Use of Ginkgo biloba flavonoidic extract substantially devoid of

Drug – bio-affecting and body treating compositions – Dentifrices – Plant extract of undetermined constitution

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424 49, 4241951, 514783, A01N 6500, A61K 3578, A61K 716, A61K 726

Patent

active

061594504

DESCRIPTION:

BRIEF SUMMARY
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-clastasic 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 ca

REFERENCES:
Computer Abstract CAPLUS 1967:1542 Bar et al "Use of bioriboflavonoids in the treatment of gingivitis and marginal periodontal disease" Minerva Stomatotl (1966) 15(8) pp. 550-554, 1967.
Computer Abstract BIOSIS 1992:527566 Herbage et al "Evaluation of the Effect of Ginkgo-biloba Extract and Its Constituents on Fibrillogenesis and Stability of Collagen Fibrils in-vitro" Phlebologie (1992) 44 (4) 873-880, 1992.
Computer Abstract CABI 1999:37961 Akiba et al "Inhibitory effect of the leaf extract of Ginkgo biloba L on oxidative stress-induced platelet aggregation" Biochem & Mol. Biol. Intern (1998) V 46, No. 6 1243-1248, 1998.
Computer Abstract CAPLUS 1996:417847 Kumagai et al "Flavones or anthocyanins as matrix metalloprotase inhibitors and their extraction from medicinal plants for therapeutic use" Jpn. Kokai 08104628, Apr. 1996.

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