Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2000-11-13
2002-06-18
Dees, José G. (Department: 1619)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S078070, C424S404000, C424S065000, C514S887000, C514S859000, C514S252010
Reexamination Certificate
active
06406708
ABSTRACT:
The present invention relates to a new composition for topical application comprising squalane, cyclodextrin, and from 1.5 to 8% of a pharmaceutically and/or cosmetically acceptable aliphatic mono-, di- and &agr;-hydroxy carboxylic acid having from 2 to 10 carbon atoms. The balance is selected from other compatible pharmaceutically and/or cosmetically acceptable active substances used for the treatment of acne and pharmaceutically and/or cosmetically acceptable paste, ointment or cream bases and additives. Further included is a method for the preparation of the new compositions as well as a method of treatment of acne. The composition may be used as a cosmetic or therapeutic, and for the preparation of a drug for treatment of diseases caused by attacks of micro-organisms, especially for the treatment of acne.
BACKGROUND OF THE INVENTION
Within the cosmetic field squalane C
30
H
62
has been used as skin lubricants in cosmetic and hygienic preparations and as fixatives in perfumes, in concentrations of up to 50%.
U.S. Pat. No. 5,079,003 to Schadiffi A., discloses creams or lotions comprising emulsions of fish oils, such as shark liver oil, squalane, and squalene, used as moisturisers, as bases for cosmetics, as hand and body lotions and as sunburn preventives. Compositions are described also comprising numerous other ingredients with therapeutic and synergistic effects on the skin.
Within the therapeutical field, squalane as well as squalene have been used as penetration enhancers of actives, and in adjuvants of vaccines (see e.g. Hoffman S L et. al. Am J Trop Med Hyg 1994 November; 51(5): 603-12). As components of oil-emulsion based adjuvants in injection preparations they are considered to have anti-irritating properties (see e.g. Stone H D et. al. Avian Dis 1990 October-December; 34(4): 979-83), and as such they also have shown an immunostimulating effect (Allison A C, Int J Technol Assess Health Care 1994 Winter; 10(1): 107-20). Moreover, they both are deemed to have a proliferation stimulating effect on the dermal as well as the muscular tissues.
Cyclodextrin is a molecule capable of forming an inclusion complex with squalane. In this type of complex cyclodextrin plays the role of a “host molecule”, forming a cavity lodging one or several “guest molecules”. In a work intituled “Cyclodextrin Chemistry” (Ed. Springer Verlag 1978) it is stated that the cavity of the cyclodextrin molecule has a calculated diameter of 7 Å and a depth of 7 Å. This may be correlated to the diameter of the “guest molecule”, which for the squalane molecule can roughly be estimated to 5 Å and 30-35 Å respectively.
Our co-pending patent application WO9822083A1 (claiming priority from our co-pending application SE 9604193-4, filed Nov. 15, 1996) relates to compositions comprising as active ingredient (i) one or several components derived from an extract of crude shark liver oil, including squalane, and (ii) one or several carbohydrates forming inclusion and/or chelate complex, including cyclodextrin, with (i) and optionally (iii) one or several non-shark liver oil derived therapeutically or cosmetically active agents. In the Example also 0.15% by weight of sorbic acid is included as a preservative.
WO9421225A1 relates to a skin care composition comprising a conjugate of vitamin A derivative and &bgr;-cyclodextrin for therapeutic or prophylactic treatment of ageing symptoms in skin.
Patent Abstracts of Japan, Vol. 11, No. 69, C-407, abstract of JP 61-227517 A and the European patent 0 366 154 disclose cosmetic compositions comprising cyclodextrin derivatives and squalane.
However, prior art gives no information about the new and unexpected advantages on the treatment of acne, obtained by the addition, to a composition, for topical application, comprising squalane and cyclodextrin, of from 1.5 to 8% of a pharmaceutically and/or cosmetically acceptable aliphatic mono--, di- and &agr;-hydroxy carboxylic acids having from 2 to 10 carbon atoms. According to our findings an amount as low as 0.15% of sorbic acid does not give any anti-acne effect.
DESCRIPTION OF THE INVENTION
The present invention relates to a composition, for the treatment of acne, comprising from 2 to 8% of squalane, from 1.5 to 8% of cyclodextrin, and from 1.5 to 8% of a pharmaceutically and/or cosmetically acceptable aliphatic mono-, di- and &agr;-hydroxy carboxylic acid having from 2 to 10 carbon atoms, and wherein the balance is selected from other compatible pharmaceutically and/or cosmetically acceptable anti-acne active substances and pharmaceutically and/or cosmetically acceptable paste, ointment or cream bases and additives. The composition may be used as a cosmetic or a drug, that creates an environment wherein the growth of pathogenic micro-organisms is repressed to the advantage of the growth of more innocuous micro-organisms. The invention further includes a method for the preparation of the compositionas well as a method of treatment of acne. The term “pharmaceutically and/or cosmetically acceptable” is meant to state that the amounts of the agent in question should be pharmaceutically and/or cosmetically acceptable.
According to established scientific apprehension acne is caused by an increased sebum production, clogging of the pores, and an inflammation caused by the bacterium Propionibactrium acnes. The increased sebum production is due to an increased testosterone production during the puberty. The testosterone stimulates an increase of the size of the sebum glands and an increased sebum production.
Acne rosacea is a chronic disease affecting the skin of the nose, forehead, and cheeks marked by flushing, followed by red coloration due to dilatation of the capillaries, with the appearance of papules and acne-like pustules.
Specifically the new composition, which are defined in the appended claims, have a prophylactic and curative effect on disorders of the skin such as acne and can be used as a drug or a cosmetic preparation for prophylactic or curing treatment of acne.
The complex squalane/cyclodextrin has a healing and anti-inflammatory effect which, in combination with the “antibacterial” effect obtained by the addition of an acid lowering the pH of the composition to a value that suppress the growth of pathological micro-organisms and supports the growth of more innocuous micro-organisms gives a drug for local application to the skin having unexpected excellent properties on the skin condition mentioned above. Preferred acids are the &agr;-hydroxy acids, especially lactic acid and azelaic acid.
Also treatment of rosacea with the composition according to the invention has shown excellent results with diminished reddening, papules, and pustules already after application of the composition for only a few days.
Pharmaceutically and/or cosmetically acceptable aliphatic mono-, di- and &agr;-hydroxy carboxylic acids according to the invention are selected from propionic, butyric, valeric, hexanoic, heptanoic, octanoic, nonanoic and decanoic acid and any isomers thereof; oxalic, malonic, succinic, glutaric, fumaric acid; adipic, pimelic, suberic, azelaic, sebacic acid; glycolic, lactic, malic, tartaric, citric and gluconic acid. Especially preferred are azelaic acid, lactic acid, and the other saturated and unsaturated aliphatic &agr;-hydroxy acids (AHA-acids).
The acids might suitably be included in the composition according to the invention in an amount of 1.5 to 8%, preferably 2 to 7% and most preferably 2.5 to 5%.
The composition according to the invention may also contain up to 0.15% of sorbic acid as a preservative.
Squalane is a softening substance moisturising dry skin in a natural way. It adds fat to the skin without causing a fatty feeling on the skin. Squalane might be included in the composition according to the invention in an amount of 2 to 8%, preferably 3 to 7% and most preferably 4 to 6%.
Cyclodextrin consists of 5, 6 or 7 &agr;-1,4 connected glucose units (&agr;- &bgr;- &ggr;-cyclodextrin) and is further described above. Cyclodextrin might be included in the composition in an amount of
Kärnerud Lars
Ölmeskog Stellan
Browdy and Neimark
Dees Jos,e G.
Haghighatian Mina
Interhealth AB
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