COMPOSES QUINONIQUES OU PHENOLIQUES A USAGE LOCAL

QUINONIC OR PHENOLIC COMPOUNDS AS TOPICAL COMPOSITIONS

Abrégé anglais

ABSTRACT OF THE DISCLOSURE
The invention is concerned with a topical composition
for use on the scalp in seborrheic alopecia, dandruff, greasy
hairs and male pattern baldness. The composition of the inven-
tion contains as active ingredient at least one aromatic com-
pound selected from the group consisting of o-benzoquinone,
p-benzoquinine, menadione, menadione sodium bisulfite, potassium
o-oxyquinolinsulfate and sodium merthiolate, together with a
liquid carrier.

Revendications

The embodiments of the invention in which an exclusive
property or privilege is claimed are defined as follows:
1. A topical composition for use on the scalp in
seborrheic alopecia, dandruff, greasy hairs and male pattern
baldness, said composition containing as active ingredient at
least one aromatic compound selected from the group consisting
of o-benzoquinone, p-benzoquinone, menadione, menadione
sodium bisulfite, potassium o-oxyquinolinsulfate and
sodium merthiolate,together with a liquid carrier.
2. A topical composition according to claim 1,
containing about 0.2% by weight of potassium o-oxyquinolin-
sulfate as active ingredient.
3. A topical composition according to claim 1,
containing about 0.6% by weight of sodium merthiolate as
active ingredient.
4. A topical composition according to claim 1,
containing about 1% to 2.5% by weight of menadione sodium
bisulfite as active ingredient.
5. A topical composition according to claim 1, in
which the liquid carrier is water and/or a lower alcohol.

Description

~ 7 8
TOPICAL COr~OSITION FO~ USE ON THE SCALP
This invention relates to new topical composi-
tions for use on the scalp in seborrheic alopecia, dandruff,
greasy hairs and male pattern baldness.
Until now the purpose of the general and local
treatments of said conditions was mainly to maintain an
abundant blood circulation in the scalp, so as to gi~e the
hair follicles and sebaceous glands as much food as possible.
On the other hand, it is well kno~n that the
androgens are responsible for the accelaration of the cell
metabolism at the level of the follicles and sebaceous glands,
so that the more the blood circulation is abundant, the more
toxic androgens are supplied per time unit.
It is therefore necessary to try a local re-
duction of the action of the androgens.
Applicant has obtained such a reduction by
modifying the blood circulation at the scalp level by
bilateral ligatures of the superficial temporal arteries,
of the back auricular arteries and o~ the occipital arteries.
Such an artery cut or strung causes a noticeable decrease
of the blood flow and an important hypoxia in the skin
territory of the seborrheic alopecia. This therapeutical
action causes an inhibition of enzymes, such as 5 - alpha-
reductase which converts the flowing testosterone into di-
hydrotestosterone which is a metabolite acting on the hair
follicles and the sebaceous glands.
It has also been proposed to inhibit the
action of the scalp by using locally steroids, such as
deoxycorticosterone, androstenedione and progesterone.
However, said steroids are not suitable.

B
Deoxycorticosterone acts on the mineral metabolism
and can therefore not be used as a useful antiandrogen.
Androstenedione is converted into testosterone in the tissues
and does therefore not any more as antiandrogen. Finally
progesterone is a precursor of the androgenic steroids.
Applicant has found products which inhibit the scalp
enzymes, without having the drawbacks of the above steroids.
In accordance with the invention, there is thus
provided a topical composition for use on the scalp in
10 seborrheic alopecia, dandruff, greasy hairs and male pattern
baldness, which contains as active ingredient at least one
aromatic compound selected from the group consisting of o-
benzoquinone, p-benzoquinone, menadione, menadione sodium
bisulfite, potassium o-oxyquinolinsulfate and sodium merthio-
late, together with a liquid carrier.
The active ingredient may be dissolved or dispersed
in the liquid carrier. The liquid carrier may comprise water
or a lower alcohol, such as methanol or ethanol, or a mixture
thereof.
The active ingredients may modify the electron
transport in several ways to inhibit some enzymatic systems
of the skin or scalp.
Some mercury salts generally known as most potent
inhibitors of the SH reagent groups of the enzymes have been
investigated. One of the more powerful of them and the most
innocuous seems to be sodium merthiolate.
Under these conditions, Applicant has treated 296
cases of male seborrheic alopecia with different topical
solutions as described hereafter. Active ingredients were
mostly diluted in water, rarely in alcohol.
--2--
,
.,

17B
249 patients suffering from dandruff, greasy hair
and hair shedding have been treated. I noticed in the other
patients only greasy hair and loss of hair.
All the patients were topically treated five times
a week.
b) Among 15 cases treated with menadione Na bisulfite
(2.5%) I noticed 86% improvement, dandruff and hair shedding
were becoming better than seborrhea.
c) Among 56 patientsj 89% were improved, using ~a
merthiolate (2/oo): hair shedding, dandruff as well as
seborrhea.
d) Among 58 patients treated with K-o-Oxyquinolin-
sulfate (6/oo ), 84% showed improvement in the three principal
symptoms.
e) Among 27 patients using catechol (1/oo ), 80~ were
improved, better hair shedding and dandruff than seborrhea.
; f) Among 69 patients using a blended aqueous lotion
including one part by weight of menadione ~a bisulfite (1%), one
part by weight of catechol (1 /oo), one part by weight of hydro-
20 quinone ~2%) and one part by weight of K-o-Oxyquinolinsulfate
(6 /OO)~ 87% improvement was noticed as well in dandruff and
; hair shedding as greasy hairs.
g) Among 26 patients using Na merthiolate (2 /OO)
and K-o-Oxyquinolinsulfate (6 /OO) mixed fifty-fifty, 95%
were totally improved.