Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2002-07-25
2003-11-18
Hartley, Michael G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S400000, C424S059000, C424S078030, C514S861000, C514S859000
Reexamination Certificate
active
06649179
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a plasminogen activator inhibitor, an external preparation for skin comprising the same, a method for improving rough skin and in particular, to improvement of an effective inorganic component.
BACKGROUND OF THE INVENTION
It has been known that various kinds of medicines, external preparations for skin and cosmetics are effective for improvement and prevention of such symptoms as skin disease, rough skin and pimples. As an effective component of these medicines and cosmetics, for example, essences extracted from plants or animals which are effective for anti-inflammation, or those having moisture retaining or water retaining effect such as amino acids, polysaccharide, lipid and natural polymer have been used because these components are effective for prevention of dermatitis or prevention of water volatilization from a horny layer of epidermis.
On the other hand, especially careful selection of effective components should be needed in case of morbid dermatitis like atopic dermatitis or serious skin pimples because there is a possibility that said effective components cause intolerance sensitivity reaction or irritation in such cases.
Further in some cases those molecules such as organic polymers used as effective components for rough skin permeate into skin by a percutaneous absorption and have a probability to give other undesired skin effects. But if it is possible to use a solid powder that does not permeate into skin by a percutaneous absorption as an effective component for improvement of rough skin, an external preparation for rough skin comprising such a powder can be used more safely relative to previously used preparations containing organic molecules as the effective components.
However, the effect on improvement or prevention of the above-mentioned components provided previously was not sufficient. Further an effective medicine which is safe and free from irritation has been required because dermatitis, especially morbid dermatitis like atopic dermatitis, is accompanied by inflammation and a failure of a barrier function.
SUMMARY OF THE INVENTION
In view of the foregoing problems described above, an object of the present invention is to provide a plasminogen activator inhibitor which is effective for improvement of rough skin and an external preparation for skin comprising the same.
As a result of diligent studies for attaining the above mentioned object, we have found that a specified zinc oxide shows an activation inhibition effect on a plasminogen activator and also shows an improvement effect on rough skin when an external preparation for skin comprising said specified zinc oxide was used. And we have simultaneously found it is possible to use a powder as an effective component for improvement of rough skin.
A plasminogen activator inhibitor of the present invention comprises zinc oxide which adsorbs a plasminogen activator and inhibits its activity.
An adsorption rate of a plasminogen activator inhibitor of the present invention is preferably more than 60 percent per total amount, and an inhibition rate of a plasminogen activator inhibitor of the present invention is preferably more than 60 percent per total amount.
An adsorption rate and an inhibition rate are measured as follows:
Measurement of Adsorption Effect on a Plasminogen Activator
After mixing 0.1 percent of a tested sample and 1 &mgr;g/ml of a single chain-urokinase in a buffer solution for a fixed time, the sample was taken away from the buffer solution, and then an adsorption rate was determined by measuring the amount of a single chain-urokinase left in the buffer solution quantitatively by ELISA method.
Measurement of Activation Inhibition Effect on a Plasminogen Activator
An inhibition rate was determined by measuring a decomposition activity for a synthetic substrate caused by a buffer solution comprising 0.1 percent of a tested sample and 100 U/ml of a urokinase type plasminogen activator.
An adsorption rate of a plasminogen activator inhibitor of the present invention is especially preferable to be more than 70 percent per total amount, and an inhibition rate of a plasminogen activator inhibitor of the present invention is especially preferable to be more than 70 percent per total amount.
It is preferable to use zinc oxide coated by 0.1 to 70 percent by weight of silica at the present invention.
An external preparation for rough skin of the present invention is characterized by comprising powder which adsorbs a plasminogen activator and inhibits its activity.
An external preparation for rough skin of the present invention is characterized by comprising zinc oxide which adsorbs a plasminogen activator and inhibits its activity.
An external preparation for diseased skin of the present invention is characterized by comprising silica-coated zinc oxide which adsorbs a plasminogen activator and inhibits its activity.
A method for restraining activity of a plasminogen activator of the present invention is characterized by adsorbing a plasminogen activator on powder and inhibiting its activity.
A method to improve rough skin of the present invention is characterized by applying powder to skin which adsorbs a plasminogen activator and inhibits its activity.
An external preparation for rough skin of the present invention is characterized by comprising zinc oxide.
DETAILED DESCRIPTION OF THE INVENTION
The present invention of a plasminogen activator inhibitor and an external preparation for skin comprising it was accomplished based on the background described below.
It has been made clear recently that an activity change of a protease, especially an activity change of a fibrinogenolysis type enzyme (a plasminogen activating enzyme) such as plasmin or plasminogen activator, is closely related to a formation of various types of diseased skin accompanied with rough skin or abnormal cornification.
For example, it was reported that a distribution of plasmin in an epidermal cell layer of rough skin experimentally formed was changed relative to a distribution of plasmin in epidermal cell layer of normal skin, and anti-plasmin agent is effective for improvement and prevention of rough skin (Kenji Kitamura: J. Soc. Cosmet. Chem. Jpn; 29(2), 1995). Further in case of atopic dermatitis high fibrinogenolysis activity in epidermis was also reported (T. Lotti: Department of Dermatology; 28(7), 1989). On the other hand, in the case of psoriasis, representative of diseased skin accompanied with inflammation and abnormal cornification, it was reported that there exists high plasminogen activator activity at a portion of parakeratosis in an epidermis of the affected part (Haustein: Arch. Klin. Exp. Dermatol; 234, 1969), and it was also reported that a plasminogen activator was extracted from a flake of psoriasis by using a high-concentration buffer solution(Fraki, Hopsu: Arch. Dermatol. Res; 256, 1976).
A plasminogen activator is a protease which selectively acts on a plasminogen, (a precursor of plasmin) and transform plasminogen to active form.
Based on the above-mentioned existing background, the present inventors attempted to develop a new medicine for rough skin, and took notice of the fact that a plasminogen activator exists in a corneal layer of epidermis of rough skin like a flake of psoriasis. Then various kinds of inorganic powder were investigated for improvement and prevention of rough skin, based on the idea that a material which adsorbs and deactivates a plasminogen activator at a surface of skin and does not have the process of percutaneous absorption would be effective for improvement and prevention of diseased skin or rough skin which accompanies an activity change for a plasminogen activating enzyme, and also would be highly safe for human body. As a result of exploring various kinds of inorganic powder, it was found that a specified zinc oxide, especially silica-coated zinc oxide where a weight percent of coated silica is 0.1 to 70 weight percent per total weight, excellently adsorbs and inhibits a plasminogen activator. It was also found that an
Kawai Eriko
Yoshida Yuzo
Haghighatian Mina
Hartley Michael G.
Shiseido Co. Ltd.
Snider Ronald R.
Snider & Associates
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