WO1997035597A1 - Traitement de l'acne - Google Patents

Traitement de l'acne Download PDF

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Publication number
WO1997035597A1
WO1997035597A1 PCT/AU1997/000190 AU9700190W WO9735597A1 WO 1997035597 A1 WO1997035597 A1 WO 1997035597A1 AU 9700190 W AU9700190 W AU 9700190W WO 9735597 A1 WO9735597 A1 WO 9735597A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
nicotinamide
tea tree
tree oil
acne
Prior art date
Application number
PCT/AU1997/000190
Other languages
English (en)
Inventor
John Alexander Staton
James Steven Rowe
Original Assignee
Mainstar One Investments Pty. Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mainstar One Investments Pty. Ltd. filed Critical Mainstar One Investments Pty. Ltd.
Priority to NZ332353A priority Critical patent/NZ332353A/en
Priority to AU21430/97A priority patent/AU710919B2/en
Priority to EP97913977A priority patent/EP0901377A1/fr
Priority to EA199800869A priority patent/EA199800869A1/ru
Priority to JP9533869A priority patent/JP2000507248A/ja
Publication of WO1997035597A1 publication Critical patent/WO1997035597A1/fr

Links

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

Abstract

Composition pour le traitement topique de l'acné, comprenant de 0,5 à 20 % en poids de NAD, de NADP ou d'un précurseur qui produit de la NAD ou de la NADP à l'usage, 0,1 à 25 % en poids de 'tea tree oil' (extrait de Melaleuca ou de Leptospermum) et un excipient acceptable sur le plan pharmaceutique.
PCT/AU1997/000190 1996-03-25 1997-03-24 Traitement de l'acne WO1997035597A1 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
NZ332353A NZ332353A (en) 1996-03-25 1997-03-24 Topical acne treatment using nicotinamide, nicotinic acid, or an alkyl nicotinate and tea tree oil
AU21430/97A AU710919B2 (en) 1996-03-25 1997-03-24 Acne treatment
EP97913977A EP0901377A1 (fr) 1996-03-25 1997-03-24 Traitement de l'acne
EA199800869A EA199800869A1 (ru) 1996-03-25 1997-03-24 Лечение угрей
JP9533869A JP2000507248A (ja) 1996-03-25 1997-03-24 ざ瘡（にきび）治療

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AUPN8924A AUPN892496A0 (en) 1996-03-25 1996-03-25 Acne treatment
AUPN8924 1996-03-25

Publications (1)

Publication Number Publication Date
WO1997035597A1 true WO1997035597A1 (fr) 1997-10-02

Family

ID=3793237

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/AU1997/000190 WO1997035597A1 (fr) 1996-03-25 1997-03-24 Traitement de l'acne

Country Status (10)

Country Link
EP (1) EP0901377A1 (fr)
JP (1) JP2000507248A (fr)
CN (1) CN1219880A (fr)
AU (1) AUPN892496A0 (fr)
CA (1) CA2250383A1 (fr)
EA (1) EA199800869A1 (fr)
NZ (1) NZ332353A (fr)
PL (1) PL328964A1 (fr)
WO (1) WO1997035597A1 (fr)
ZA (1) ZA972515B (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000032179A2 (fr) * 1998-12-01 2000-06-08 University Of Kentucky Research Foundation Methode de renforcement des reponses cellulaires protectrices contre le stress genotoxique cutane
WO2001078730A1 (fr) * 2000-04-14 2001-10-25 Niadyne Corporation Procedes et compositions permettant d'ameliorer l'alimentation de cellules en oxygene
EP2240192A1 (fr) * 2008-01-07 2010-10-20 Robert Alan Armstrong Traitement d'états dermatologiques
ITMI20101727A1 (it) * 2010-09-23 2012-03-24 Forem Pharma S R L Composizione per il trattamento dell'acne.
CN112245311A (zh) * 2020-11-19 2021-01-22 泉后(广州)生物科技研究院有限公司 一种祛痘组合物
WO2023135186A1 (fr) * 2022-01-12 2023-07-20 S-Biomedic Nv Composition de soin de la peau et ses utilisations

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0305070A (pt) * 2002-06-17 2004-09-21 Vicuron Pharm Inc Uso de derivado amida de ge 2270 fator a3 para tratamento da acne
CN103099756B (zh) * 2013-02-01 2014-07-16 广州市白云区天芳化妆品厂 一种除粉刺抗过敏霜及其制备方法
WO2015172801A1 (fr) * 2014-05-12 2015-11-19 Unilever N.V. Niacinamide induisant la production de peptides antimicrobiens
KR101604212B1 (ko) 2015-07-17 2016-03-17 울산대학교 산학협력단 Ｎａｄ를 함유하는 비만 또는 내당능장애의 예방 및 치료용 조성물
CN108619062B (zh) * 2018-07-17 2020-06-19 广州澳希亚实业有限公司 祛痘组合物及其应用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
INTERNATIONAL JOURNAL OF DERMATOLOGY, Volume 34, Number 6, June 1995, SHALITA et al., "Topical Nicotinamide Compared With Clindamycin Gel in the Treatment of Inflammatory Acne Vulgaris", pages 434-437. *
THE MEDICAL JOURNAL OF AUSTRALIA, Volume 153, 15 October 1990, BASSETT et al., "A Comparative Study of Tea-tree Oil Versus Benzoylperoxide in the Treatment of Acne", pages 455-457. *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000032179A2 (fr) * 1998-12-01 2000-06-08 University Of Kentucky Research Foundation Methode de renforcement des reponses cellulaires protectrices contre le stress genotoxique cutane
WO2000032179A3 (fr) * 1998-12-01 2001-12-13 Univ Kentucky Res Found Methode de renforcement des reponses cellulaires protectrices contre le stress genotoxique cutane
US6337065B1 (en) * 1998-12-01 2002-01-08 University Of Kentucky Research Foundation Method for enhancing protective cellular responses to genotoxic stress in skin
AU762770B2 (en) * 1998-12-01 2003-07-03 University Of Kentucky Research Foundation, The A method for enhancing protective cellular responses to genotoxic stress in skin
WO2001078730A1 (fr) * 2000-04-14 2001-10-25 Niadyne Corporation Procedes et compositions permettant d'ameliorer l'alimentation de cellules en oxygene
EP2240192A1 (fr) * 2008-01-07 2010-10-20 Robert Alan Armstrong Traitement d'états dermatologiques
EP2240192A4 (fr) * 2008-01-07 2013-02-27 Robert Alan Armstrong Traitement d'états dermatologiques
AU2009203892B2 (en) * 2008-01-07 2014-10-30 Robert Alan Armstrong Treatment for dermatological conditions
ITMI20101727A1 (it) * 2010-09-23 2012-03-24 Forem Pharma S R L Composizione per il trattamento dell'acne.
CN112245311A (zh) * 2020-11-19 2021-01-22 泉后(广州)生物科技研究院有限公司 一种祛痘组合物
WO2023135186A1 (fr) * 2022-01-12 2023-07-20 S-Biomedic Nv Composition de soin de la peau et ses utilisations

Also Published As

Publication number Publication date
JP2000507248A (ja) 2000-06-13
ZA972515B (en) 1998-01-26
AUPN892496A0 (en) 1996-04-18
NZ332353A (en) 2000-02-28
PL328964A1 (en) 1999-03-01
CA2250383A1 (fr) 1997-10-02
EP0901377A1 (fr) 1999-03-17
CN1219880A (zh) 1999-06-16
EA199800869A1 (ru) 1999-06-24

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