Drug – bio-affecting and body treating compositions – Chewing gum type
Reexamination Certificate
2000-06-23
2002-01-22
Lilling, Herbert J. (Department: 1651)
Drug, bio-affecting and body treating compositions
Chewing gum type
C424S049000, C424S058000, C424S752000, C424S780000
Reexamination Certificate
active
06340456
ABSTRACT:
The invention relates to the use of a flavonoid extract of ginkgo biloba, and more specifically an extract substantially devoid of terpenes, in the dentibuccal field. The invention also relates to an dentibuccal composition containing such extract.
A flavonoid extract of ginkgo biloba leaves devoid of terpenes according to the invention comprises flavonoid glycosides and little or no terpenes. When the extract contains terpenes, the terpene content is 1% maximum, and preferably 0.5% maximum. This extract contains from 28 to 35% of flavonoid glycosides, and preferably 28 to 32%. Such extracts are preferably obtained from leaves from pruned young ginkgo biloba trees.
A subject of the invention is a process for obtaining such an extract, a process which comprises several extraction stages of ginkgo biloba leaves by solvents and characterized in that one of the extraction stages is a deterpenation stage and the solvent used is a compound of formula RC(O)OR′ in which R and R′ represent, independently, a lower alkyl, alone or mixed with a saturated aliphatic hydrocarbon containing at least 5 carbon atoms. The extraction stage can be carried out at any stage in the process. Preferably, the solvent used during the deterpenation stage contains from 0 to 20% of saturated aliphatic hydrocarbon.
Extraction stages other than the deterpenation stage are known in the literature in particular in Patents EP431535, EP 431536, EP 360556 and EP324197. These Patents are incorporated into the present Application by way of reference.
In the definitions indicated above, the expression lower alkyl preferably represents a linear or branched alkyl radical having from 1 to 6 carbon atoms, and in particular an alkyl radical having from 1 to 4 carbon atoms such as the methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl and tert-butyl radicals. The solvents of formula RC(O)OR′ in which the radicals R and R′ represent methyl, ethyl or propyl and in particular ethyl acetate are preferably used. The saturated aliphatic hydrocarbon can be chosen from hexane, heptane and octane. Preferably, heptane is used.
A flavonoid extract of ginkgo biloba leaves as defined above has an anti-elastasic and anti-inflammatory activity on human gums. An illustration of these properties is to be found below in the experimental part.
These properties render the ginkgo extract as defined above suitable for pharmaceutical use. A subject of the present Application is therefore, as a medicament, and in particular as a medicament intended for the dentibuccal sphere, a flavonoid extract of ginkgo biloba leaves as defined above.
A subject of the invention is also a pharmaceutical composition intended in particular for the treatment of the dentibuccal sphere and containing as active ingredient a flavonoid extract of ginkgo biloba leaves as defined above, optionally combined with a pharmaceutically acceptable support.
A more particular subject of the invention is an anti-elastasic pharmaceutical composition containing, as an anti-elastasic agent, at least one effective quantity of a ginkgo extract as defined above. A more particular subject of the invention is also an anti-inflammatory pharmaceutical composition containing, as an anti-inflammatory agent, at least one effective quantity of a ginkgo extract as defined above.
A pharmaceutical composition according to the invention preferably contains from 0.05 to 0.6% of ginkgo extract, and preferentially from 0.1 to 0.5%. Such a composition can also contain at least one other agent having similar or complementary activities. Preferably, a pharmaceutical composition according to the invention contains ginkgo extract as defined above combined with ceramides. Preferentially, such a composition contains from 0.1 to 0.5% of ginkgo extract and from 0.05 to 0.3% of ceramides.
A pharmaceutical composition according to the invention can be presented in any appropriate form according to the chosen administration method. It can be presented in liquid form such as, for example, a solution, a suspension or an emulsion. It can also be presented in the form of a gel, spray, toothpaste or chewing gum. It is preferably presented in the form of a gel or chewing gum. It can contain, in addition to the ginkgo extract, alone or in combination, and an appropriate support, the ingredients or adjuvants commonly used for producing such compositions.
A subject of the invention is also the use of a flavonoid extract of ginkgo as defined above for the preparation of a pharmaceutical composition intended for treatment in the dentibuccal sphere.
A more particular subject of the invention is the use of a flavonoid extract of ginkgo as defined above for the preparation of a pharmaceutical composition intended to inhibit elastase. A more particular subject of the invention is also the use of a flavonoid extract of ginkgo as defined above for the preparation of pharmaceutical composition intended to inhibit inflammation in the dentibuccal sphere. Such a flavonoid extract can be used alone or in combination with another agent having similar or complementary properties according to the sought result, optionally in the presence of an appropriate support. An extract as defined above is preferably used in combination with ceramides.
Ceramides are sphingolipids present in all cell structures. They are also notably present in the plant world and in particular in wheat, rice, soya, millet and spinach. They can also be synthsized. Owing to their structure, they can advantageously be used as a vector, considerably increasing the bioavailability of the active agent they are conveying. The term ceramide used in the present Application has the standard meaning known to a person skilled in the art. The term ceramide thus includes all ceramides, of synthetic or natural origin (vegetable, animal or human) optionally substituted, for example, by a sugar such as mono- or polyglucosylceramides.
Owing to a high flavonoid glycoside content, the state of the art suggests that an extract as defined above has an anti-oxidant and anti-radicular activity. Moreover, given on the one hand its anti-inflammatory, anti-elastasic properties but also vasoregulatory and collagen activating properties and, on the other hand, an almost total absence of terpenes in its composition, such an extract can advantageously be used in cosmetics or in dermatology.
A subject of the invention is also the use of a flavonoid extract of ginkgo biloba leaves as defined above for the preparation of a vasoregulatory and/or collagen activating medicament. The invention also relates to the use of a cosmetic composition containing a flavonoid extract as defined above as a vasoregulator and/or a collagen activator. A subject of the invention is also a cosmetic treatment method characterized in that a flavonoid extract is used as defined above as a vasoregulator and/or a collagen activator.
A subject of the invention is also a cosmetic composition intended in particular for the dentibuccal sphere and containing a flavonoid extract of ginkgo biloba leaves as defined above. This extract can be used on its own or in combination with at least one other agent having a similar or complementary activity, and optionally with an appropriate support. Preferably, the ginkgo extract is used in combination with ceramides. A cosmetic composition according to the invention can contain from 0.05 to 0.6% of ginkgo extract as defined above, and from 0.05 to 0.3% of ceramides. Such a composition can be presented in any appropriate form for this type of use such as creams, emulsions, milks, gels, oils, makeup products, lipsticks and lotions. In addition to ginkgo extract, alone or in combination, and an appropriate support, it can contain the ingredients or adjuvants commonly used to produce such compositions.
A subject of the invention is also a flavonoid extract of ginkgo biloba as defined above for the cosmetic treatment of affections in the dentibuccal sphere and in particular gingivitis.
The following examples are presented in order to illustrate the invention and
Bierman, Muserlian and Lucas
Lilling Herbert J.
Societe de Conseils de Recherches et d'Applications Scienti
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