Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2000-09-21
2002-01-01
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S574000, C514S649000
Reexamination Certificate
active
06335368
ABSTRACT:
The present invention relates to the use of at least an effective amount of Alverine or a salt thereof in a composition or for the preparation of a composition, the Alverine or a salt thereof or the composition being intended to decontract and/or relax skin tissue and/or subcutaneous tissue, in particular in order to reduce the wrinkles and fine lines of the skin.
Women, and even men, nowadays tend to wish to look young for as long as possible and consequently seek to fade out the marks of ageing of the skin, which are reflected in particular by wrinkles and fine lines. In this respect, advertisement and the fashion world mention products intended to maintain, for as long as possible, a radiant skin free of wrinkles, which are signs of a youthful skin, and all the more so since physical appearance has an influence on the psyche and/or the morale. It is important to feel physically and psychologically young.
Hitherto, wrinkles and fine lines were reduced using cosmetic products containing active agents that act on the skin, for example by moisturizing it or by improving its cell renewal or alternatively by promoting the synthesis of collagen, of which skin tissue is composed. However, it is not known at the present time how to treat wrinkles by acting on the muscular components present in the skin. The present invention lies in this approach.
It is known that the skin muscles of the face are under the control of motor nerve afferences of the facial nerve and that, moreover, the interlobular septa of the hypoderm contain fibers which constitute a striated muscle tissue (panniculus carnosus). Moreover, it is also known that a sub-population of dermal fibroblasts, known as myofibroblasts, has characteristics in common with muscle tissue.
The Applicant has in particular observed, in certain pathological and therapeutic situations, the role played on the facial wrinkles by the nerves controlling this assembly of muscle tissue. Thus, in attacks of the facial nerve, in which the transmission of the nerve influx is interrupted and/or diminished, the innervation region reveals paralysis of facial muscles. This facial paralysis is reflected, among other clinical signs, by an attenuation or even a disappearance of wrinkles.
Conversely, in states of muscular hypercontraction of the face, the Applicant has observed an increase in facial wrinkles. Furthermore, it has also observed an increase in facial wrinkles in the muscular hypertonic states of Parkinson's disease and side effects induced by neuroleptic agents.
Moreover, it has been shown that botulinum toxin, which was originally used to reduce spasms, can act on muscle spasticity conditions (see A. Blitzer et al., Arch. Otolaryngol. Head Neck Surg., 1993, 119, pages 1018 to 1022) and on the wrinkles of the glabella, which are the wrinkles between the eyebrows (see J. D. Carruters et al., J. Dermatol. Surg. Oncol., 1992, 18, pages 17 to 21). This botulinum toxin is moreover conventionally used in plastic surgery in the treatment of wrinkles. Consequently, it is possible to act with a pharmacological action on the neuromuscular component of wrinkles.
After numerous tests, the Applicant has been able to determine that contractile muscle fibers, and in particular striated muscle fibers, which are under the direct control of the neuromuscular influx, play an essential role in the formation of wrinkles and that modulating the neuromuscular influx attenuates not only wrinkles but also fine lines and also has a “smoothing” effect on the skin microrelief.
Physiologically, the activity of striated muscles (with the exception of the cardiomyocyte) is triggered by the nervous system, and the activity of smooth muscles is spontaneous and modulated by various stimuli of hormonal or nervous type.
The cells which are the cause of spontaneous contractions are the “pacemaker” cells: the propagation of the electrical excitation wave takes place little by little in the zone of least electrical resistance of the cell membranes.
Outside of spontaneous activity, the excitation of smooth muscle fibers can be triggered by various stimuli: mechanical stretching, the presence of neurotransmitters or intestinal hormones acting specifically on certain cell receptors, certain agents having an agonist or antagonist effect on these same receptors.
Irrespective of the type of fibre (smooth or striated), the common final messenger which is the cause of the contraction is the calcium ion (Ca
2+
).
However, the intervention of this cation in the contractile mechanism is entirely different depending on the type of fiber (smooth or striated).
The studies by the Ebashi group have shown that, in smooth muscles (unlike striated muscles), the sliding of the actin and myosin molecules does not take place after the inhibition exerted by troponin has been lifted with Ca
2+
. The cation exerts a direct activating effect on the actin-myosin linkage in combination with a protein known as leiotonin C. The joint action of Ca
2+
and leiotonin C is responsible for the phosphorylation of the light chains of myosin which causes the contraction.
Furthermore, the relaxation of smooth muscles is very active, unlike that of striated muscle. It is dependent on hormonal and nervous mediators.
The demonstration of these physiological activities is at the origin of the control of the digestive motility by pharmacological agents.
Thus, Alverine or di(phenylpropyl)ethylamine, also known as Spasmaverine or Diproline, is known as a digestive smooth muscle relaxant.
The Applicant has now discovered that the relaxing effect of Alverine is not specific for smooth muscle.
Alverine can induce a decontracting and/or relaxing effect on striated muscle and thus, consequently, can constitute an active agent that is advantageous for correcting wrinkles and/or fine lines and for promoting smooth skin.
To the Applicant's knowledge, such a property is not described or suggested anywhere in the prior art.
The present invention thus relates to the use in a composition or for the preparation of a composition, of at least an effective amount of Alverine or of a salt thereof, the Alverine or the salt thereof or the composition being intended to relax and/or decontract the skin tissue and/or subcutaneous tissue.
According to the invention, the expression “Alverine salts” means the organic or inorganic salts of Alverine.
As organic salts which can be used according to the invention, mention may be made of Alverine gluconate, Alverine acetate, Alverine citrate, Alverine oleate and Alverine oxalate.
Inorganic Alverine salts which may be mentioned are mineral salts such as Alverine chloride, Alverine borate, Alverine nitrate, Alverine phosphate, Alverine sulphate and Alverine carbonate.
It is thus understood that in the text, except where otherwise indicated, the use of the term “Alverine” should be understood as meaning Alverine both in ionic form and in the form of salts.
Preferably, according to the invention, the organic salt is Alverine citrate and the inorganic salt is Alverine chloride.
This use is found to be particularly effective for reducing wrinkles and/or fine lines and/or for making the skin smooth.
Thus, a subject of the invention is also the use of at least an effective amount of Alverine or of a salt thereof in a composition or for the preparation of a composition, the Alverine or a salt thereof or the composition being intended for reducing wrinkles and/or fine lines.
More particularly, the relaxation and/or decontraction of the skin tissue and/or subcutaneous tissue is a muscular decontraction or relaxation.
The use of Alverine according to the invention can be preventive and/or curative.
A subject of the invention is also a composition intended for relaxing and/or decontracting skin tissue and/or subcutaneous tissue, comprising at least an effective amount of Alverine or a salt thereof.
A subject of the invention is also a composition intended for reducing wrinkles and fine lines and/or for smoothing the skin, comprising at least an effective amount of Alverine or a salt thereo
Breton Lionel
Liviero Christel
Pineau Nathalie
Henley III Raymond
Societe L'Oreal S.A.
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