Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Reexamination Certificate
1997-03-27
2001-05-01
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
C424S043000, C424S059000, C424S063000, C424S195110, C424S401000, C514S725000
Reexamination Certificate
active
06224850
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Technical Field of the Invention
The present invention relates to novel cosmetic/pharmaceutical compositions containing an effective amount of at least one extract of at least one Iridaceae, for loosening and/or relaxing the cutaneous and/or subcutaneous tissue, especially for treating (reducing or eliminating) normal and small (fine) skin wrinkles.
2. Description of the Prior Art
Women, or even men, today seek to maintain a youthful appearance for as long as possible and, consequently, seek to attenuate the signs of skin aging, which manifest themselves especially by normal and small wrinkles. In this regard, advertisements and fashion promote products intended to maintain a radiant skin for as long as possible and without wrinkles, which is the sign of a youthful skin, all the more so since physical appearance is important for peace of mind and/or for morale. Thus, it is important to feel physically and spiritually young.
To date, normal and small wrinkles were treated with cosmetic products containing active agents acting on the skin, for example by moisturizing it or by enhancing its cellular renewal or by promoting the synthesis of collagen which constitutes the cutaneous tissue. However, also to date, it was not known to this art how to treat wrinkles by acting on the muscular elements present in the skin.
It is known that the facial platysma muscles are under the control of the motor nerve afferences of the facial nerve and that, moreover, the interlobular septa of the hypodermis contain therein fibers which constitute a striated muscular tissue (
panniculus carnosus
). Too, it is also known that a subpopulation of fibroblasts of the dermis, designated myofibroblasts, exhibits characteristics which are common with the muscular tissue.
Prologue:
In the laboratories of the assignee hereof, in certain pathological and therapeutic conditions, the influence exerted on facial wrinkles by the nerves controlling all of this muscular tissue has been observed. Thus, in facial nerve conditions, in which the transmission of the nerve impulse is interrupted and/or reduced, there is observed in the area of innervation a paralysis of the facial muscles. This facial paralysis results, besides other clinical signs, in an attenuation, or even disappearance of the wrinkles.
In contrast, in the states of facial muscular hypercontraction, accentuation of facial wrinkles has also been observed. Furthermore, an accentuation of the facial wrinkles in the muscular hypertonia states in Parkinson's disease and side effects induced by neuroleptics too has been observed.
Moreover, it has been demonstrated that the botulinus toxin, originally used for treating spasms, is active on muscular spasticity states (see A. Blitzer et al.,
Arch. Otolaryngol. Head Neck Surg
., 119, pages 1018 to 1022 (1993)) and on the wrinkles on the glabella which are intersuperciliary wrinkles (see J. D. Carruters et al.,
J. Dermatol. Surg. Oncol
., 18, pages 17 to 21 (1992)). Consequently, it is possible to influence, via a pharmacological action, the nervous component of the wrinkles.
In the peripheral nervous system, the junction between a nerve and a muscle constitutes the neuromuscular plate, upstream of which there is the afferent nerve route denominated “motoneuron.”Moreover, the cellular membranes of each nerve fiber comprise numerous ion channels, and especially chlorine channels, capable of permitting the corresponding element in ionic form, and in the case of the chlorine channels in chloride form, to pass therethrough. These channels are associated with neuronal receptors. The neuronal receptors associated at the periphery with the chlorine channels are especially receptors for glycine (glycine-strychnine sensitive receptors) and receptors for type A GABA (GABA-A receptors) (GABA=&ggr;-aminobutyric acid).
It too is known that it is possible to reduce the excitability of the motoneuron by various pharmacological agents acting on the glycine-strychnine sensitive receptors or on the GABA-A receptors of the peripheral nervous system (see W. Sieghart,
Trends in Pharmacological Science
, December 1992, Vol. 131, pages 446 to 450). Thus, it is possible to modulate the excitability of the motoneuron, for example by glycine or gamma-aminobutyric acid (GABA).
The activation of these receptors opens the chlorine channels and permits entry of chloride ions, which results in an increase in the chloride ions in the cells of the nerve fiber and therefore to a hyperpolarization of the motoneurons which become, as a result, less excitable. This reduction in excitability of the motoneuron causes a lesser stimulation of the muscle fiber, thereby effecting its loosening.
SUMMARY OF THE INVENTION
After numerous clinical trials, it has now been determined that the contractile muscle fibers, in particular the striated muscle fibers, which are under the direct control of the neuromotor impulse, play an essential role in the pathogenicity of wrinkles and that the modulation of the neuromotor impulse attenuated not only the normal wrinkles, but also the small (fine) wrinkles and also exerted a “smoothing” effect on the cutaneous microrelief.
It has also now been determined that the cutaneous and subcutaneous tissues contained receptors associated with the chlorine channels, which, to date, had not been envisaged. It has therefore been found that it was possible to act on these channels in order to loosen or relax these tissues, and thus to reduce the normal and small wrinkles.
Also to date, no link had been established between the chlorine channels of the nerve fibers and wrinkles, and it was not considered to treat wrinkles by acting on the chlorine channels via activation of the receptors which are present in or close to these channels. Substances which may activate the receptors of the chlorine channels and therefore initiate the entry of chloride into the cells, are designated agonist substances.
Several receptors associated with the chlorine channel exist. These are especially the glycine-strychnine sensitive receptors and the GABA-A receptors, the latter themselves comprising several subunits including the GABA site, the benzodiazepine site, a type of steroid site and the site for the barbiturates. All of the substances or substrates which serve as agonists for these receptors or sites may be used to loosen or relax the cutaneous and/or subcutaneous tissues in accordance with the invention.
For a substance or species to be recognized as an agonist for the receptors of the chlorine channels, it must satisfy the following two requirements:
(a) be able to bind selectively to at least one of the different receptors associated with the chlorine channel;
(b) exert a relaxation effect on a contracted muscular tissue.
The first characteristic, which entails the possibility of binding to a receptor associated with a chlorine channel, does not permit distinguishing an agonist activity from an antagonist activity, but it makes it possible to define a potential affinity for the receptor.
The second characteristic permits selecting the agonists. The agonist activity of the substance studied may be demonstrated by the relaxation effect which it elicits on a muscular tissue which has been previously contracted by a chlorine channel antagonist substance. As chlorine channel antagonist substance, these may be selected from among known agents such as, and especially the following: bicuculline, strychnine, tert-butyl-bicyclophosphoro-thionate and picrotoxin.
Surprisingly, it has now been demonstrated that an extract of at least one Iridaceae satisfies the criteria for chlorine channel receptor agonist as defined above.
JP-A-60-201249 describes the use of Iridaceae extract for the treatment of rough skin by means of the dilatory activity of the blood vessels of the skin.
To the contrary, the present invention features antiwrinkle cosmetic/pharmaceutical compositions comprising an effective amount of an extract of at least one member of the Iridaceae family for relaxing and/or loosening the cutaneous and/
Breton Lionel
De Lacharriere Oliver
Martin Richard
Burns Doane Swecker & Mathis L.L.P.
Page Thurman K.
Seidleck Brian K.
Societe L'Oreal S.A.
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