopherol.
• the invention concerns a composition, comprising an ingredient selected among safflower oil, evening primrose oil, blackcurrent seed oil, borage oil, and hemp seed oil.
• the invention concerns a composition comprising an ingredient selected among borage oil, evening primrose oil and blackcurrant oil. According to an embodiment, the invention concerns a composition comprising borage oil.
• Borage oil is a preferred source of GLA. Borage seed oil is a particularly preferred source of GLA. Other suitable sources of GLA may be utilized.
• the invention concerns a composition
• a composition comprising 1% - 99%, preferably 5% - 95%, more preferred 10% - 90%, preferably 20% - 80%, more preferred 30% - 70%, preferably 40% - 60%, more preferred 50 % borage oil.
• the invention concerns a composition
• a composition comprising 1% - 99%, preferably 5% - 95%, more preferred 10% - 90%, preferably 20% - 80%, more preferred 30% - 70%, preferably 40% - 60%, more preferred 50 % Squalane.
• the invention concerns a composition
• a composition comprising 0.1% - 25%, preferably 0.5% - 20%, more preferred 1% - 15%, preferably 3% - 10%, more preferred 5% vitamin E.
• the invention concerns a composition, comprising 0.05% - 10%, preferably 0.1% - 5%, more preferred 0.2% - 2%, preferably 0.3% - 1%, more preferred 0.5% vitamin E.
• the invention concerns a composition, comprising 0.001% - 10%, preferably 0.005% - 5%, more preferred 0.007% - 2%, preferably 0.01% - 1%, more preferred 0.02% - 0.5%, preferably 0.03% - 0.2%, more preferred 0.05% - 0.1% Rosemary Extract.
• the invention concerns a composition, comprising 10 - 50000, preferably 50 - 10000, more preferred 100 - 5000, preferably 300 - 2000, more preferred 500 -1000 ppm (w/w) Rosemary Extract.
• the invention concerns a composition, comprising 0.1% - 25%, preferably 0.2% - 10%, more preferred 0.3% - 5%, preferably 0.5% - 2%, more preferred 0.9-0.95% Sunflower oil.
• the invention concerns a composition comprising 500 - 250000, preferably 1000 - 100000, more preferred 3000 - 50000, preferably 5000 - 20000, more preferred 9000 - 9500 ppm (w/w) Sunflower oil.
• the invention concerns a composition
• a composition comprising 1% - 50%, preferably 2% - 40%, more preferred 3% - 30%, preferably 4% - 25%, more preferred 5% - 20%, preferably 7% - 15%, more preferred about 10% ethyl lactate.
• Ethyl lactate may stabilize, adjust and/or lower the pH to a value suitable for skin treatment.
• the invention concerns a composition
• a composition comprising 1% - 50%, preferably 2% - 40%, more preferred 3% - 35%, preferably 5% - 30%, more preferred 7% - 25%, preferably 10% - 20%, more preferred about 15% kigelia oil.
• Kigelia oil is a mixture of about 80% olive oil and about 20% Kigelia. Kigelia may provide antifungal, anti bacteriological, antioxidant and anti quorum sensing properties.
• the invention concerns a composition comprising 0.5% - 15%, preferably 1% - 10%, more preferred 2% - 5%, preferably 2.5% - 4%, more preferred about 3% kigelia.
• the invention concerns a composition for use as a medicament.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms of a skin disorder, such as Dermatitis.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms of an indication selected among Diaper Dermatitis (DD), Atopic Dermatitis and Seborrheic Dermatitis (SD).
• DD Diaper Dermatitis
• SD Seborrheic Dermatitis
• Diaper Dermatitis also known as “Irritant diaper dermatitis” and “napkin dermatitis” and commonly known as diaper rash or nappy rash, is a generic term applied to skin rashes in the diaper area that are caused by various skin disorders and/or irritants.
• Seborrheic Dermatitis is an inflammatory skin disorder affecting the scalp, face, and torso. Typically, Seborrheic Dermatitis presents with scaly, flaky, itchy, and red skin. It particularly affects the sebaceous-gland-rich areas of skin. It is also known as "cradle cap” in infants and “dandruff” in adolescents.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms of Diaper Dermatitis (DD).
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms of Seborrheic Dermatitis (SD).
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms of infantile Seborrheic Dermatitis (ISD).
• ISD infantile Seborrheic Dermatitis
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms of an indication selected among the group consisting of dandruff and cradle cap.
• Further potential indications for the present compositions comprise anti-inflammatory disorders, arthritis, eczema, atopic eczema, atopic dermatitis, and psoriasis.
• Additional envisaged indications comprise hyperactive gastrointestinal, respiratory and cardiovascular disorders, such as
• gastrointestinal colic, cramps, diarrhea
• airways asthma, bronchitis
• cardiovascular cardiovascular
• cardiotonic antihypertensive and blood purifier
• urinary urinary (diuretic and kidney/bladder disorders).
• envisaged indications or uses comprise acute respiratory distress syndrome, periodontitis (gum disease)/ gingivitis, rheumatoid arthritis, alcohol-induced hangover, cystic fibrosis, hyperlipidemia, infant development / neonatal care, malnutrition (inflammation complex syndrome), stress, supplementation in preterm and very low birthweight infants.
• the invention concerns a composition, wherein said composition reduces, inhibits and/or does not allow proliferation of Malassezia. This may be tested by comparing with a negative control.
• Malassezia (formerly known as Pityrosporum) is a genus of fungi. Many researchers and clinicians believe that Malassezia play a pivotal role in the pathogenesis of
• Seborrheic Dermatitis (SD), according to the article "Seborrheic Dermatitis and Malassezia species - How Are They Related?" by Grace K. Kim et al., J Clin Aesthet Dermatol. 2009 November; 2(11): 14- 17.
• the invention concerns a composition, wherein said composition reduces, inhibits and/or does not allow proliferation of Malassezia strains MRL 821 and 822.
• the invention concerns a composition, wherein said composition does not form precipitate upon storage.
• no precipitate is formed within 1 week, preferably 1 month, more preferred 3 months, preferably 6 months, more preferred 12 months.
• compositions of the present invention are intended for human use, animal use is also envisaged.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms, comprising topical administration of said composition.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms, wherein 0.001 - 5 mg, preferably 0.005 - 1 mg, more preferred 0.01-0.5 mg, preferably 0.02-0.1 mg, more preferred 0.05 mg GLA/kg body weight is administered.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms, comprising at least daily administration of said composition.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms, comprising administering said composition at a site affected by DD or SD.
• the invention concerns a composition for use in the treatment, prophylaxis or alleviation of symptoms, comprising administering said composition at a site not affected by DD or SD.
• the invention concerns the composition in an administration form selected among a liquid, solution, topical solution, shake lotion, shampoo, oil, gel, ointment, cream, lotion, liquid, aerosol, spray, skin patch, transdermal patch, foam, solid, powder, sponge, tape, paste, and tincture; preferably a spray.
• a spray comprising ethyl lactate may provide a viscosity suitable for application without requiring subsequent rubbing on the sensitive skin.
• the invention concerns a method of manufacture of a composition, comprising mixing Squalane, gamma-linolenic acid (GLA) and vitamin E.
• GLA gamma-linolenic acid
• the invention concerns a use of vitamin E and Rosemary Extract for stabilizing gamma-linolenic acid (GLA).
• Vitamin E and Rosemary Extract may stabilize GLA for example using the amounts of vitamin E and Rosemary Extract indicated in the claims, embodiments and examples.
• the invention concerns the use of Squalane and GLA for the manufacture of a medicament for the treatment, prophylaxis or alleviation of symptoms of Diaper Dermatitis (DD) or Seborrheic Dermatitis (SD).
• DD Diaper Dermatitis
• SD Seborrheic Dermatitis
• the invention concerns a use, wherein borage oil is used as a source of GLA.
• the invention concerns a use, wherein said medicament is for topical application.
• the invention concerns a use, wherein said medicament is for a treatment, prophylaxis or alleviation of symptoms, wherein 0.001 - 5 mg, preferably 0.005 - 1 mg, more preferred 0.01-0.5 mg, preferably 0.02-0.1 mg, more preferred 0.05 mg GLA/kg body weight is administered.
• the invention concerns a use, wherein said medicament is for a treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered at least daily.
• the invention concerns a use, wherein said medicament is for a treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered at a site affected by DD or SD.
• the invention concerns a use, wherein said medicament is for a treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered at a site not affected by DD or SD.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms of DD or SD comprising application of a composition according to the invention.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein said application is topical. According to an embodiment, the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein 0.001 - 5 mg, preferably 0.005 - 1 mg, more preferred 0.01-0.5 mg, preferably 0.02-0.1 mg, more preferred 0.05 mg GLA/kg body weight is administered.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered at least daily.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered a number of times selected among 1, 2, 3, 4, 5, and 6 times daily.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered a number of times selected among 1, 2, 3, 4, 5, 6 and 7 times weekly.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered at a site affected by DD or SD.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms, wherein said composition is administered at a site not affected by DD or SD.
• the invention concerns the treatment, prophylaxis or alleviation of symptoms of DD or SD comprising administration of Squalane and GLA.
• compositions of the invention may provide advantages selected among, but not limited to: 1. Adjusting the pH (ethyl lactate).
• Figure 1 shows Malassezia growth on LNA with various agents 3 days post inoculation.
• Figure 2 shows Malassezia growth on LNA with various agents 11 days post inoculation.
• Figure 3 shows Malassezia growth on LNA with various agents 21 days post inoculation.
• Figure 4 shows the induction time of different compositions of the invention.
• Figure 5 shows the protection factor of different compositions of the invention.
• LNA Leeming-Notman
• the Squalane/borage oil formulation comprised 30% Squalane, 65% Borage oil and 5% vitamin E.
• Figure 1 shows Malassezia growth of strain M L 822 on LNA with various agents 3 days post inoculation. The following symbols are used.
• FIG. 2 shows Malassezia growth of strain M L 822 on LNA with various agents 11 days post inoculation. The following symbols are used.
• FIG 3 shows Malassezia growth of strain MRL 822 on LNA with various agents 21 days post inoculation. The following symbols are used.
• LNA without glycerol monostearate with 0.5 g Squalane/borage oil formulation LNA without glycerol monostearate or glycerol with 0.5 g Squalane/borage oil formulation and unmodified LNA (growth control) demonstrated similar Malassezia colony growth and size.
• LNA without glycerol monostearate, glycerol, or glucose with 0.5 g Squalane/borage oil formulation and LNA without glycerol monostearate, glycerol, glucose or Squalane/borage oil formulation (negative control) had smaller colony growth.
• LNA without glycerol monostearate with 0.5 g Squalane/borage oil formulation LNA without glycerol with 0.5 g Squalane/borage oil, LNA without glycerol monostearate or glycerol, with 0.5 g Squalane/borage oil formulation, and unmodified LNA (growth control) all had similar large Malassezia colonies.
• Table 2 below shows the colony counts for the 2 strains of Malassezia tested on each media.
• LNA growth control
• 111 151 w/o glycerol monostearate, glycerol, or glucose (negative control) 105 133
• composition according to the invention (used in sample D), surprisingly provided less growth than the negative control, (sample F).
• a composition according to the invention is able to reduce the growth of Malassezia strains. This is evidenced by Fig. 1, Fig. 2 and Fig. 3, as well as by the data of Table 2.
• ingredients such as glycerol, monostearate glycerol, and glucose may enhance the growth of Malassezia.
• Subjects suffering from Seborrhoeic Dermatitis or Infantile Seborrhoeic Dermatitic are topically administered a composition according to the invention containing 65% Borage oil, 30% Squalane and 5% vitamin E (w/w) to the affected areas. This administration is conducted once daily for four weeks.
• Rosemary Mixture is a mixture comprising Sunflower oil (90-95%) and Rosemary Extract (5-10%).
• compositions were tested, with and without Rosemary Mixture (The compositions prepared without Rosemary Mixture had additional borage oil):
• Composition A (w/w %) Borage oil 69% Squalane 30% Vit E 0.5 % [Rosemary Mixture 0.5%]
• Composition B (w/w%) Borage oil 68.5% Squalane 30% Vit E 0.5 %
• Composition C (w/w%) Borage oil 65% Squalane 30% Vit E 5 %
• composition D (w/w%) Borage oil 69% Squalane 30% [Rosemary Mixture 1%]
• Composition E (w/w%) Borage oil 65% Squalane 30% Vit E 4% [Rosemary Mixture 1%]
• Protection factor of each treatment was calculated by measuring the oxidative stability of samples using an Omnion Oxidative Stability Instrument (Rockland, MA).
• the Oxidative Stability Instrument (OSI) provides a rapid instrumental determination of the oxidative stability of fats, oils and other organic materials by measuring the induction period (length of time before rapid acceleration of oxidation occurs. The induction period, as indicated by the OSI, is positively correlated with antioxidant efficacy and the subsequent oxidative stability of the substrate.
• the compositions A, B, C, D and E were tested with and without Rosemary Mixture.
• Figure 4 shows the Induction Time results for all the Formulas treatments. Rosemary Mixture showed excellent effect in increasing the induction time of formula A, B, D and E relative to the untreated control.
• Figure 5 shows the Protection Factor imparted by the different treatments. Rosemary Mixture addition improved the oxidative stability of formulas significantly. Rosemary Mixture added at 1.0% resulted in a 310% improvement in formula B, 250% in E and 244% in D. Rosemary Mixture added at 0.5% also resulted in a 171% improvement in formula A.
• composition B comprising Rosemary Mixture
• composition D comprising Rosemary Mixture
• vitamin E and Rosemary Mixture together provide a synergy effect.
• this synergy effect appears only to be present at lower vitamin E levels. This is seen by comparing compositions D and E, both with Rosemary Mixture. The synergy effect appears to be absent or very small in composition E with Rosemary Mixture.
• composition B provided the best storage stability of the tested compositions, while the storage stability of Composition D and E were about the same. This may indicate that for these compositions, 1% Rosemary Mixture provides superior storage stability compared to 0.5% Rosemary Mixture.
• the optimum vitamin E contents may be between 0 and 5% (all percentages by weight) when mixed with Rosemary Mixture, for the storage stability. Table 4 below provides examples of manufactured as well as envisaged embodiments compositions of the present invention.
• compositions which may be particularly effective in the treatment or alleviation of symptoms of Dermatitis, in particular Diaper Dermatitis.
• compositions are provided in Table 5 below.
• Kigelia oil is a mixture, comprising 20% Kigelia and 80% olive oil.
• canola oil may be replaced with borage oil, as indicated in Composition N.
• compositions may be manufactured by mixing the ingredients.
• Compositions of this example have shown good efficacy and safety in the treatment of Diaper Dermatitis using a spray for application. The spray has been used morning and evening for 1 - 4 weeks, with good results.

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• 2014
  • 2014-11-24 EP EP14811758.3A patent/EP3074005A2/de not_active Withdrawn
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