Drug – bio-affecting and body treating compositions – Live hair or scalp treating compositions
Reexamination Certificate
2000-04-14
2001-08-07
Dodson, Shelley A. (Department: 1616)
Drug, bio-affecting and body treating compositions
Live hair or scalp treating compositions
C424S401000, C514S880000
Reexamination Certificate
active
06270752
ABSTRACT:
The present invention provides new formulations useful in the prevention and therapy of hair loss, based on the combination of substances with vasokinetic, antibacterial and antiandrogenic activities. It is known from the literature and from the cosmetic practice that the hair loss is negatively influenced by a reduced periferic microcirculation in the “
galea capitis
”, by its altered relation with the bacterial flora and by an altered local androgenic methabolism. The androgens, in particular the increased deposit of dihydrotestosterone in the hair bulb, are considered to play an important role in the pathogenesis of androgenic alopecia.
In Japanese patent JP-8310923, the essential oils obtained by steam distillation of Citrus aurantium peels, and of Salvia officinalis,
Mentha piperita, Eucaliptus globulus, Artemisia princeps
and
Rosmarinus officinalis
leaves and flowers, are considered inhibitors of testosterone 5-alpha-reductase and therefore useful in the treatment of alopecia, hirsutism and seborrhoea. European patent EP-433131A claims essential oils incorporated in lipidic material in the presence of known vasodilators like methyl nicotinate or other synthetic compounds for the prevention of hair loss or of dandruff formation, and like antiparasites. The chemical composition of these essential oils is not reported and their effects are likely mediated by other synthetic compounds present in the final formulations.
Now, a mixture of monoterpenes obtained through alcoholic extraction followed by distillation of some plants alone or in combination, has surprisingly shown vasokinetic, antibacterial and antiseborrhoic activities. The antibacterial activity which was known for the essential oils, was never associated to a marked vasokinetic activity, which was demonstrated by the control of the blood flow in cutaneous areas treated before and after the application of the mixture, using Laser Doppler technique and computer videocapillary-scopy.
The monoterpene mixture, combined with salicylic acid which is known to strongly inhibit cyclooxygenase I and II, and with saturated and unsaturated fatty acids having acyl chains from 10 to 14 carbon atoms, in particular 12 carbon atoms like lauric and myristic acids, has shown particularly useful for the treatment of hair loss in normal conditions and in androgenic alopecia. The monoterpene mixture can be obtained by mixing the single commercial monoterpenes in suitable ratios, or better by mixing roots, rhizomes, leaves, barks and seeds of some hexotic plants containing essential oils, which so far have never been used in cosmetics for the prevention or the therapy of hair loss (with the exception of rosemary oil, the cosmetic use of which is known and it is based on mechanisms different from those reported in the present invention), by steeping the same in 70% ethanol and finally by collecting the alcohol which contains the desired monoterpens through distillation at room pressure.
For example, the mixture of essential oils can be obtained by steeping in 70% aqueous ethanol similar amounts of rhizomes from
Curcuma longa, Myristica fragrans, Ferule galbaniflua, Liquidambar orientalis, Alpinia officinarum, Acorus calamus, Aloe vera, Cannarium commune, Commiphora molmol, Eugenia aromatica, Cinnamonum cassia, Curcuma zedoaria, Arnica montana, Rosmarinus officinalis
and lower amounts of oil of turpentine, the vegetal material amount being comprised between 10 and 50 g, preferably 20 g of each plant, in 1.2 1 of 70% ethanol for two days with stirring at room temperature, then distilling the alcohol at room pressure and collecting from 0.7 to 0.95 1 of distillate, preferably 0.850 lt; this distillate, after suitable water dilution, preferably up to 50% w/w, can be used as such, after removal of the insoluble oily residue, to inhibit hair loss or it can serve as the basis for the addition of other active ingredients. In particular the mixture obtained through distillation, combined with salicylic acid and menthol, after dilutions with 25 to 75% w/w hydroalcoholic solutions, preferably up to 50%, is steeped for a period of 3 to 60 days, preferably 30 days, and it is used after removal of insoluble oily residues.
Said hydroalcoholic mixture, which contains as the main ingredients beta-pinene, camphene, beta-myrcene, limonene, cineole (I,8-epoxy-p-menthane), camphor, linalool, bornyl acetate, isobornyl acetate, menthol, terpinen-ol, isoborneol, in ratios corresponding to the gas chromatogram of the Figure, is the first object of the invention. Said chromatogram was obtained using a HP-Innowax column (cross -linked polyethylene glycol, N. of part 19091 N-133, 30 m×0.25 mm I.D., 0.25 &mgr;m film thickness), according to the following temperature program: 60° C.×5 min, 60° C. to 250° C. at 3°/min, 250° C. for 3 min; injection with PTV (Programmed Temperature Vaporizer), from 120° C. to 250° C. The addition to the mixture of salicylic acid or the salts thereof and of fatty acids with anti androgenic activity, results in a surprising synergistic effect which reduces the hair loss improving the hair growth and strength. Therefore, a second object of the invention is represented by a formulation which contains the above described mixture in combination with salicylic acid or the salts thereof, and with saturated or unsaturated C
10
-C
14
fatty acids.
According to a preferred embodiment of the invention, the mixture of essential oils is obtained by steeping 20 g of
Curcuma zedoaria
rhizomes, 20 g of
Myristica fragrans
seeds, 20 g of
Cinnamomum cassia
branch bark, 20 g of
Eugenia aromatica
flowers, 20 g of
Acorus calamus
rhizomes, 20 g of
Zingiber officinalis
rhizomes and 20 g of
Alpinia officinarum
, in 0.9 1 ethanol. After one day, resin oils of
Ferula galbaniflua, Liquidambar orientalis, Aloe vera, Cannarium commune, Commiphora molmol, Arnica Montana, Rosmarinus officinalis
and turpentine oil are added to the steeped product in amounts variable from 5 to 50 g, to favour the alcohol dispersion of the resin oils.
Afterwards water is added up to an alcoholic grade of about 70% and after stirring the mixture for two hours at 40° C., the distillation is started and about 0.85 1 of alcoholic distillate are collected. The distillate is a colourless clear liquid with a strongly aromatic smell.
The distillate, without the addition of other substances, has vasokinetic, antibacterial and antiseborrhoic activities.
The monoterpene-containing hydroalcoholic mixture increases the volume and flow-rate at the capillary level, which, as mentioned above, is extremely important in the primitive and secondary alopecia. In fact, when the mixture is applied on the cutis, it integrates the blood flow in various organic districts and in particular it increases the blood flow in the “
galea capitis
” as it results from the data reported in table I, wherein the flow increment has been tested using Laser Doppler.
TABLE I
Cutaneous blood flow variations determined
using Laser Doppler after single administration of the
alcoholic distillate 1:1 diluted with water.
Substances
0
30′
60′
90′
120′
Distillate
4.45
13.33
14.12
9.7
10.32
Placebo
5.24
5.63
7.78
4.64
6.61
The administration of the formulations of the invention for periods variable from one week to three months causes in humans a remarkable reduction of androgenic alopecia as it results from the data reported in tables II and III. Table II reports the flow increase caused by the application of the formulation of the example I, as evidenced by Laser Doppler analysis. Laser Doppler flowmetry was performed to test the vasokinetic effects, using the PeriFlux(R) PF3 flowmeter which is an instrument emitting a subtle bundle of 632 nm wavelenght monocromatic light, which is produced by a low potency He—Ne laser source. By this technique, the scalp blood flow was measured in basal conditions and after the application of the test products, with an interval of 15 min from the first application (acute effect) and after 30, 60 and 90 day treatment (chr
Dodson Shelley A.
George Konata M.
Young & Thompson
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