Hair loss abstract
The present invention relates to novel formulations useful in the
preventive and curative treatment of hair loss and of seborrhea,
containing coumarins such as khellin, visnadin, esculoside or alkaloids
such as raubasine, vincamine and derivatives thereof, combined with
unsaturated and saturated fatty acids.
Hair loss claims
What is claimed is:
1. A composition for the treatment of hair loss and seborrhea,
comprising a therapeutically effective amount of the combination
of (1) at least one fatty acid or fatty acid ester, and (2) at least
one coumarin, alkaloid, alkaloid fatty acid, alkaloid ester, or
combination thereof.
2. The composition according to claim 1, wherein:
the fatty acid or fatty acid ester is ximenynic acid, a saturated
C.sub.12 -C.sub.14 acid, a ximenynic acid ester, or a saturated
C.sub.12 -C.sub.14 acid ester,
the coumarin is khellin, visnadin, esculoside, or esculetin, and
the alkaloid is raubasine, vincamine, or a fatty acid or ester
thereof.
3. The composition according to claim 1, comprising a mixture of
esculoside, ximenynic acid, and lauric acid.
4. The composition according to claim 1, comprising a mixture of
visnadin, ximenynic acid ethyl ester, and lauric acid.
5. The composition of claim 1, which further comprises a liquid
carrier so that the composition is in the form of a lotion or gel.
6. A composition for the treatment of hair loss and seborrhea,
comprising about 0.2% to about 3% of visnadin or khellin, about
0.2% to about 10% of ximenynic acid or a ximenynic acid ester, and
about 0.1% to about 1% of lauric acid.
7. The composition according to claim 6, comprising about 0.5 to
1.5% of ximenynic acid or ester thereof and about 0.2 to 0.5% of
lauric acid.
8. A composition for the treatment of hair loss and seborrhea,
comprising about 0.3% to about 4% of esculoside or esculetin, about
0.2% to about 10% of ximenynic acid or an ester thereof, and about
0.1% to about 1% of lauric acid.
9. The composition according to claim 8, wherein the composition
comprises about 1 to 2% of esculoside or esculetin, about 0.5 to
1.5% of ximenynic acid or ester thereof, and about 0.2 to 0.5% of
lauric acid.
10. A method for the treatment of hair loss or seborrhea, comprising
applying to a subject a therapeutically effective amount of a composition
comprising the combination of (1) at least one fatty acid or ester
thereof, and (2) at least one coumarin, alkaloid, alkaloid fatty
acid, alkaloid ester, or combination thereof.
11. The method according to claim 10, wherein:
the fatty acid or ester is ximenynic acid, a saturated C.sub.12
-C.sub.14 acid, a ximenynic acid ester, a saturated C.sub.12 -C.sub.14
acid ester, or a mixture thereof,
the coumarin is khellin, visnadin, esculoside, esculetin, or a
mixture thereof, and
the alkaloid is raubasine, vincamine, a fatty acid or ester thereof,
or a mixture thereof.
12. The method according to claim 10, wherein the composition comprises
the combination of esculoside, ximenynic acid, and lauric acid.
13. The method according to claim 10, wherein the composition comprises
the combination of visnadin, ximenynic, acid ethyl ester, and lauric
acid.
14. The method according to claim 10, which further comprises adding
a liquid carrier to the composition to form a lotion or gel to facilitate
application thereof.
15. The method according to claim 10, wherein the composition comprises
about 0.2% to about 3% of visnadin or khellin, about 0.2% to about
10% of ximenynic acid or an ester thereof, and about 0.1% to about
1% of lauric acid.
16. The method according to claim 12, wherein the composition comprises
about 0.5 to 1.5% of ximenynic acid or ester thereof and about 0.2
to 0.5% of lauric acid.
17. The method according to claim 10, wherein the composition comprises
about 0.3% to about 4% of esculoside or esculetin, about 0.2% to
about 10% of ximenynic acid or an ester thereof, and about 0.1%
to about 1% of lauric acid.
18. The method according to claim 17, wherein the composition comprises
about 1 to 2% of esculoside or esculetin, about 0.5 to 1.5% of ximenynic
acid or ester thereof, and about 0.2 to 0.5% of lauric acid.
19. The method of claim 10, further comprising treating the scalp
of the subject with the composition for a period of about 2 days
to about 6 months.
20. The method of claim 10, wherein an amount of about 0.1 to about
1 g of the composition is applied to the subject each day.
21. The composition of claim 1 further comprising lauric acid in
an amount effective to enhance the therapeutic effect of the combination
of components (1) and (2).
22. The method of claim 10, where the composition to be applied
also contains lauric acid in an amount effective to enhance the
therapeutic effect of the combination of components (1) and (2).
Hair loss description
TECHNICAL FIELD
The present invention relates to novel formulations useful in the
preventive and curative treatment of hair loss, containing combinations
of substances activating the microcirculation of "galea capitis"
and products having antiseborrhoic and antiandrogen actions. It
has surprisingly been found that formulations containing coumarins
such as khellin, visnadin, esculoside, or alkaloids such as raubasine,
vincamine and derivatives thereof, combined with unsaturated fatty
acids such as ximenynic acid, the ethyl ester or other esters thereof,
as well as acids such as lauric, myristic or isomyristic acids,
are synergistically active in stimulating hair regrowth or in preventing
its loss.
BACKGROUND OF THE INVENTION
The vasokinetic activity of some of these substances, such as visnadin
and khellin, have already been described in Patent application IT-21786A/89,
which evidenced the effect thereof on the increase in the volume
and in the blood flow rate at the level of the capillary network,
and the use of these substances in peripheral vasculopathies and
in primitive and secondary alopecias had been provided. Similarly,
ximenynic acid free or in the form of triglyceride and generally
of esters, was found to increase the blood flow with mechanisms
different from those of visnadin and khellin (Patent IT-1223290).
SUMMARY OF THE INVENTION
The present invention provides a composition for the prevention
and curative treatment of hair loss and seborrhea, which comprises
at least one fatty acid or fatty acid ester, and at least one coumarin,
alkaloid, or alkaloid derivative or a combination thereof. These
active ingredients may be present in a liquid carrier, such as an
alcohol, or in the form of a gel. The present invention also provides
a method of preventing or curing hair loss or seborrhea, which includes
forming a composition, which comprises at least one fatty acid or
fatty acid ester, and at least one coumarin, alkaloid, alkaloid
derivative, or a combination thereof, and topically applying a functional
amount of the liquid or gel composition to a patient or subject.
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to a composition and method for the
prevention and curative treatment of hair loss and seborrhea. The
claimed composition comprises at least one fatty acid or fatty acid
ester, such as ximenynic acid, a ximenynic acid ester, a saturated
C.sub.12 -C.sub.14 acid, or a saturated C.sub.12 -C.sub.14 acid
ester, and at least one coumarin, such as khellin, visnadin, esculoside,
or esculetin, or an alkaloid or alkaloid derivative, such as raubasine,
vincamine, or a derivative thereof. The composition may also contain
a mixture of at least one coumarin and at least one alkaloid or
alkaloid derivative in addition to the fatty acid. In the method
of the present invention, the claimed composition is topically applied
to a patient or a subject to prevent or cure hair loss or seborrhea.
Ximenynic acid and the esters thereof, when applied topically for
a long time, exert a double effect at the cutaneous level: a microvasculokinetic
one and antiseborrhoic one. Such two actions combined in the same
molecule are particularly useful for keeping the skin effectively
vascularized and at the same time dry thanks to a decreased sebum
secretion. C.sub.12 and C.sub.14 acids, such as lauric, myristic
and isomyristic acids, turned out to be strong inhibitors of dihydrotestosterone
receptor binding, therefore, when suitably carried through the epicutaneous
layer, they can exert a remarkable antiandrogen action, thus, contributing
to a sebaceous regulation.
The combination of substances with vasokinetic activity (coumarins
or alkaloids) with unsaturated fatty acids or the esters thereof
as antiseborrhoic agents and with C.sub.12 and C.sub.14 acids with
antiandrogen activity is one of the objects of the invention, and
is proved to be particularly useful for stimulating the hair follicle
and keeping the skin nourished thanks to a higher supply of blood,
and, therefore, of trophic substances. As a result, after a few
days of treatment, a marked change in the skin occurs, with an increased
number of perfused capillaries and an absence of dandruff; hair
follicles are normal and patent, and the sebum production is normal.
The above mentioned products, when combined together, are suitable
for the administration in the form of hydroalcoholic lotions (which
are those preferred for treatments of the scalp,) or in the form
of gels.
The preferred combinations for said treatments contain a combination
of visnadin or khellin, in concentrations ranging from 0.2% to 3%;
preferably 1 to 2% ximenynic acid or esters thereof, in concentrations
ranging from 0.2% to 10% (preferably 0.5 to 1.5%); and lauric acid
in concentrations ranging from 0.1% to 1% (preferably 0.2 to 0.5%).
In typical treatment, about 0.1 to about 1 g, and preferably 0.5
g of a lotion or gel of this formulation is applied topically. Visnadin
and khellin can advantageously be replaced by esculoside or by its
aglucon esculetin, in concentrations varying from 0.3% to 4% (preferably
1 to 2%). Typically, about 0.1 to about 1 g, preferably 0.5 g of
a lotion or gel containing esculoside or esculetin is applied topically.
Esculoside, in combination with ximenynic acid and the esters thereof
and lauric, myristic and isomyristic acids, is particularly suitable
for the treatment of early hair loss and for the stimulation of
hair growth. These components are used in combinations in the amounts
described above. The balance of the formulation contains a liquid
carrier, such as an alcohol, preferably ethyl alcohol, optionally
in combination with about 1 to about 20 weight percent of a siloxane
compound or mixture of siloxane compounds. The treatment with these
substances can vary from a few days to 6 months. About 0.1 to 1
g of the compositon is applied to the subject each day to assure
that therapeutically effective amounts of the active ingredients
are delivered. |