EP0901377A1 - Traitement de l'acne - Google Patents

Traitement de l'acne

Info

Publication number
EP0901377A1
EP0901377A1 EP97913977A EP97913977A EP0901377A1 EP 0901377 A1 EP0901377 A1 EP 0901377A1 EP 97913977 A EP97913977 A EP 97913977A EP 97913977 A EP97913977 A EP 97913977A EP 0901377 A1 EP0901377 A1 EP 0901377A1
Authority
EP
European Patent Office
Prior art keywords
composition
nicotinamide
tea tree
tree oil
acne
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP97913977A
Other languages
German (de)
English (en)
Inventor
John Alexander Staton
James Steven Rowe
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Mainstar One Investments Pty Ltd
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
Publication of EP0901377A1 publication Critical patent/EP0901377A1/fr
Withdrawn legal-status Critical Current

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

Landscapes

  • 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)
  • Mycology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Birds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Plant Substances (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.
EP97913977A 1996-03-25 1997-03-24 Traitement de l'acne Withdrawn EP0901377A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AUPN8924A AUPN892496A0 (en) 1996-03-25 1996-03-25 Acne treatment
AUPN8924/96 1996-03-25
PCT/AU1997/000190 WO1997035597A1 (fr) 1996-03-25 1997-03-24 Traitement de l'acne

Publications (1)

Publication Number Publication Date
EP0901377A1 true EP0901377A1 (fr) 1999-03-17

Family

ID=3793237

Family Applications (1)

Application Number Title Priority Date Filing Date
EP97913977A Withdrawn EP0901377A1 (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)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1143954E (pt) * 1998-12-01 2004-12-31 Univ Kentucky Res Found Utilizacao de derivados de acido nocotinico para o tratamento de danos no adn em celulas da pele
DK1272183T3 (da) * 2000-04-14 2006-11-27 Niadyne Corp Fremgangsmåder og sammensætninger der er nyttige til forögelse af oxygentilförsel til celler
ATE509633T1 (de) * 2002-06-17 2011-06-15 Naicons S C A R L Verwendung eines amid-derivats des ge 2270 faktors a3 für die behandlung von akne
US20100291223A1 (en) * 2008-01-07 2010-11-18 Robert Alan Armstrong Treatment for dermatological conditions
IT1401957B1 (it) * 2010-09-23 2013-08-28 Forem Pharma S R L Composizione per il trattamento dell'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
EA031758B1 (ru) * 2014-05-12 2019-02-28 Юнилевер Н.В. Ниацинамид для стимуляции продуцирования антимикробных пептидов
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
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9735597A1 *

Also Published As

Publication number Publication date
CN1219880A (zh) 1999-06-16
CA2250383A1 (fr) 1997-10-02
WO1997035597A1 (fr) 1997-10-02
EA199800869A1 (ru) 1999-06-24
JP2000507248A (ja) 2000-06-13
AUPN892496A0 (en) 1996-04-18
PL328964A1 (en) 1999-03-01
NZ332353A (en) 2000-02-28
ZA972515B (en) 1998-01-26

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