WO2003047609A1 - Formulation topique contre les demangeaisons et procede de preparation de celle-ci - Google Patents

Formulation topique contre les demangeaisons et procede de preparation de celle-ci Download PDF

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Publication number
WO2003047609A1
WO2003047609A1 PCT/IN2002/000228 IN0200228W WO03047609A1 WO 2003047609 A1 WO2003047609 A1 WO 2003047609A1 IN 0200228 W IN0200228 W IN 0200228W WO 03047609 A1 WO03047609 A1 WO 03047609A1
Authority
WO
WIPO (PCT)
Prior art keywords
weight
formulation
tea tree
oil
glycol carbonate
Prior art date
Application number
PCT/IN2002/000228
Other languages
English (en)
Inventor
Mini Thomas
Sandeep Gadgil
Ajit Sitaram Manke
Alain Khaiat
Original Assignee
Johnson & Johnson Limited
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 Johnson & Johnson Limited filed Critical Johnson & Johnson Limited
Priority to EP02796955A priority Critical patent/EP1461057A1/fr
Priority to JP2003548864A priority patent/JP2005515204A/ja
Publication of WO2003047609A1 publication Critical patent/WO2003047609A1/fr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/53Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/534Mentha (mint)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/61Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/75Anti-irritant

Definitions

  • a topical anti-itch formulation and a process for the preparation thereof are provided.
  • corticosteroids such as hydrocortisone.
  • dexametliasone or betamethasone are generally used.
  • the side effects/adverse effects of long term use of corticosteroids such as skin thi ing or atrophy are clinically well known and reported (Medicine in practice. Issue 1, pg 14).
  • centella asiatica is well known to have medicinal properties. Centella whole extract isolated from the herb is purified for therapeutic use. Purified centella extract enriched with its triterpen ⁇ actives viz asiaticocide, asiatic acid and madeeassie acid in 1% is reported to be used in healing of various types of wounds o ⁇ ulcers or in disinfection thereof or in cicatrisation thereof by regeneration or in stimulation of skin and also as a. scar minimising agent ("Clinical study of a new antikeloid agent", Annals of Plastic Surgery, Vol 3, No 1, pp 13 to 21, by Bbsse J P et al, French Patent No 2594690A, European Patent No 22046A, Belgium Patent No 699410A). Preparation of purified centella extract by techniques like nanofiltrat m, liquid- liquid extraction or column cliromatography is laborious, time consui iing and expensive thus rendering purified centella extract very expensive.
  • Tea tree oil in 0.2% and above is reported to exhibit antibacterial properties and is used in cosmetics and toiletries ('Optimising the activity of tea tree oil in cosmetics and toiletries" - a Paper presented at the 4th Joint Conference of Australian and New Zealand Societies of Cosmetic Chemists, Surfer's Paradise. Australia, 1994).
  • An object of the. invention is to provide a topical anti-itch formulation, which provides fast and effective relief from itching.
  • Another object of the invention is to provide a topical anti-itch formulation, which also provides cooling and moisturising effects.
  • Another object of the invention is to provide a topical anti-itch formulation, which is safe for use over a long period of time.
  • Another object of the invention is to provide a topical anti-itch I rmuMon, which is economical.
  • Another object of the invention is to provide a topical anti-itch formulation j Whicli is easy and convenient to use.
  • Another object of the invention is to provide a process for preparing a topical anti-itch formulation which is safe for use over a long period of time.
  • Another object of the invention is to provide a process for preparing a topical anti-itch formulation which is economical.
  • Another object of ⁇ ie invention is to provide a process for preparing a topical anti-itch formulation which is easy and convenient to use.
  • a topical anti-itch formulation comprising centella asiatica whole extract in 0.1- 2% by weight and tea tree oil in 0.1 - 2% by weight in combination with formulating agents.
  • a process for preparing a topical anti-itch formulation comprising mixing centella asiatica whole extract in 0.1-2% by weight and tea tree oil in 0.1-2% by weight with formulating agents ai 25-80°C.
  • the formulation may comprise a cooling cum moisturising agent in 0.3 - 2% by weight and the process may comprise mixing a cooling cum moisturising agent in 0.3 - 2% by weight with the centella asiatica whole extract and tea tree oil and foimularing agents.
  • the cooling cum moisturising agent may be men hone ⁇ ycerine acetal or a mixture of 5-methyl-2 ⁇ (l-methyIemyl)-cyclohexanol, menthol propylene glycol carbonate, menthol ⁇ thylene glycol carbonate and peppermint oil, herein after referred to as menthol-mint compound.
  • menthol-mint compound a mixture of 5-methyl-2 ⁇ (l-methyIemyl)-cyclohexanol, menthol propylene glycol carbonate, menthol ⁇ thylene glycol carbonate and peppermint oil, herein after referred to as menthol-mint compound.
  • the menthone glycerine acetal or meitfhol-mint compound is in 0.3-0.5% by weight.
  • Formulating agents used to prepare the formulation may be anliydrous lanoline, ethylene glycol monostearate, mineral oil, carbomer, carbopol, propylene glycol, isopropyl myristate, myristyi myristate, sodium dioctyl sulfosuccinate (DOSS), bee wax, borax, absolute alcohol, cetyl alcohol, stearyl alcohol, a mixture of phenoxyethanol, methyl paraben, ethyl paraben, propyl paraben and butyl paraben, ethylene dia iiie tetracetic acid (EDT ), glyceryl monostearate, benzophenone, benzyl alcohol, propenic acid polymer, polysorbate 20, 2-amino-2-methyl-l-propanol, polyethyleneg ycol-40- hydrogenated castor oil, monomer of homopropenic acid, sorbiton monostearate, glycerine or butylated
  • Dyes like amaranth or brilliant blue or perfumes such as “BBA 1022” of Bush Boake Allen, USA; “BV 2723” of Takasago, Japan or “Cora ⁇ Hto” of Harmer & Reimer, India also may be added to the formulation which may be a el ⁇ cream or lotion.
  • the centella asiatica whole extract is in 1 -2% by weight and tea tree o ⁇ is in 0.2 - 2% by weight.
  • the mixing of the ingredients of the formulation is carried out at 25-75°C.
  • the formulation of the invention provides fast and effective relief from itching. Because it is based on cenie]ll& asiatica whole extract and tea tree oil, both of which are of plant origin, it is safe for use over a long period of time without adverse/side effects. It is economical due to the use of whole extract of centella asiatica which is easily available and cheap. Due to the cooling cum moisturising agent, the affected areas treated with the formulation of the invention experience cooling and soothing effects which provide a sense of iimnediate relief from itching. Besides these areas also remain moisturised thereby facilitating penetration of the actives into the skin thus acclerating healing. It is also convenien to use or apply as a cream, gel or lotion.
  • Centella asiatica whole extract 1.0 (Amsar Pvt Ltd, ⁇ ndore, India) Tea tree oil (Southern Cross
  • DOSS was dissolved in hot water (150 gms) at 80°C.
  • propylene glycol at 70°C phenonip and polysorbate 20 were added and this solution was mixed with the solution of DOSS.
  • Centella asiatica whole extract followed by carbopol were dispersed in the above solution and the dispersion stirred for 45 minutes.
  • mineral oil at 70°C tea tree oil and ethylene glycol monostearate, isopropyl myristate, lanoline anhydrous and "Frescolate” were added and stirred to form an emulsion.
  • the emulsion was mixed with the above dispersion comprising centella and cooled to 25°C.
  • 10% NaOH was added to adjust the pH to 6.68 and the formulation was made upto 100 gms by adding water to obtain a cream.
  • Isopropyl myristate 3.5 A iiiixtur ⁇ of phenoxyethanol, methyl paraben, ethyl paraben, propyl paraben and butyl paraben ("Phenonip",
  • An aqueous phase was prepared by miring polysorbate 20 glycerine, centella asiatica whole extract phenonip, EDTA and BHT in water at 70 - 75°C.
  • An oil phase was prepared by mixing mineral oil, bee wax, glyceryl monostearate, sorbiton monostearate, tea tree oil, myristyi myristate, isopropyl myristate and "Frescolate" at 25°C.
  • the oil and aqueous phases were mixed together followed by rnix ng with borax, perfiune, c ⁇ tyl and stearyl alcohol to give a lotion.
  • Glycerine 6.0 A mixture of phenoxyethanol, methyl paraben, ethyl paraben, propyl paraben and butyl paraben ("Phenonip",
  • Menthol-mint compound (“Opta int” of Harmer & Reimer, Maharashtra, India) 0.3
  • the volunteers provided ratings on a scale of 0-4 with respect to the parameters of swelling, redness, pain, itching and erythema wherein "0" implied 100%, “1” implied 25%, “2” implied 50%, “3” implied 75% and "4" implied 0% maaifest- ⁇ tion. of the above sa para eters.
  • the &v «stag Tsafcsngjs of the various parameters by the volunteers in the three groups using P, G and H at various time intervals were as shown in the following Table 2 Table
  • the anti-itch activity of the formulation of the invention is higher when compared to placebo and comparable with hydrocortisone butyrate.
  • a consumer use test was conducted for mosquito bite on 100 volunteers including women and children under 15 years of age. 50 volunteers

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

Abstract

L'invention concerne une formulation topique contre les démangeaisons qui comprend de l'extrait total de Centella asiatica à raison de 0,1-2 % en poids, et de l'huile de mélaleuca à feuilles alternes à raison de 0,1-2 % en poids, combinés à des agents de formulation ; un procédé de préparation de cette formulation contre les démangeaisons qui consiste à mélanger de l'extrait total de Centella asiatica à raison de 0,1-2 % en poids, et de l'huile de Mélaleuca à feuilles alternes à raison de 0,1-2 % en poids, avec des agents de formulation à une température comprise entre 25 et 80 °C.
PCT/IN2002/000228 2001-12-05 2002-12-04 Formulation topique contre les demangeaisons et procede de preparation de celle-ci WO2003047609A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP02796955A EP1461057A1 (fr) 2001-12-05 2002-12-04 Formulation topique contre les demangeaisons et procede de preparation de celle-ci
JP2003548864A JP2005515204A (ja) 2001-12-05 2002-12-04 局所適用かゆみ止め製剤およびその調製方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AU97047/01 2001-12-05
AU97047/01A AU771707B2 (en) 2001-12-05 2001-12-05 A topical anti-itch formulation and a process for the preparation thereof

Publications (1)

Publication Number Publication Date
WO2003047609A1 true WO2003047609A1 (fr) 2003-06-12

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PCT/IN2002/000228 WO2003047609A1 (fr) 2001-12-05 2002-12-04 Formulation topique contre les demangeaisons et procede de preparation de celle-ci

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EP (1) EP1461057A1 (fr)
JP (1) JP2005515204A (fr)
CN (1) CN1263474C (fr)
AU (1) AU771707B2 (fr)
WO (1) WO2003047609A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004073674A1 (fr) * 2003-02-19 2004-09-02 Bonapharm Gmbh Preparation a base d'huile d'arbre a the, ses procedes de production et son utilisation
WO2007010023A1 (fr) * 2005-07-21 2007-01-25 Svas Biosana S.R.L. Gaze medicale
GB2439385A (en) * 2006-06-20 2007-12-27 Sukhdip Singh Sidhu A preservative composition for a menthol and aqueous cream preparation
WO2008038806A1 (fr) * 2006-09-29 2008-04-03 Kobayashi Pharmaceutical Co., Ltd. Agent antipruritique
WO2021010953A1 (fr) * 2019-07-15 2021-01-21 The Procter & Gamble Company Compositions topiques de soin de la peau comprenant centella asiatica

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100459972C (zh) * 2006-11-07 2009-02-11 华南农业大学 一种祛痘润肤乳及其制备方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR4209M (fr) * 1965-03-03 1966-06-06
US4318906A (en) * 1979-06-25 1982-03-09 Establissement Rinrone Medicinal composition for external use for treating wounds
JPH08133952A (ja) * 1994-11-07 1996-05-28 Shiseido Co Ltd 皮膚外用剤
WO1998029089A1 (fr) * 1996-12-28 1998-07-09 Singh Verma Shyam B Preparations cosmetiques contenant des extraits de phyllanthus emblica et de centella asiatica et/ou de bacopa monnieri
DE29913476U1 (de) * 1999-08-02 1999-09-23 Breithaupt Gunter Präparat zur Behandlung von Hauterkrankungen
DE19910990A1 (de) * 1999-03-12 2000-09-14 Schwarz Monika Heilmittel auf Teebaumölbasis
KR20010084813A (ko) * 2000-02-29 2001-09-06 김종철 알레르기성 비염 치료용 향유조합

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR4209M (fr) * 1965-03-03 1966-06-06
US4318906A (en) * 1979-06-25 1982-03-09 Establissement Rinrone Medicinal composition for external use for treating wounds
JPH08133952A (ja) * 1994-11-07 1996-05-28 Shiseido Co Ltd 皮膚外用剤
WO1998029089A1 (fr) * 1996-12-28 1998-07-09 Singh Verma Shyam B Preparations cosmetiques contenant des extraits de phyllanthus emblica et de centella asiatica et/ou de bacopa monnieri
DE19910990A1 (de) * 1999-03-12 2000-09-14 Schwarz Monika Heilmittel auf Teebaumölbasis
DE29913476U1 (de) * 1999-08-02 1999-09-23 Breithaupt Gunter Präparat zur Behandlung von Hauterkrankungen
KR20010084813A (ko) * 2000-02-29 2001-09-06 김종철 알레르기성 비염 치료용 향유조합

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 200219, Derwent World Patents Index; AN 2002-146096, XP002978818 *
PATENT ABSTRACTS OF JAPAN *

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004073674A1 (fr) * 2003-02-19 2004-09-02 Bonapharm Gmbh Preparation a base d'huile d'arbre a the, ses procedes de production et son utilisation
WO2007010023A1 (fr) * 2005-07-21 2007-01-25 Svas Biosana S.R.L. Gaze medicale
US7923042B2 (en) 2005-07-21 2011-04-12 Svas Biosana S.R.L. Medicated gauze
GB2439385A (en) * 2006-06-20 2007-12-27 Sukhdip Singh Sidhu A preservative composition for a menthol and aqueous cream preparation
GB2439385B (en) * 2006-06-20 2010-09-29 Sukhdip Singh Sidhu Menthol in aqueous cream
WO2008038806A1 (fr) * 2006-09-29 2008-04-03 Kobayashi Pharmaceutical Co., Ltd. Agent antipruritique
WO2021010953A1 (fr) * 2019-07-15 2021-01-21 The Procter & Gamble Company Compositions topiques de soin de la peau comprenant centella asiatica

Also Published As

Publication number Publication date
AU9704701A (en) 2003-06-12
CN1516593A (zh) 2004-07-28
AU771707B2 (en) 2004-04-01
CN1263474C (zh) 2006-07-12
JP2005515204A (ja) 2005-05-26
EP1461057A1 (fr) 2004-09-29

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