WO2015040637A1 - Formulation améliorée de goudron de houille pour le traitement des pellicules et d'autres maladies du cuir chevelu, et son procédé de préparation - Google Patents

Formulation améliorée de goudron de houille pour le traitement des pellicules et d'autres maladies du cuir chevelu, et son procédé de préparation Download PDF

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Publication number
WO2015040637A1
WO2015040637A1 PCT/IN2014/000611 IN2014000611W WO2015040637A1 WO 2015040637 A1 WO2015040637 A1 WO 2015040637A1 IN 2014000611 W IN2014000611 W IN 2014000611W WO 2015040637 A1 WO2015040637 A1 WO 2015040637A1
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WO
WIPO (PCT)
Prior art keywords
composition
coal tar
oil
ingredients
formulation
Prior art date
Application number
PCT/IN2014/000611
Other languages
English (en)
Inventor
Amit Bhatia
Deepak Nandkishore KAPOOR
Baljit BANGAR
Original Assignee
MITTAL, Aman
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.)
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Publication date
Application filed by MITTAL, Aman filed Critical MITTAL, Aman
Publication of WO2015040637A1 publication Critical patent/WO2015040637A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/006—Antidandruff preparations
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/965—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of inanimate origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/02—Preparations for cleaning the hair

Definitions

  • the field of invention is pharmaceutical formulations. More specifically, the invention describes an improved, water dispersible coal tar formulation for treatment of dandruff and other scalp diseases and its method of preparation thereof.
  • Dandruff ⁇ Pityriasis capitis is a global phenomenon usually associated with excessive shedding of dead skin cells from the scalp. The process of dying and flaking off of the skin cells in unusually large amount accompanied by redness and irritation is considered as dandruff.
  • the fungus Malassezia furfur previously known as Pityrosporum ovale
  • dandruff can also be a manifestation of an allergic reaction to chemicals in hair gels/sprays, hair oils.
  • Dandruff Treatment Shampoos Traditionally, regular shampoos were used to get the symptomatic relief but their failure to provide proper treatment leads to the usage of OTC (over the counter) dandruff shampoos, which are classified on the basis of active ingredients as below:
  • Zinc pyrithione based e.g. Head & Shoulders®
  • Salicylic acid based e.g. Ion i 1 T®
  • Coal Tar is also known as 'liquor carbonis detergens ' (LCD) and 'liquor picis carbonis '.
  • Composition Coal tars are complex combinations of hydrocarbons, phenols and heterocyclic oxygen, sulphur and nitrogen compounds. It is prepared during the production of coke and gas and these are the by-products of destructive distillation of coal. Over 400 compounds have been identified in coal tars, and as many as 10,000 may actually be present. Composition of coal tar varies with its origin and type of coal (e.g. lignite, bituminous or anthracite) used to make it.
  • type of coal e.g. lignite, bituminous or anthracite
  • Coal tar has been used for dermatological conditions for over 2000 years, when it was referred to "asphalt" by Dioscorides, a Greek physician and pharmacologist. More recently, therapeutic coal tar in dermatology was emphasized in 1681 by Bechar and Serle. It has been a very popular traditional treatment for various types of scalp disorders including dandruff, atopic dermatitis, seborrheic dermatitis and chronic stable plaque psoriasis. Tar is used mainly in the treatment of various scalp disorders either alone or in combination therapy with other medications, phototherapy, or both.
  • coal tar is a valuable, safe and inexpensive treatment option for millions of people with psoriasis and other scalp or skin conditions.
  • Coal tar concentrations between 0.5% and 5% are safe and effective for psoriasis and no scientific evidence suggests that the coal tar in the concentrations seen in non-prescription treatments is (or is not) carcinogenic because there are too few studies and insufficient data to make a judgement.
  • Formulations based on coal tar Both prescription and non-prescription preparations of coal tar are available and include cleansing bars, creams, gels, lotions, ointments, shampoos, and other topical solutions and suspensions. When used in topical medications, it is supplied in the form of Coal Tar Topical Solution USP (United States Pharmacopeia), which consists of a 20% w/v solution of coal tar in ethyl alcohol, with an additional 5% w/v of polysorbate 80 USP; this must then be diluted in an ointment base such as petrolatum.
  • Coal Tar Topical Solution USP United States Pharmacopeia
  • Coal tar Being a crude material and having a complex composition, the exact mechanism of action of coal tar is not known yet. But there are many theories which are thought to play a role in treating varied scalp diseases by coal tar.
  • Coal tar belongs to a class of drugs known as keratoplasties. It works by causing the skin to shed dead cells from its top layer and slow down the growth of skin cells. This effect decreases scaling and dryness. Coal tar can also decrease itchiness from these skin conditions. Coal tar helps to decline the rapid proliferation of the skin cells and return to skin to a normal appearance.
  • Coal tar preparations are more effective and cheaper than most other available treatments for scalp psoriasis, including corticosteroids and calcipotriol and extend the length of remission without causing systemic side effects.
  • Topical lipid vesicles formulations Development of topical lipid vesicles formulation of the drugs is a promising alternative to overcome the problems associated with conventional formulations as discussed earlier.
  • Lipid vesicles were originated in 1965 by Bingham and the name given was "Bingham bodies" which play a major role in modelling biological membranes and in the transport and targeting of active agents. Consequently, a number of vesicular delivery systems such as liposomes, niosomes, sphingosomes, ethosomes, transferosomes and pharmacosomes were developed and used to improve therapeutic index of both existing and new drug molecules by encapsulating an active pharmaceutical ingredient inside the vesicular structure in one such system.
  • Lipid emulsions- Lipid emulsions are suitable for drug delivery of lipophilic drugs. Thus these systems have the potential for an improved benefit/risk ratio of the topical drug therapy and have high degree of effectiveness in the treatment of diseases.
  • Nano-emulsions- Nano-emulsions have several significant advantages including low skin irritation, powerful permeation ability, and high drug- loading capacity for the topical delivery when compared with other carriers.
  • coal tar based formulations Some of the commercially available coal tar based formulations are given in Table 1 below. All of these formulations contain coal tar solution which is a 20% w/v solution of coal tar in alcohol. Only one marketed formulation-LIPOTAR uses coal tar but that also contains alcohol (ethanol), which evaporates fast and has a drying effect on the skin.
  • Ionil T solution Lauromacrogol 1 150, Ethanol and
  • Coal tar solution is ethanolic extract of coal tar
  • Cooling sensates have also been added in compositions for the treatment of dandruff and other scalp diseases. Use of cooling sensates such as menthol and menthyl lactate is disclosed in U.S. Pat. No. 6,294, 186, cited above.
  • US Patent No. 6075017 A discloses a composition for the treatment of dandruff. The same is a synergistic combination of a cytotoxic agent and an antifungal agent.
  • the cytotoxic agent is selected from the group consisting of coal tar and zinc pyrithione and the antifungal agent is an antifungal imidazole.
  • US Patent No. 6319392 B l discloses a coal tar extract with reduced aromatic hydrocarbon content, method for obtaining same and dermatological and cosmetic compositions based on the same.
  • US 4178373 A discloses a coal tar gel composition for topically treating skin conditions, especially psoriasis and eczema which contains as an essential ingredient coal tar in a gel base. None of the prior art compositions or marketed formulations based on coal tar/coal tar solution discloses the composition of the present invention which comprises coal tar, water and emulsifiers as the major ingredients. Further, ethyl alcohol has been eliminated from the composition. Ethyl alcohol owing to its fast evaporation led to drying of the skin.
  • coal tar is already an established ingredient for treatment of scalp infections, it suffers from several disadvantages, particularly lack of aqueous dispersibility and messiness.
  • Topical formulations containing coal tar as the active ingredient are extensively employed in the treatment of skin disorders, such as dermatitis.
  • the active ingredient must be in a molecular dispersion to facilitate desired percutaneous absorption which is particularly important in achieving a therapeutic response for the management of psoriasis or eczema.
  • coal tar is practically insoluble in water.
  • the composition of the present invention is an improved coal tar based formulation which comprises coal tar, water and emulsifiers as the major ingredients. It has been able to overcome the limitations of existing formulations in an innovative manner by introduction of ingredients which enable formation of emulsion with lotion like consistency.
  • the formulation is thus a lipid based coal tar formulation with acceptable consistency, washability, enhanced penetrability and retention on the scalp and skin.
  • Salicylic acid is used in the formulation to remove excessive dead tissue from the skin.
  • coal tar and salicylic acid has been disclosed in prior art, nothing in the prior art discloses or suggests, the unexpected and unobvious advantages obtained as a result of using emulsifiers such as lecithin and tween in combination with coal tar and other anti-dandruff substances in an aqueous phase.
  • emulsifiers such as lecithin and tween in combination with coal tar and other anti-dandruff substances in an aqueous phase.
  • the combination of these elements in a personal care product provides the following benefits for a substantial period of time post-use:
  • the invention pertains to an improved, water dispersible coal tar formulation and its method of preparation thereof.
  • the formulation comprises coal tar, water and emulsifiers as the major ingredients. It offers distinct advantages of enhanced efficacy in treatment of diseases of scalp, enhanced patient compliance due to ease of application, reduced frequency of application and overall duration of treatment, improved general appearance of patient and reduced side effects due to reduction in the doses of the active ingredients used. Owing to elimination of ethyl alcohol from the composition, drying of skin is considerably reduced. Further, the composition of the present invention being water dispersible, is easy to wash and does not stain the clothes. DETAILED DESCRIPTION OF THE INVENTION
  • the present invention relates to an improved, water dispersible, coal tar and salicylic acid, lipid-based, oil-in-water type emulsion, with the consistency of a lotion, processes for preparing the same and methods of use and treatment.
  • This has been achieved by incorporation of one or more emulsifiers from about 4% to about 18% by weight, based on said composition and presence of aqueous phase as the major phase in the said composition which contains coal tar at concentration of about 1 to about 4% by weight.
  • the composition contains one or more emulsifiers selected from the group consisting of lecithin, sorbitan monoester (Span) and polyethoxylated sorbitan monoester (Tween).
  • Novelty - The novelty of the present invention lies in incorporation of emulsifiers into the composition along with coal tar and water, resulting in an improved, water- dispersible, coal tar formulation not disclosed in the prior art or in commercially available formulations.
  • inventive Step- The inventive step of the present invention lies in incorporation of emulsifiers into the composition along with coal tar and water, resulting in an improved, water- dispersible, coal tar formulation.
  • the formulation of the present invention is easy to apply and wash away, does not stain clothes, and has higher efficacy and reduced side-effects. This has been made possible by use of specific ingredients in specific ratios as given in Table 2 and incorporation of emulsifiers into the composition.
  • Industrial application- Formulation of the present invention can be manufactured on industrial scale and has applications in the treatment of various skin diseases, including scalp related skin problems like dandruff, seborrheic dermatitis and psoriasis.
  • Example 1 illustrates an improved coal tar based formulation and its various embodiments. The same are for illustrative purposes only and may not be construed as limiting in nature.
  • Example 1 illustrates an improved coal tar based formulation and its various embodiments. The same are for illustrative purposes only and may not be construed as limiting in nature.
  • Step 1 Heat and melt the components of oil phase as per the concentrations given above and mix them by gentle stirring.
  • Step 2 Prepare Carbopol and Poloxamer solutions as per the concentration separately and mix into the mixture prepared at Step 1.
  • Step 3 Add Tween into this mixture.
  • Step 5 Maintain temperature of oil and aqueous phase at 70 ⁇ 5 °C.
  • Step 6 Add oil phase in aqueous phase under continuous stirring and mixing.
  • Step 7 Keep temperature at 70 ⁇ 5°C till formation of homogenous dispersion.
  • Step 8 Allow the temperature of formulation to come down to room temperature under constant stirring and mixing.
  • the formulation formed is stable.
  • This particular embodiment offers the advantage of high concentration of aqueous phase wherein the coal tar is dispersed uniformly in the aqueous phase.
  • the improved coal tar formulation is in form of a gel due to presence of a gelling agent such as HPMC (Table 3).
  • a gelling agent such as HPMC (Table 3).
  • HPMC gelling agent
  • an oil such as oleic acid is also included in the composition.
  • Step 1 Heat and melt the components of oil phase.
  • Step 2 Mix the melted ingredients.
  • Step 3 Prepare HPMC solution and add tween into this.
  • Step 4 Maintain temperature of oil and aqueous phase at 70 ⁇ 5°C.
  • Step 5 Add oil phase in aqueous phase under continuous stirring and mixing.
  • Step 6 Keep temperature at 70 ⁇ 5°C till formation of homogenous dispersion.
  • Step 7 Allow the temperature of formulation to come down to room
  • Step 8 Transfer the obtained formulation in suitable container.
  • the improved coal tar formulation has the following composition (Table 4).
  • the formulation offers the advantages of having almond oil in place of oleic acid. Almond oil provides better nourishment to the skin.
  • Step 1 Heat and melt the components of oil phase.
  • Step 2 Mix the melted ingredients.
  • Step 3 Prepare Carbopol and Poloxamer solutions separately and mix.
  • Step 4 Add Tween into this mixture.
  • Step 5 Maintain temperature of oil and Aqueous phase at 70 ⁇ 5°C.
  • Step 6 Add oil phase in aqueous phase under continuous stirring and mixing.
  • Step 7 Keep temperature at 70 ⁇ 5 °C till formation of homogenous
  • Step 8 Allow temperature of formulation to come down to room temperature under constant stirring and mixing.
  • the improved coal tar formulation has the following composition (Table 5).
  • the formulation offers the advantages of having methyl salicylate and canthradin oil for their analgesic, counterirritant and hair growth enhancing action, respectively. Additionally, these agents are also useful in masking the unpleasant odor of coal tar.
  • Step 1 Heat and melt the components of oil phase.
  • Step 2 Mix the melted ingredients.
  • Step 3 Prepare HPMC and Poloxamer solutions separately and mix.
  • Step 4 Add Tween into this mixture.
  • Step 5 Maintain the temperature of oil and aqueous phase at 70 ⁇ 5 °C
  • Step 6 Add oil phase in aqueous phase under continuous stirring and mixing.
  • Step 7 Keep temperature at 70 ⁇ 5 °C till formation of homogenous
  • Step 8 Allow the temperature of formulation to come down to room
  • the basic innovation lies in the combination of specific ingredients comprising coal tar, water and emulsifiers in specific concentrations, due to which the formulation offers the distinct advantages not offered in the prior art or the existing formulations available commercially. It offers distinct advantages of enhanced efficacy in treatment of diseases of scalp, enhanced patient compliance due to ease of application, reduced frequency of application and overall duration of treatment, improved general appearance of patient and reduced side effects due to reduction in the doses of the active ingredients used. Owing to elimination of ethyl alcohol from the composition, drying of skin is considerably reduced. Further, the composition of the present invention being water dispersible is easy to wash and does not stain the clothes.
  • the invention thus comprises an improved, water dispersible coal tar formulation in which coal tar, water and emulsifiers are the major ingredients. Variations in the formulation can easily be carried out by those skilled in the art, once the basic concept is understood and such embodiments should be regarded as within the scope of the present invention.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une formulation aqueuse améliorée de goudron de houille et son procédé de préparation. Ladite formulation comprend du goudron de houille, de l'eau et des émulsifiants en tant que principaux principes actifs. Elle présente des avantages distincts en termes d'efficacité améliorée dans le traitement de maladies du cuir chevelu, de respect amélioré du traitement par le patient grâce à sa facilité d'application, de diminution de la fréquence d'application et de la durée totale du traitement, d'amélioration de l'aspect général du patient, et de diminution des effets secondaires en raison de la réduction des doses des principes actifs utilisés. Grâce à l'élimination de l'alcool éthylique de la composition, le séchage de la peau est considérablement réduit. En outre, la composition selon la présente invention est dispersible dans l'eau, facile à laver et ne tâche pas les vêtements.
PCT/IN2014/000611 2013-09-19 2014-09-19 Formulation améliorée de goudron de houille pour le traitement des pellicules et d'autres maladies du cuir chevelu, et son procédé de préparation WO2015040637A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2764DE2013 2013-09-19
IN2764/DEL/2013 2013-09-19

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WO2015040637A1 true WO2015040637A1 (fr) 2015-03-26

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109745261A (zh) * 2019-03-06 2019-05-14 中国人民解放军陆军特色医学中心 一种头皮护理液及其制备方法
CN111511209A (zh) * 2017-09-22 2020-08-07 德科全球收后处理股份私人有限公司 通过可食用涂层处理和控制水果采后生理病害的方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4102995A (en) * 1976-05-13 1978-07-25 Westwood Pharmaceuticals Inc. Tar gel formulation
WO1998052518A1 (fr) * 1997-07-02 1998-11-26 Neutrogena Corporation Procedes d'utilisation de compositions contenant du dichlorophenyle imidazoldioxolanne pour traiter l'eczema seborrheique, les pellicules, le psoriasis et l'acne, et leurs compositions
US20070104747A1 (en) * 2005-10-28 2007-05-10 Virginie Masse Cosmetic composition comprising at least one anti-dandruff agent and also oxyethylenated sorbitan monolaurate, and cosmetic treatment process using said composition
WO2012138696A2 (fr) * 2011-04-07 2012-10-11 The Procter & Gamble Company Compositions de shampooing à dépôt accru de microcapsules de polyacrylate
WO2013015665A1 (fr) * 2011-07-25 2013-01-31 Aguilar Sanchez Jose Luis Formulation à base d'extrait de plantes médicinales, de goudron de houille et d'acide salicylique pour lutter efficacement contre le psoriasis, procédé d'obtention de l'extrait et modes d'administration de cette formulation

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4102995A (en) * 1976-05-13 1978-07-25 Westwood Pharmaceuticals Inc. Tar gel formulation
WO1998052518A1 (fr) * 1997-07-02 1998-11-26 Neutrogena Corporation Procedes d'utilisation de compositions contenant du dichlorophenyle imidazoldioxolanne pour traiter l'eczema seborrheique, les pellicules, le psoriasis et l'acne, et leurs compositions
US20070104747A1 (en) * 2005-10-28 2007-05-10 Virginie Masse Cosmetic composition comprising at least one anti-dandruff agent and also oxyethylenated sorbitan monolaurate, and cosmetic treatment process using said composition
WO2012138696A2 (fr) * 2011-04-07 2012-10-11 The Procter & Gamble Company Compositions de shampooing à dépôt accru de microcapsules de polyacrylate
WO2013015665A1 (fr) * 2011-07-25 2013-01-31 Aguilar Sanchez Jose Luis Formulation à base d'extrait de plantes médicinales, de goudron de houille et d'acide salicylique pour lutter efficacement contre le psoriasis, procédé d'obtention de l'extrait et modes d'administration de cette formulation

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111511209A (zh) * 2017-09-22 2020-08-07 德科全球收后处理股份私人有限公司 通过可食用涂层处理和控制水果采后生理病害的方法
CN109745261A (zh) * 2019-03-06 2019-05-14 中国人民解放军陆军特色医学中心 一种头皮护理液及其制备方法
CN109745261B (zh) * 2019-03-06 2021-09-21 中国人民解放军陆军特色医学中心 一种头皮护理液及其制备方法

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