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L'OREAL PATENTS AN ORAL TAURINE NUTRIENT
COMPOUND FOR THE TREATMENT OF
ANDROGENIC ALOPECIA

L'OREAL - A large cosmetic and hair care company based in France was recently issued a US Patent for an oral hair growth/hair loss prevention compound that utilizes the amino acid taurine in combinaton with certain catechins, polyphenols, and essential fatty acids. Of particular interest are the assertions and claims made for the oral administration of taurine in combination with polyphenols, catechins and EFA’s and its implications for the treatment of hair loss.

The usage of taurine at a dose of approximately 500 mg daily corrects what they term the "rigidification" of the connective sheath that surrounds the Pilosebaceous unit and hair follicles, specifically those affected by pattern hair loss. This is a novel and previously undisclosed angle on hair loss treatment that has yet to be touched upon in any of the medical literature or prior publications.

Additionally, it is claimed that specific oral extracts rich in polyphenols, proanthocyanidins, catechins, and essential fatty acids prevent the "cutaneous activation of testosterone and increases in sebaceous function, without sexual side effects". The specific compounds noted or grape seed extract, green tea extract, red wine extract (resveratol) in various milligram dosages that approximate what is already recommended in our protocol. The essential fatty acid compounds noted were a combination of omega 6 and omega 3 fatty acids. The omega 6 sources included Evening Primorose Oil, Borage Oil, and Black Currant Oil. The Omega 3 sources included fish and walnut oils.

Below are excerpts from the patent itself:

The use of taurine and/or hypotaurine and/or salts thereof that are acceptable in an oral composition, for the preparation of an oral composition that is useful for treating and preventing aging of the pilosebaceous unit and/or alopecia.

The use as claimed in claim 1, characterized in that the oral composition is useful for reducing or preventing impairment of the hair follicle induced by rigidification of the connective sheath.

The use as claimed in claim 1, characterized in that the daily dose of taurine and/or hypotaurine and/or acceptable salts thereof, as taurine equivalent, is between 10 and 500 mg/day.

The use as claimed in claim 1, characterized in that the taurine and/or hypotaurine and/or acceptable salts thereof are used in combination with at least one of the compounds chosen from fatty acids, polyphenols and extracts comprising the same.

The use as claimed in claim 12, characterized in that the polyphenols are chosen from flavones, flavonols, isoflavones, anthocyanins, flavanols, proanthocyanidins and flavanones, and stilbenes.

The use as claimed in claim 16, for the preparation of an oral composition that is useful for reducing or preventing the impact of testosterone on the pilosebaceous unit.

The use as claimed in claim 12, characterized in that the daily dose of polyphenols is from about 0.5 to 1000 mg/day.

A cosmetic process for treating and preventing disorders of the pilosebaceous unit via the oral administration of at least one fatty acid, one polyphenol or an extract comprising the same, optionally in combination with taurine and/or hypotaurine and/or acceptable salts thereof.

The present invention relates mainly to the use of taurine and/or hypotaurine in oral compositions for preventing and treating functional disorders of the pilosebaceous unit and especially for preventing and treating alopecia. The invention is also directed toward the use of fatty acid(s) polyphenol and/or extracts containing the same, optionally in combination with taurine in food supplements for treating and preventing these same disordersAmong the causes of alopecia, it has in fact been determined that impairment of the perifollicular connective tissue was reflected by rigidification of the connective sheath, which is thought to explain the miniaturization of the hair follicle, a sign of aging of the pilosebaceous unit.

[0005] Furthermore, these impairments in the hair are often accompanied by impairment in the condition of the scalp, such as the abundant production of sebum. Hypersecretion of sebum or seborrhea and its consequences, for example acne, often appear during puberty, but may continue into adulthood, especially in women, for hormonal reasons.

The Applicant has demonstrated, surprisingly, firstly that taurine is advantageous in regulating the impairment of the connective tissue of the hair follicle, and may thus be used advantageously in the treatment and prevention of aging of the pilosebaceous unit and/or of alopecia. Specifically, it has been possible to observe that taurine reduces the incorporation of proline without impairing that of leucine; this shows the advantage of taurine for specifically reducing the accumulation of collagen, without impairing the overall synthesis of proteins.

Moreover, the Applicant has noted that favoring an oral administration made it possible to obtain a hair-loss-preventing effect without inducing a stimulatory effect on the growth of the pilous system other than the hair system. It thus found that an oral administration of the active materials under consideration according to the invention was particularly effective for maintaining a good head of hair by acting on the hair density, i.e. the number of hairs per cm.sup.2 of scalp, and by reducing the heterogeneity of the hair diameters.

In one particular embodiment, the taurine, hypotaurine or acceptable salts thereof is (are) administered at a dose of from 0.5 to 4000 mg per day, as taurine equivalent, the fatty acid(s) is (are) administered at a dose of from 0.5 to 5400 mg/day and/or the polyphenol(s) is (are) administered at a dose of from 0.5 to 2000 mg/day.

By way of example, mention may be made of an extract of grapeseed containing 40% PCO, an extract of red wine containing 30% total polyphenols and/or an extract of green tea containing 30% catechins.

The procyanidin oligomers (PCO) may be used at doses of from 0.5 to 1000 mg/day and preferably 20 to 250 mg/day. They may be provided by an extract of grapeseed, which is dosed according to its PCO content. By way of example, for an extract of grapeseed containing 40% PCO, above, a dose of 150 mg/day, i.e. 60 mg/day PCO, is used.

[0052] Moreover, the catechins may be used at doses of from 0.5 to 1000 mg/day and preferably 20 to 300 mg/day. They may be provided, for example, by an extract of green tea containing 30% catechins, the extracted dose then being about 375 mg/day, i.e. 112.5 mg/day of catechins.

The Applicant has especially demonstrated that the oral administration of a dose of 37 mg/kg/day of a red wine concentrate, which is equivalent to a dose of 220 mg/kg/day for a person weighing 60 kg, had an efficacious effect on hair loss without showing any adverse side effects on the prostate. This is especially illustrated in the examples below:


9 FORMULATION OF SUGARCOATED TABLET TYPE mg/sugarcoated tablet Taurine 50 Grapeseed extracts (40% PCO) 100 Green tea extracts (30% catechins) 125 Zinc sulfate (22.75%) 22 Excipient for the core of the sugarcoated tablet Microcrystalline cellulose 70 Encompress .TM. 60 Magnesium stearate 3 Anhydrous colloidal silica 1 Coating agent Shellac 5 Talc 61 Sucrose 250 Polyvidone 6 Titanium dioxide 0.3 Colorant 5Example 21.

19 FORMULATION OF SUGARCOATED TABLET TYPE mg/sugarcoated tablet Taurine 50 Grapeseed extracts (40% PCO) 50 Green tea extracts (30% catechins) 125 Zinc sulfate (22.75%) 22 Excipient for the core of the sugarcoated tablet Microcrystalline cellulose 70 Encompress .TM. 60 Magnesium stearate 3 Anhydrous colloidal silica 1 Coating agent Shellac 5 Talc 61 Sucrose 250 Polyvidone 6 Titanium dioxide 0.3 Colorant 5.

[0169] This type of sugarcoated tablet may be taken 1 to 3 times a day.

0066] The sources of .gamma.-linolenic acid will be chosen from plant oils (evening primrose oil, borage oil, blackcurrant pip oil and hemp oil), and extracts of spirulina, Spirula maxima and S. platensis.

[0067] For the polyunsaturated fatty acids of the n-3 series, known as "omega-3" polyunsaturated fatty acids, the first is alpha-linolenic acid (18:3.omega.3); stearidonic acid (C18:4n-3) is also a fatty acid that is particularly advantageous in the invention.

[0068] Plant oils from walnut (Juglans regia) and from soybean (Glycina max), for example, are rich in omega-3 polyunsaturated fatty acids in the same respect as fish oils.

[0069] The .omega.3 polyunsaturated fatty acids are found, via the food chain, in zooplankton, crustaceans/molluscs and fish.

[0070] Fish oils constitute the main industrial source of EPA (eicosapentaenoic acid=20:5 .omega.3) and DHA (docosahexaenoic acid=22:6 .omega.3). However, microalgal biomasses may also constitute a raw material for extraction of .omega.3 fatty acids.

It is more than gratifying to see a major international corporation pursue a patent for some of the same recommendations we have been making for years. The mixing of taurine with varying combinations of these nutrients is essentially what has been patented. By reviewing the often confusing labyrinth of patent application text, one can decipher the ingredients used, and their dosages, and have "patent protected" information in hand that can be readily utilized long before a "patented" and often overpriced product becomes commercially available. In this case L'OREAL'S patented oral hair loss treatment can be easily formulated by using a combination of the disclosed ingredients.



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