Cosmetic or medical preparation for topical use

Details Cosmetic or medical preparation for topical use Cosmetic or medical preparation for topical use

2001-11-14

2003-04-15

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Cosmetic, antiperspirant, dentifrice

C424S064000

Reexamination Certificate

active

06548075

ABSTRACT:

DESCRIPTION
The present invention relates to a cosmetic or medicinal preparation for topical application, in particular a skincare composition, comprising spherical microparticles which consist entirely or partially of at least one linear water-insoluble polyglucan, and the use of spherical microparticles which consist entirely or partially of at least one linear water-insoluble polyglucan in preparations of this type. In particular, the present invention relates to a cosmetic or medicinal preparation for topical application which on application imparts a particularly pleasant soft feel.
The use of polysaccharides based on starch, such as polyglucans, for cosmetic purposes has been known since time immemorial.
Recently, polysaccharide products for cosmetic and therapeutic purposes have been increasingly developed which have specific property profiles. Thus a high caring action for irritated, dry skin is described by H. Eggensperger, M. Wilker in SÖFW-Journal, 123, issue August 1997, pages 542 to 546, “Multiaktivwirksame Polysaccharide, Teil I—Pilzestrakte [Multiactive polysaccharides, part I—Fungal extracts]” for beta-polyglucans from fungi such as yeasts and their carboxymethylated derivatives. Particularly advantageous effects on the skin were demonstrated for beta-1,3-polyglucans having beta-1,6 linkages for which additionally immunostimulating action and tumor activity was observed (loc. cit., F. Züll et all., loc. cit., pages 535 to 541).
Cyclodextrins, cyclic alpha-, beta- or gamma-1,4,-oligosaccharides having 6 to 8 glucan units, are also increasingly used for functional skincare, since they form inclusion compounds with a large number of active compounds and caring substances and can thereby bring about a delayed release of these substances at the application site (U. Citernesi, M. Scaiacchitano in Cosmetics and Toiletries magazine, vol. 110, March 1995, pages 53 to
61 “Cyclodextrins in functional Dermocosmetics”).
Although a large number of products are known for all sorts of cosmetic and medicinal intended uses, there is a constant need for novel improved products. Products are in particular desirable which, on application to the skin, produce a pleasant feel and impart a smooth, soft impression.
Products of this type are advantageous for application in the case of sensitive skin and are especially also suitable for the production of medicinal preparations for topical application.
It has been shown that preparations for topical application (subsequently also called topical preparation) impart a particularly pleasant, soft feel on application if spherical microparticles are added to them which consist entirely or partially of linear water-insoluble polyglucans.
According to the invention, a preparation for topical application is thus made available which contains spherical microparticles which consist entirely or partially of at least one linear water-insoluble polyglucan.
Preparations for topical application are understood within the meaning of the invention very generally as meaning cosmetic compositions, i.e. bodycare compositions and decorative cosmetics. According to the invention, the term also includes human and veterinary medicinal preparations which are applied externally.
Preparations according to the invention can be creams, compact creams, lotions, masks, powders in any desired form, e.g. liquid, loose, compact, particulate etc., ointments, ointment bases, soaps etc. for decorative, caring or medicinal application.
Examples of the decorative cosmetics are creams, powders or foundations for make-up, e.g. rouge, eyeshadow, lipsticks.
Essential for the achievement of this object is the use according to the invention of the spherical microparticles, which consist entirely or partially of at least one water-insoluble linear polyglucan.
Microparticles of this type are distinguished by a high uniformity in size and shape. Moreover, they can easily form stable suspensions themselves without addition of dispersant aids, which is particularly advantageous for the production of the preparations according to the invention if they are based on emulsions.
The microparticles employed according to the invention are furthermore distinguished by high biocompatibility.
The naturally identical character of the water-insoluble linear polyglucans used for the preparation and of their degradation products is in particular of high importance for the biocompatibility of the microparticles employed according to the invention.
Spherical microparticles are understood as meaning microparticles which have approximately spherical shape. In the case of description of a sphere by axes of equal length starting from a common origin and directed into space, which define the radius of the sphere in all spatial directions, a difference in the lengths of the axes of 1% to 40% from the ideal state of the sphere is possible for the spherical particles. Preferably, the difference is 25% or less, particularly preferably 15% or less.
The microparticles can have a mean diameter Dn (numerical average value) of 1 nm to 100 &mgr;m, preferably of 50 nm to 10 &mgr;m, and particularly preferably of 100 nm to 3 &mgr;m.
The surface of the spherical particles can be compared macroscopically with a raspberry, the depth of irregularities on the particle surface, such as dents or clefts, being at most 20%, preferably 10%, of the mean diameter of the spherical microparticles.
The specific surface area of the microparticles is in general from 1 m
2
/g to 100 m
2
/g, preferably 1.5 m
2
/g to 20 m
2
/g and particularly preferably 3 m
2
/g to 10 m
2
/g.
The particles according to the invention further preferably exhibit a dispersity D=weight-average value of the diameter (d
w
)
umerical average value of the diameter (d
n
) of 1.0 to 10.0, in particular of 1.5 to 5.0 and particularly preferably of 2.0 to 3.0.
The mean values used here are defined as follows:
d
n
=sum of
n
i
×d
i
/sum of
ni=
numerical average value
 
d
w
=sum of
n
i
×d
i
2
/sum of
n
i
×d
i
=weight-average value
where
n
i
=number of particles of diameter d
i
,
d
i
=a determined diameter,
i=constant parameter.
Microparticles can also be employed for the present invention whose surface has been modified, e.g. by derivatization of functional groups, such as hydroxyl groups of the polyglucans.
Linear water-insoluble polyglucans within the meaning of the present invention are polysaccharides which are constructed from glucans as monomeric structural units, such that the individual units are always linked to one another in the same manner. Each base unit or structural unit defined in this way has exactly two linkages, in each case one to another monomer. Excluded from this are only the two base units which form the beginning or the end of the polysaccharide.
These have only one linkage to a further monomer and form the end groups of the linear polyglucan.
If the base unit has three or more linkages, this is referred to as branching. The ‘degree of branching’ results here from the number of hydroxyl groups per 100 base units which are not involved in the synthesis of the linear polymer backbone and which form branchings.
According to the invention, the linear water-insoluble polyglucans have a degree of branching of at most 8%, i.e. they have at most 8 branchings to 100 base units. The degree of branching is preferably less than 4% and in particular at most 2.5%.
Polyglucans are particularly preferred whose degree of branching in the 6-position is less than 4%, preferably at most 2% and in particular at most 0.5%, and in the other positions, e.g. in the 2- or 3-position, is preferably in each case at most 2% and in particular 1%.
Polyglucans are in particular suitable for the invention which have no branching, or whose degree of branching is so minimal that it is no longer detectable using conventional methods.
Examples of preferred water-insoluble linear polyglucans are linear poly-D-glucans, where the nature of the linking is insignificant as long as linearity wi

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