Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-07-14
2000-02-08
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3134
Patent
active
06022889&
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF INVENTION
R. T. Major (Science 157, 1967, 1270-1273) was the first person to report on the isolation of a lactone having the formula C.sub.15 H.sub.18 O.sub.8 from the leaves of the Ginkgo biloba tree. K. Weinges and W. Bahr termed the substance "bilobalide" and investigated and described the physicochemical properties of bilobalide and its derivatives (Liebigs Ann. Chem., 724, 1969, 214-216). According to a joint publication by the research teams of K. Nakanishi et al., R. T. Major et al., and K. Weinges et al. (J. Amer. Chem. Soc. 93, 1971, 3544-3546), bilobalide has the formula I ##STR1## Since 1965 extracts from leaves of the Ginkgo biloba tree have been used in the therapy of central and peripheral circulatory disturbances. Such extracts contain flavone glyocsides as their main components and have also been standardized to include those ingredients. A typical representative of this group is 5,7,3',4'-tetrahydroxyflavono-3-O-alpha-rhamnopyranosyl-4-O-beta-D-(6'"-tr ans-cumaroyl)glycopyranoside having the formula II ##STR2## Generally, those extracts may also contain lower amounts of bilobalide and ginkgolides A, B, C, and J.
U.S. Pat. No. 4,571,407 discloses that bilobalide is useful in the treatment of various degenerative, neuronal diseases. Such diseases particularly include neuropathies, encephalopathies, and myelopathies associated with one or more of the following symptoms: paresthesias, pareses, abnormal reflexes, muscular atrophies, muscular spasms, tremors, headaches, speech disorders, hearing defects, dizziness, disturbances of consciousness, impaired coordination, etc.
Surprisingly, it has now been found that bilobalide exhibits anxiolytic activities in addition to the known pharmacological effects on degenerative, neurological diseases. This is the first time that psychopharmacological effects of bilobalide have become known.
The fear that actually represents a useful mechanism to protect the human being in that it frequently warns him against exposing himself to certain dangers becomes pathological when it is unfounded or extremely strong. Anxiety patients show, among others, symptoms such as agitation, unrest, apathy and frequently have difficulty in falling asleep and in sleeping through.
Pathological fear is a frequently occurring symptom that is often not paid enough attention to, although fear is frequently the cause of so-called psychosomatic diseases. Pathological fear has so far been treated by psychotherapy and/or drug therapy using anxiolytic drugs.
The pharmacological anxiolytics are predominantly derived from the group of benzodiazepines (e.g., diazepam). More recent anxiolytics have been characterized pharmacologically as 5HT.sub.1a agonists (e.g., buspiron). Surprisingly, bilobalide shows activity essentially corresponding to that of diazepam or buspiron in various animal models.
SUMMARY OF INVENTION
Thus the invention relates to the use of bilobalide or Ginkgo biloba extracts supplemented with bilobalide as an anxiolytic. In preferred embodiments it is used for the treatment or prophylaxis of anxiety, tension and depressive conditions.
BRIEF DESCRIPTION OF DRAWINGS
FIG. 1 shows Table A which summarizes the administered substances, dosages, and observations of rats subjected to elevated plus maze tests.
FIG. 2 shows Table B which summarizes the administered substances, dosages and observations of mice subjected to light/dark box tests.
FIGS. 3a-3d are graphs showing the influence of bilobalide, diazepam and ethanol on the time that the rats spent in the open arm of the elevated plus maze.
FIGS. 4a-4d are graphs showing the influence of bilobalide and diazepam on the frequency with which the rats switched side arms and on the time they stayed on the open side arms in the elevated plus maze tests.
FIGS. 5a-5c are graphs showing the influence of bilobalide and diazepam and buspiron on the time that mice spent in the light compartment of the light/dark box.
FIG. 6 is a graph showing the influence of bilobalide, diazepam and mephenesin on a stress-induced incr
REFERENCES:
patent: 4571407 (1986-02-01), Chatterjee et al.
Investigation Medica Internacional, vol. 17, No. 3 (1990), pp. 130-141.
La Presse Medicale, vol. 15, No. 31, Sep. 25, (1986), pp. 1595 to 1604.
Fortschritte der Medizin, vol. 108, No. 29, Oct. 10, (1990), pp. 557-560.
Chem. Abstracts, Oct. 22, (1990), vol. 113, No. 17, p. 664, CA 113:151138d.
Chatterjee Shyam S.
Noldner Michael
Jordan Kimberly
William Schwabe GmbH & Co.
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