Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/673—Vitamin B group
  • A61K8/675—Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
• • 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)
  • A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
• • 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
  • A61P17/10—Anti-acne agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin

Definitions

• TITLE "ACNE TREATMENT" FIELD OF THE INVENTION relates to a topical composition for the treatment of acne and related conditions, the composition comprising melaleuca (tea tree) oil and NAD, NADP or a precursor which generates NAD or NADP in use inclusive of nicotinamide, nicotinic acid or lower C r C 4 alkyl nicotinate.
• the characteristic lesion is the comedo, a collection of sebaceous secretions and dead cells retained in the hair follicle and excretory duct of the sebaceous gland.
• Pimples are the common name for non ⁇ inflammatory comedomes and can be open (blackheads) or closed (whiteheads). If bacteria are present, the bacteria can cause breakout of the oily sebaceous materials resulting in the release of free fatty acids. The release of free fatty acids results in inflammation causing erythema and swelling around the comedomes. If the comedomes are ruptured, skin may become elevated (papules), filled with pus (pustules) or cysts may form.
• the main causes of acne are generally considered to be oily skin, hyperkeratosis of the follicular wall and bacterial infection, particularly by the anaerobic Propionibacterium acnes.
• Treatment is with peeling agents and topically applied antiseptics such as benzoyl peroxide, salicylic acid, resorcinol and triclosan.
• Severe cases can be treated systemically with antibiotics such as minocycline, tetracycline, erythromycin or retinoic acid.
• Topical treatment with erythromycin or clindamycin can also be employed.
• Bullous pemphigoid is a chronic autoimmune disease characterised by erythematous plaques, vesicles and lense bullae.
• U.S. Patent 4607101 refers to a method of treatment of acne vulgaris which comprises administration of 1-15% by volume of a carrier of carbamide peroxide alone or in combination with nicotinic acid or nicotinamide in o concentrations of 1 -10% by volume of the carrier.
• U.S. Patent 4505896 refers to a method of treatment of acne vulgaris using nicotinamide and/or nicotinic acid in concentrations of from 1-7% by volume of the carrier in combination with sulfur salicylic acid, benzoyl peroxide, vitamin A acid, erythromycin base, clindamycin and tetracycline.
• the amount of lower alkyl nicotinate utilized is from 5-2.2 by weight of a composition including a suitable carrier.
• U.S. Patent 5459153 refers to the treatment of acne vulgaris using a composition comprising pantothenic acid or derivative thereof together with nicotinic acid or derivative thereof which may generate NAD or NADP.
• concentration of nicotinic acid utilized in the composition is from 0.5-10% by weight of the composition.
• the present invention consists in a composition for the topical treatment of acne, said composition comprising 0.5-20% w/w of NAD, NADP or a precursor thereof which generates NAD or NADP in use, which precursor may include nicotinamide, nicotinic acid or lower C r C 4 alkyl nicotinate.
• the composition may also comprise 0.1- 25% w/w tea tree oil and a pharmaceutically acceptable carrier.
• the concentration of nicotinamide is preferably in the range of 2-7% w/w, most preferably 5% w/w.
• the concentration of tea tree oil is preferably 2-20% w/w, most preferably 5% w/w.
• the tea tree oil is preferably Melaleuca alternifolia oil of Australian Standard (AS) 2782, i.e. Intemational Standard (DIS) 4730.
• AS Australian Standard
• DIS Intemational Standard
• tea tree oil may be used in any of its natural forms which are obtained from any other appropriate Melaleuca species or Leptospermum species, such as, for example, M. linariifolia, M. dessitafolia as well as modified extracts thereof.
• tea tree oil may also include one or more active components thereof, such as terpinen-4-ol and/or alpha terpineol.
• the composition may be in any conventional form suitable for topical application such as in the form of a cream, stick, gel, ointment, paint, lotion or spray.
• the balance of ingredients up to 100% may include additives and excipients conventionally found in topical formulations such as emulsifiers, surfactants, thickening agents, emollients, stabilisers, humectants and preservatives.
• composition of the invention may be used as a clear aqueous solution.
• a clear aqueous solution may comprise 1- 20% surfactant, emulsifier or solubilising agent and, more preferably, a non-ionic surfactant, such as POLYSORBATE or TWEEN. More preferably, this may comprise 1-10% of surfactant and, most preferably, 1- 5% of surfactant.
• the composition of the invention may include 1-10% of an emollient which moisturizes the skin or, more preferably, 1-5% of the emollient.
• a suitable emollient is CETIOL or PEG 7 glyceryl cocoate.
• a humectant such as glycerol or .
• propylene glycol and 1-5% of a thickener or viscosity increasing agent such as a gum, in the form of a guar gum, gum tregacanth, xanthan gum, or galactomannan gum.
• a detergent such as sodium lauryl ether sulphate and/or ammonium lauryl sulphate.
• a cleaning agent such as coconut diethanolamide.
• the composition When used as a cream, the composition may include waxes, such as 1-10% and, more preferably, 1-5% of cetyl alcohol or stearyl alcohols. There also may be included essential oils, herbs, vitamins, such as Vitamin E or Vitamin A, hydrolysed collagen, amino acids, panthenol and other nutritional factors as may be required.
• the present invention consists in a method of treating or reducing incidence of acne comprising applying an effective amount of a composition to skin in need of such treatment, said composition comprising 0.5-20% w/w of NAD, NADP or the abovementioned precursor which generates NAD or NADP in use, which precursor preferably comprises nicotinamide, nicotinic acid or lower C ⁇ C- 4 alkyl nicotinate.
• the composition also includes 0.1-20% w/w tea tree oil and a pharmaceutically acceptable carrier.
• the composition is applied directly to the lesions and preferably also the surrounding areas of skin.
• the composition can also be applied to skin susceptible to acne outbreak to reduce the incidence of lesions.
• the desired frequency of application will vary with the severity of the acne. Application once to three times per day is recommended for milder cases, with more frequent application for severe cases.
• the composition may be applied to acne affected areas or areas susceptible to acne and then rinsed off with water. Washing with such a composition can be repeated once to three times per day, or more often if desired. .Without being bound by theory, it is hypothesized that the mechanism of action of nicotinamide and related compounds as described above is associated with its ability to form NAD or NADP in use which is an enzymatic co-factor.
• a suitable gel composition of the present invention is as follows :-
• a suitable cream composition of the present invention is as follows:-
• Nicotinamide BP 5.0%
• a suitable lotion composition of the present invention is as follows:-
• Nicotinamide BP 5.0%
• the anti-bacterial activity of a composition containing 5% w/w tea tree oil and 5% w/w nicotinamide was compared with the activity of 5% w/w tea tree oil, 5% w/w nicotinamide and two commercial preparations containing benzoyl peroxide as the active ingredient.
• the comparison was by way of a suspension test using P. acnes ATCC6919. Tea tree oil was AS2782 grade.
• the current ISO standard reference is DIS (draft International Standard) 4730.
• Example 5 The ratio of nicotinamide to tea tree oil was varied as shown in Table 3 in this Example such that the ratio of tea tree oil to nicotinamide varied between 5:5 to 1.25:5 on a weight for weight basis. Results of a P. acnes suspension test show that there is no significant difference between any one of the results when the content of nicotinamide was at least 5.0%.
• Example 6 Further studies as shown in Table 4 using the P. acnes suspension test show that at concentrations below 5%, nicotinamide was not as effective as concentrations at 5% or above. Concentrations of nicotinamide in excess of 5% did not appear to enhance the activity of the combination.
• Example 7 Further studies as shown in Table 4 using the P. acnes suspension test show that at concentrations below 5%, nicotinamide was not as effective as concentrations at 5% or above. Concentrations of nicotinamide in excess of 5% did not appear to enhance the activity of the combination.
• Example 7 Further studies as shown in Table 4 using the P. acnes suspension test show that at concentrations below 5%, nicotinamide was not as effective as concentrations at 5% or above. Concentrations of nicotinamide in excess of 5% did not appear to enhance the activity of the combination.
• Example 7 Further studies as shown in Table 4 using the P. acnes suspension test show that at concentrations below 5%, nicotinamide was not as effective as concentration
• N-methyl nicotinamide cfu/mL >25000000 20000 10000 1200 ⁇ 100 log 10 reduction ⁇ 0.1 2.2 3.5 4.4 >6.0

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Natural Medicines & Medicinal Plants (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Pharmacology & Pharmacy (AREA)
• Dermatology (AREA)
• Epidemiology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Microbiology (AREA)
• Botany (AREA)
• Medical Informatics (AREA)
• Biotechnology (AREA)
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• Alternative & Traditional Medicine (AREA)
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• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Cosmetics (AREA)
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• Medicines Containing Plant Substances (AREA)

Applications Claiming Priority (3)

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• 1996
  • 1996-03-25 AU AUPN8924A patent/AUPN892496A0/en not_active Abandoned
• 1997
  • 1997-03-24 PL PL97328964A patent/PL328964A1/xx unknown
  • 1997-03-24 EA EA199800869A patent/EA199800869A1/ru unknown
  • 1997-03-24 JP JP9533869A patent/JP2000507248A/ja active Pending
  • 1997-03-24 CN CN97194879A patent/CN1219880A/zh active Pending
  • 1997-03-24 NZ NZ332353A patent/NZ332353A/en unknown
  • 1997-03-24 EP EP97913977A patent/EP0901377A1/en not_active Withdrawn
  • 1997-03-24 WO PCT/AU1997/000190 patent/WO1997035597A1/en not_active Application Discontinuation
  • 1997-03-24 CA CA002250383A patent/CA2250383A1/en not_active Abandoned
  • 1997-03-24 ZA ZA9702515A patent/ZA972515B/xx unknown

Non-Patent Citations (1)

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