Title of Invention


Abstract A process of preparing a herbal composition comprising of reacting (a) a herbal (botanical) ingredient from the group consisting of Soya Sterols in an amount from 0.01% to 1.5% by total weight of the composition (b) standardised herbal (botanical) extract of Centella asiatica containing at least 40% asiaticosides, the concentration of which ranges from 0.01% to 1% by total weight of the composition (c) natural vegetable oils of Olea europaea (Olive) and Prunus amygdalus dulcis (Sweet Almond), each in a range from 1% to 3% by total weight of the composition.
Full Text The Patent Act, 1970
Complete Specification
(Section 10; Rule 13)
A process for preparing herbal composition
Godrej Soaps Limited
Pirojsha Nagar, Eastern Express Highway Vikhroli (E), Mumbai- 400 079 (Maharashtra)
An Indian Company
The following specification particularly describes and ascertains the nature of this invention in the manner in which it is to be performed:
21/3/2000 20-1-2005

This invention relates to a herbal cosmetic composition for controlling wrinkle formation due to photo-damage.
The ageing of the skin is attributed to two processes; true ageing related to the intrinsic passage of time and photo-ageing resulting from chronic UV light exposure. The physiologic decline of skin as one ages is, manifested by changes in the appearance of skin of which the wrinkling of the skin is most prominent. Unlike intrinsic or chronologic ageing, photo-ageing is related to cumulative damage to the cellular constituents of the skin, at least in part at the DNA level by UV and infrared radiation (Calderone, D.C., and Fenske, N.A., The clinical spectrum of actinic elastosis, J. Am. Acad. Dermatol., 1995 32,1016-24.)
Photo-ageing accounts for more than 90% of the skin's age-associated cosmetic problems and is almost synonymous with "true chronologic ageing" in the public's mind. It has been pointed out lately that photo-ageing changes start in skin at a very young age. The increase of freckles (solar lentigenes) is noticeable by the age of three to five years. Chronologic ageing of the skin without sunlight exposure leads to remarkably few visible changes. In contrast, photo-ageing leads to marked changes in the skin such as wrinkles, roughness, sallowness, mottled hyper-pigmentation, telangiectasias, laxity, and a variety of benign and malignant neoplasms. Evidence of photo-ageing is found primarily in the dermal connective tissue, although sun damaged skin typically has a thicker startum corneum. The extracellular matrix of the dermis consists mainly of type I collagen, some type III collagen, elastin, proteoglycans, and fibronectin. Chronically sun-exposed sites, show a loss of mature type I collagen and a relative increase in type III collagen.
There have been a number of pharmacologic developments to reverse the visual signs of photo-ageing. These include retinoic acid and its derivatives, alpha-hydroxy acids, antioxidants, and many natural products. These materials have been tested and have performed with variable effectiveness. Solar photo-ageing is a profound change in the skin architecture that evolves over a long time to the final state. Therefore prevention is a better approach than cure. (Duthie, M.S., et al., The effect of ultraviolet radiation on the human immune system, Brit. J. Dermatol., 1999 140 995-1009; Gilchrest. B.A., A review of skin aging and its medical therapy, Brit. J. Dermatol, 1998 135, 867-875.)
A number of successful present-day beauty treatments and lines of cosmetics are promoted for their plant-origin ingredients. There are efficacious herbs with useful properties for cosmetic applications. Many herbs, or plant-derived biological materials, have been used to treat the skin to improve its appearance.
The present invention is based on the use of skin beneficial herbals (botanicals) comprising of plant sterols (phytosterols), extract and oils which have properties that help in controlling the formation of wrinkles.
Phytosterols are regarded as non-toxic substances, common in a vegetable diet. The chemical structures of phytosterols are similar to cholesterol but can only be synthesised by plants. (Bhattacharyya, A.K., et al., The journal of Investigative Dermatology, 80, (1983), 294-296.)

The natural content and composition of phytosterols in vegetable oils is characteristic for each raw material. Phytosterols occur mainly in free form or as esters of fatty acids. The main phytosterols found in vegetable oils are Beta-sitosterol, Campesterol, Stigmasjerol, Delta 5-avenasterol and Delta 7-stigmasterol. Depending on their structure, sterols and their derivatives'- such as fiormohes and vitamin precursors - impart various important biological functions within the.human body and skin.
Sterols have been demonstrated to have a structural role, similar to cholesterol, by interacting with the
skin lamellar lipid layers, increasing the stability and lowering the permeability and fluidity of the
membranes. Increased skin moisturisation has been demonstrated for both topical phytosterols and
( Chlebarov, S., Notabene Medici 2 and 3, (1989), 74-76 and 124-127; Zettersten, E.M., et al.,.
Journal of the American Acad, of Dermatology, 37(3 part 1), (1997), 403-408.)
An additive protective effect against UV-B and UV-A radiation has been further reported from binary combinations of an antioxidant and an(anti-inflammatory agent.. (Bissett, D. L., et al, J. Soc. Cosmet. Chem., 43, March/April, (1992), 85-92.) The effect of phytosterols is exhibited mainly on skin that is either damaged or harmed by environmental influences.(R.Wachter, B. Salka and A. Magnet, Cos & Toil 110 (7) 72-82(1995).)
Scientific research - including a large number of in vivo and in vitro tests has confirmed that natural phytosterols may protect the skin and the cell membranes from environmental insults caused by various sources, such as UV-radiation, chemical pollutants, unfavourable climatic conditions and irritants. (Functional Lipids; Karslshamns Technical Bulletin, Sept. 1998.)
Due to their important skin smoothing properties they are good natural ingredients for anti-ageing formulations. (Matzik, I. & Koch, C, Natural Cosmetics at the Millennium, SOFW- Journal (126), Jan-Feb. 2000.) Phytosterols nave been claimed to enhance collagen synthesis. (Speciality Lipids, in Harry's Cosmeticology, 8th Ed., 2000, 323-331)
Centella asiatica extract
The plant, Centella asiatica, grows in India, Madagascar and in tropical areas of Africa and Indonesia. Centella asiatica contains pentacyclic triterpene_acids of the alpha-amirin series, both in free form and as glucosides; madecassic acid, asiatic acid, asiaticosides and madecassosides. In vitro studies have shown that secretion of Collagen-I, by human fibroblasts, is enhanced by asiaticosides and madecassosides. Madecassosides enhance the secretion of Collagen-III. Collagen-I is the most abundant type of collagen present in human connective tissue (from 80%-90% of total collagen content), while Collagen-III comes in second.
Influence of Asiatic Acid, Madecassic Acid and Asiaticoside on Human Collagen-I Synthesis.( F. Bonte, M. Dumas, C. Chaudgne and A. Meybeck. Planta.Med. 60, 1994, pp. 133-135), A reinvestigation of the triterpenes of Centella asiatica. (B. Singh and R.P. Rastogi, Phytochemistry, Pergamon Press, 1969, Vol.8, pp.917-921), Chemical examination of Centella asiatica. ( B. Singh and R.P. Rastogi. Phytochemistry,

Pergamon Press, 1968, Vol.7, pp.1385-1393.) There are a few natural products, which are known to stimulate collagen synthesis one of these is Centella asiatica.
Maquart et al., in Conn. Tissue Res., (1990), 24 pp. 107-120, showed that the triterpene' extract from Centella asiatica stimulated collagen synthesis in fibroblast monolayer cultures, and asiatic acid was found to be the major component responsible for collagen synthesis stimulation.
Collagen, the predominant matrix skin protein, is known to impart tensile strength to skin. If.has been shown that collagen is significantly reduced with age and UV exposure. The degradation or destruction of the architecture of these proteins decreased the tensile strength of the skin causing wrinkles and laxity. Many studies involving human subjects have shown that collagen type I is decreased mth increasing severity of photo-damage and some correlation in the histology of wrinkles and reduction in collagen levels in the sun-exposed skin has been reported. ( Kligman, A., JAMA, (1969), 210, pp. 2377-2380; Lavker, R., J. Inv. Derm., (1979), 73, 79-66; Smith, J. et al., J. Inv. Derm., (1962), 39, pp. 347-350 and Shuster, S. et al., Br. J. Dermatol., (1975), 93, pp. 639-643.)
Studies indicate that Centella asiatica promotes greater elasticity and suppleness to the skin by its action on the collagen synthesis by the fibroblasts. (Tenni, R. et al., J. Biochem, (1988), 38. pp. 69-77; Maquart, F. et al., Actualite Therapeutique, (1989), pp. 1571-1574.)
Centella asiatica is also suitable for other cosmetic applications, i.e., skin conditioning improvement, anti-cellulite effect, and improvements in skin colour. (Adolphe, M. et al., Int. J. Cosmetic Soc, (1984), 6, pp. 55-58.)
Natural tocopherols are the most important lipid soluble antioxidants, and essential nutrients for humans and animals. Tocopherols are relatively heat stable and non-toxic substances used in food products as well as in cosmetic and pharmaceutical applications. Tocopherols act by a free radical scavenging mechanism inhibiting lipid peroxidation in biological cell membranes and cell organelles, as well as acting as a quencher of excited oxygen atoms (singlet oxygen) which are part of numerous photo-oxidation reactions, considered to be one of the factors for premature ageing of skin. ( Kamal-EldiiCA., AppeTqvSt, L-A7Lipids, 31, no.7, (1996), 671-701; Traber, M.G., et al, Lipids, 33, no 1, (1998), 87-90; Rieger, M.M., Cosmetic & Toiletries, 108, December (1993), 43-56.)
Vitamin E is the generic term for all substances possessing vitamin E activity. The natural d-tocopherols have been proven to show significantly higher biological activity than the synthetic dl-tocopherols. The two most important tocopherols in topical applications, are generally agreed to be the d-alpha and d-gama-tocopherols, (Kamal-Eldin, A., Appelqvist, L-A, Lipids, 31, no.7, (1996), 671-701; Ehnadfe, I. and Wagner, K-H., Fett/Lipid, 99, no.7, (1997), 234-238.)
UV radiation damage to the human skin is related to both short-term and long- term effects. Topical application of natural alpha and gama tocopherols prior to irradiation has been demonstrated in several in

vivo studies to reduce UV induced skin damage such as eiythema, oedema, skin sensitivity and skin wrinkling. (Beijersbergen van Henegouwen, G.M.J.," Journal of Photochemistry and Photobology B.Biology 29, (1995), 45-51.; Gensler, H„ et al., Nutrition & Cancer,,26t no 2,: (1996), 183-191; Potokar, M. et al., Fat Sci. TechnoL. 92, no 10, (1990), 466-410; Colin, C, et al., 1FSCC presentation, 1, A105, (1994) 50-72; Record, I.R., et al. Nutr Cancer 16, (1991), 219-22.) Research has further demonstrated, in vitro, that tocopherols may protect epidermal cells from the deleterious effects of specifically UV-A irradiation. (Clement-Lacroix, P., et al., Br. J Dermatol., 134, (1996), 77-84.)
Tocopherols are also shown to have a physico-chemically stabilising effect in biological membranes. The proposed interaction with membrane phospho-lipids may have functional consequences such as reduction of the membrane permeability and prevention of phospho-lipid degradation. (Kagan, V. E., Ann. N.Y.Acad Sci., 570, (1989), 121-135; Lucy, J.A., Ann. N.Y. Acad. Sci., 203, (1972), 4-11;
Diplock, A.T. and Lucy J.A., Febs letters, 29, no. 3, (1973), 205-210.) The protection of cell membranes is shown to exert beneficial effects on the water binding and moisturisation properties of the skin. (Veris Research Summary, May 1997.)
Olea europaea oil
Oil of Olea europaea (Olive oil) has high Oleic, Palmitic Linoleic fatty acid contents which are good for skin., The oil has been proven to efficiently scavenge the super-oxide anion (Visoli, Biochem Biophys Rev Com 247 60-4 (1988) ) and reduce lipid peroxidation by 70% (De La Cruz, Biochem Biophys Acta 1485 36-44 (2000)). The oil has strong anti-oxidant properties. It also has skin soothing properties and gives relief from pruritus, burns, stings and is a good vehicle for liniments. Olive oil has been found to be very beneficial for UV irridated skin. (Ichihashi, J Dermatol Sci 23 suppl. 1 45-50 (2000))
Prunus amygdalus dutch oil
Sweet Almond Oil has a high oleic content (of more than 50%), it is good for skin moisturisation, conditioning and nourishment.
The present invention relates to a process for preparing a composition, for topical application to human skin, comprising of plant-sterols (phytosterols), herbal (botanical extract and alls in a cosmetic vehicle, providing synergistic effects, which control the-wrinkle formation on the skin due to photo-damage and also for the composition prepared by this process.
According to the process of preparing the composition of the invention consists of mixing of the herbal (botanical) extracts and oils together comprising 5% to 10%, bv the total weight of the composition, most preferably 5% to 7%.

Phytosterols extracted from Glycine max (or Soya sterols) are the essential ingredient of the inventive composition. The Soya Sterols used in the present invention are of 95% (+) purity, having the following composition; Beta Sitosterols (60%-70%), Stigmasterol (20%-30%) and Campesterof(5%-10%. The concentration of Soya Sterols in the inventive compositions ajre in the range of from 0.01% to 2%, most preferably in the range of from 0.05% to 1% by the total weight of the composition to attain optimum activity at a minimum cost.
Soya Sterols have been extracted from Glycine max of Indian origin by a process, which gives odourless and colourless pure white powder, fit for cosmetic applications.
The Centella asiatica extract containing minimum of 40% asaiticosides used in present composition is an organic soliest extract, e.g., alcoholic extract, ethyi acetate extract, propylene glycol extract, ethylene glycol extract, ether extract. Centella extract is used as a source of asiaticosides. The extract must be present in the composition in an amount of from 0.01% to 1% Preferably in the range of from 0.1% to 1% but most preferably in the range from of 0.1% to 0.5%^by the total weight of the composition. The extract is from Qentella asiatica of Indian origin using a process whereby the final product is a low odour, light coloured, water-soluble, spray dried extract powder, suitable for cosmetic applications.
The composition, further comprises of natural oils of Olea europaea (Olive) and Prunus amygdalus dulcis (Sweet Almond) each in the range of 0.5% to 4%, preferably 1% to 2.5% The alpha tocopherol is used in the range of 0.01% to 2%, preferably from 0.1% to 1% by the total weight of the composition.
The composition of the invention also comprises of a cosmetic vehicle, which acts as a dispersant or carrier for the active components, so as to facilitate their optimal distribution when the composition is applied to the skin. Vehicle other than water can include emollients, solvents, and humectants. The cosmetic vehicle is usually form from 5% to 40%, preferably from 5% to 20% by the total weight of the emulsion, and can, in the absence of other cosmetic adjuncts, form the balance of the composition.
Other active ingredients present in the composition of the present invention are sunscreens.
Sunscreens include those materials commonly employed to block ultraviolet light, especially UV-A
and UV-B radiation, which are responsible for photo-damage and premature wrinkling of the skin.
Illustrative compounds are the derivatives of PABA, Cinnamate and Salicylate. For example, Octyl
methoxycinnamate, 2-hydroxy-4-methoxy benzophenone (also known as oxybenzone) and Methylene
Bis-Benzotriazolyl Tetramethylbutylphenol can be used The type and exact amount of sunscreen(s)
employed in the emulsions can vary depending upon the degree and type of protection desired from
the sun's UV -A/B radiation. The UVA sunscreens may be present in a concentration from 0.1% to
4%, while the UVB sunscreens in a concentration from 0.1% to 4% by the total weight of the
The long chain fatty acids and fatty alcohols are used as emulsifiers. In the present invention Glycerol stearate and Glycerol stearate with PEG 100 stearate have been use as emulsifiers. Stearic acid and Cetostearyl alcohol are used as co-emulsifiers. Amount of the emulsifiers and the co-emulsifiers in the composition of the invention ranges from 0.1% to 5% by the total weight of the composition.

Emollients are incoiporated into the cosmetic composition of the present invention, levels of which may range from 5% to 10% by weight of the total composition. Emollients may be classified under general chemical categories of esters, polyols and hydrocarbons.
Esters include Isopropyl myristate, 2-Octyldodecyl myristate, Cetyl 2-ethyl hexonate etc., in the present invention. Isopropyl myristate and Glyceryl myristate are preferred in the range of 0.5% to 10%.
Polyols, which are linear and branched chain alkyl polyhydroxyl compounds, serve as emollients, e.g. Propylene glycol, Sorbitol and Glycerin. Butylene and Propylene glycol are also especially used as penetration enhancers. In the present invention Propylene glycol is preferred in the range of 1% to 10% by weight of the composition.
Hydrocarbons having chain of carbon atoms from 12 to 30, serve as emollients. Examples include Mineral oil, Petroleum jelly, Squalene etc., in the present invention preferably mineral oil is used in a concentration 0.1% to 5% by total weight of the composition.
Silicones contain the siloxane chain and examples include Methylpolysiloxane and Dimethylpolysiloxane. In the present invention Dimethylpolysiloxane is preferred in the range from 0.1% to 5% by total weight of the composition.
In the present invention Methyl paraben and Propyl paraben are preferred as preservatives and Di-sodium EDTA as a chelating agent in amounts ranging from about 0.5% to 1% by total weight of the composition. Other minor components may include perfumes. Amounts of which may range anywhere from 0.01% up to 1% by total weight of the composition.
As an example the cosmetic composition of the invention was prepared by mixing the following ingredients in the percentages given against each of them.
Phase A
Stearic Acid Cetostearyl Acid GMS (SE) Propyl Paraben Dimethicone
Phase B
Water (sufficient to make 100%) Propylene Glycol Methyl Paraben EDTA (Di Sodium)
Phase C
Botanical Extract

Phase D

Ingredients %
Propylene glycol 3.00
Methyl paraben 0.15
Ethylenediaminetetraacetic acid 0.05
Methylene Bis-Benzatriazolyl - 0.25
Tetramethylbutylphenol Stearic acid 0.50
Cetostearyl alcohol 2.25
Glycerol monostearate 2.00
Propyl paraben 0.10
Polydimethylsiloxane 0.50
Glyceryl Stearate & PEG 100 Stearate 1.00
Octyl methoxycinnamate 1.00
Isopropyl myristate 2.00
Mineral Oil 2.00
Soya Sterols 0.50
Centella asiatica extract 0.10
Prunus amygdalus d ulcis oil 2.00
Oleo europaea oil 2.00
Alpha-tocopherol 0.50
Perfume 0.20
DM Water q.s.

The cosmetic composition of the aforementioned example was tested against a commercial wrinkle control cream by a qualified dermatologist in a panel study, using a half face design with right and left balance. The objective of the study was to test the efficacy of the inventive formulation for a set of attributes, which are investigated for anti-ageing cosmetic products. The period of study was eight weeks. Result of the study demonstrated that the inventive formulation was effective for the attributes it was tested for. The cosmetic composition was also tested for dermatological safety aspects by an external accredited testing laboratory.

We claim:
1. A process of preparing a herbal composition comprising of reacting (a) a herbal (botanical) ingredient from the group consisting of Soya Sterols in an amount from 0.01% to 1.5% by total weight of the composition (b) standardised herbal (botanical) extract of Centella asiatica containing at least 40% asiaticosides, the concentration of which ranges from 0.01% to 1% by total weight of the composition (c) natural vegetable oils of Olea europaea (Olive) and Prunus amygdalus dulcis (Sweet Almond), each in a range from 1% to 3% by total weight of the composition.
2. A process as claimed in claim 1 wherein the resulting mixture is further mixed with alpha-tocophetol In a range from 0.01% to 1% by the total weight of the composition and a known cosmetic vehicle or carrier.
3. A process as claimed in claim 1 wherein the Soya Sterols having the following composition; Beta Sitosterols (60%-70%), Stigmasterol (20%-30%) and Campesterol (5%-10%).
4. A process as claimed in claim 1 wherein the Centella asiatica is in the range of 0.1% to 0.5% by
total weight of the composition.
Dated this 20th day of June 2001

H. W. Kane Applicant's Agent


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Patent Number 204341
Indian Patent Application Number 244/MUM/2000
PG Journal Number 43/2008
Publication Date 24-Oct-2008
Grant Date 15-Feb-2007
Date of Filing 21-Mar-2000
# Inventor's Name Inventor's Address
PCT International Classification Number C 11 B 1/00 1/07
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA