Note: Descriptions are shown in the official language in which they were submitted.
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The present invention relates to an androgen agent for
growing hair on the human body and increasing vitality in males.
It is an established theory that the growth of all
body hair such an eyebrows, mustaches, and underarm hair, ex-
cluding hair on the head is primarily controlled by androgens
and does not grow very long. Further hair on the head is
primarily controlled by estrogens and grows to great lengths.
It is also known that while there are baldheaded men
there are few baldheaded women from natural causes. Further the
reason why body hair is thick on males and thin on females is
explainable by such hormonal action. In addition, it is also
well known that male vitality can be increased by replenishing
androgens.
As such, several agents for growing body hair consis-
-ting mainly of androgens have been marketed. However, all such
agents cause skin inflammation.
Medical treatments have often been carried out to
enhance the vitality of males by injecting high-ur,i-ts of andro-
gen or by topical application. It is however now cornmon that
strong adverse side effects occur in injection of the high-unit
androgens and topical application thereof causes skin inflam-
mation.
Further, by using androgens for both body hair growth
and as vitality increasing agents, an effect is recognized
because highly concentrated androgen agents are used. Ilowever,
adverse side effects or skin inflammation due to the high con-
centration of the androgen is inevitable.
The present invention provides an androgen agent w'nich
has an excellent effect in increasing a body hair growth in
humans and vitality in males with no significant adverse side
effects and causes no significant skin inflammation as the
androgen is Fed into the skin.
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According to the present invention therefore -there is
; provided an androgen agent for dermatological application for
growing hair on the human body and/or increasirlg its vitality
which cornprises per 100 9 of an ointment base up to 20 mg of
androgen; up to 20 nlg of an adrenocortical hormone and up to 20
mg of vitamin B2.
The present invention is based on the concept that
androgen is a generic nalne for hormones, in particular
testosterone, secreted from the testicles which promote the
growth of the male reproductive organs and has secondary sexual
character, namely they have an androgenic activity. Testoster-
one propionate, methyltestosterone and Fluoxymesterone are
synthetic derivatives of testerone and all have androgen
activity.
It is now considered by the inventor that the androgen
has a body hair generating activity as well as the androgen
activity described above. Thus body hair generation is a live
body phenomenon controlled by androgens in the cutaneous tissue
system, and is required for hair to grow from proteins to
arrange to cultivating conditions while maintaining the normal
living conditions of the cutaneous tissue system.
As in my prior invention as disclosed in my copending
Canadian Patent Application Serial No. 459,176 which is directed
to the development of hair on the head I have found tha-t the
following three conditions are required for the development of
hair on the body; (1) not only to replenish androgen to -the
body, but also to reduce the concentration of androgen until no
skin inflarnmation occurs and there are no other bad side effects
due to its accumulation in the body; (2) to reduce the inflam-
matory action of the androgen by the action of andrenocortical
hormone; and (3) to apply~the metabolism of vitamirl B2 to the
grow-th of hair from protein. I-t has thus been found when an
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androgen agent satisfying these three conditions is applied to
the skin to generate hair on the body, that good hair develop-
ment occurs with no skin inflammation.
For replenishing androgen onto the skin For enhancing
. male vitality, it has been found that such an effect occurs
without adverse side effects and without skin inflalnmation, when
the conditions under which androgen acts is as aforesaid for
hair development on the human body namely healthy living condi-
tions of -the skin tissue. The androgen agent was evaluated by
deterlnining the development of pubes as well as by investiga-
ting the increase vitality of males by applying the androgen
agent locally to the skin of a male. It was found -that the
agent is very good in enhancing vitality with no adverse side
effects and skin inflammation.
Adrenocortical hormones are hormones secreted from the
adrenal cortex including prednisolone acetate, cortisone
acetate, hydrocortisone acetate, methylprednisolone acetate, and
prednisolone sodium succinate, all of which, excep-t aldosterone,
have antiphlogistic action.
In one embodiment of the present invention an androgen
agent for use in growing body hair and increasing vitality in
males according to the present invention is prepared by uni~
formly distributing 1 mg of testosterone propionate (androgen),
1.1 mg of prednisolone acetate (andrenocortical hormone), 0.5 mg
of riboflavine phosphate (vitamin B2 compound), 0.01 mg of
falvine-adenine dinucleotide (vitarnin B2 compound), 0.3 mg of
chlorophenylamine maleate, 1.0 mg of pyridoxine hydrochloride,
2.0 mg of nicotinamide, 1.0 mg of panthothenyl alcohol and 4.0
mg of DL-methionine, 100 g of an ointment base. For such pre-
paration, an ampoule for the injection of each component was
used. For example, for t~he testosterone propionate, 10 mg (1
cc) of injec-tion liquid containing 0.1 cc of testosterone
3B~
propionate was used. Also for each of the ingredients, 2 cc o-f
; injection liquid were used and the injection liquid is an oily
or aqueous liquid.
In a second embodiment in a similar manner as in the
first embodiment, an androgen agent was made up except -that
cortisone acetate (adrenocortical hormone) was used instead of
the prednisolone acetate.
In a third embodiment in a similar manner as in the
first embodiment an androgen agent was made up except that 1 mg
of testosterone enanthate was used instead of the -testos-terone
propionate. For the testosterone enanthate, an equivalent
quanti-ty corresponding to 1/125 of 125 mg (lcc) injection liquid
was used.
In the application of the aforesaid androgen agent
according to the present invention, no skin inflamlnation occurs
and nothing is accumulated in the skin, since the main com-
ponent, i.e. the testosterone propionate (androgen) is present
in the ultra-low concentration of 0.001 percent.
The prednisolone acetate (adrenocortical hormone)
suppresses the inflammatory action of the androgen, and vitamin
B2 compound (riboflavine phosphate and flavine-aden-ine dinu-
cleotide) promotes the growth of body hair and enhances the
vitality activity because it also promotes the metabolism of
proteins in the healthy living conditions of cutaneous -tissue.
Heretofore the actions of the androgen, adrenocortical
hormone and vitamin B2 which is postulated play leading roles in
the effect of agent of the present invention have been given the
other components it is believed also play supporting roles in
-the effec-t of enhancement of hair growth and vitality of the
agent of the present invention. It is believed that chloro-
phenylamine maleate enhances the action of adrenocortical hor-
mone and pyridoxine hydrochloride, nicotinamide, pantho-thenyl
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alcohol, and DL-me-thionine promote respectively the development
of body hair and the increase in vitality by enhanc-ing -the
protein metabolism of vitamin B2.
Fur-ther, it has been found that when the agent
according to the invention is applied for example to the hair
roots of eyebrows, eyelashes grow substantially or when it is
applied to a man's pudenda, -there is seen an increase in
vitality and hair generation in both feet. This means that the
agent according to the invention has its effect on other
locations of the body than the location on which it was applied
due to absorption into the body.
The concentration of the androgen agent according to
the invention is 1 mg of the androgen in 100 9 o-f -the ointment
base, i.e. 0.001 percent and is more concentrated than the
concen-tration of the estrogen of 0.2 mg in 4 litres of distilled
water, namely 0.000005 percent according to the invention of my
aforesaid copending Canadian application. Therefore there was
no fundamental to consider the accumulation of estrogens for
such hair development agent. However the androgen agents
according to the present invention should not be used in a wide
range and over a long period of time without considering the
accumulation of the androgen.
It has been found that the androgen agen-t according to
the present invention has absolutely no adverse side effects and
causes no skin inflammation whilst providing For the substantial
development of hair on the human body and increase in vitality
of males.
The androgen agent according to the present invention
may be used for hair generation by rubbing it into an area where
hair development is desired or for vitality enhancement by
locally rubbing it into t~he skin.
The eFfects of the androgen agent of the present
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inven-tion are given hereafter.
(1 ) A woman 45 years old applied a cupful of the agent with an
earpick once a day and felt i-tching at the applied location.
After approximately one month, it was seen that hair was
generated on her eyebrows and at the same time her eyelashes
grew. She nad continued the application for four months with no
discernable skin inflammation.
(2) A man 55 years old applied the agent in an amount the size
of a bean to his pudenda once a day for approximately three
years. It was found that his pubic hair developed and the hair
simultaneously grew on both his feet. Further when the quantity
of agent at each application was increased, he complained of a
dull pain in his testicles. However he felt no dull pain with
the similar quantity of agent and had no discernable skin
inflammation during the three years of application.
(3) A woman ~0 years old had no pubic hair on her vulva. The
androgen agent according to the invention was applied directly
to her vulva and pubic hair grew in about three months.
