U.S. patent application number 10/533517 was filed with the patent office on 2006-02-16 for daily melatonin dosing units.
This patent application is currently assigned to ASAT AG Applied Science & Technology. Invention is credited to Hans W. Schmid.
Application Number | 20060035924 10/533517 |
Document ID | / |
Family ID | 32233793 |
Filed Date | 2006-02-16 |
United States Patent
Application |
20060035924 |
Kind Code |
A1 |
Schmid; Hans W. |
February 16, 2006 |
Daily melatonin dosing units
Abstract
The present invention relates to a disposable container for a
medicament or cosmetic agent for topical application, containing a
single dose of melatonin or of a melatonin derivative which
corresponds to a locally effective dose but which does not cause
any systemic effect.
Inventors: |
Schmid; Hans W.; (Zug,
CH) |
Correspondence
Address: |
ROTHWELL, FIGG, ERNST & MANBECK, P.C.
1425 K STREET, N.W.
SUITE 800
WASHINGTON
DC
20005
US
|
Assignee: |
ASAT AG Applied Science &
Technology
Baarerstrasse 77
Zug
CH
CH-6302
|
Family ID: |
32233793 |
Appl. No.: |
10/533517 |
Filed: |
October 30, 2003 |
PCT Filed: |
October 30, 2003 |
PCT NO: |
PCT/EP03/12099 |
371 Date: |
August 17, 2005 |
Current U.S.
Class: |
514/310 ;
514/419 |
Current CPC
Class: |
A61K 8/67 20130101; A61P
43/00 20180101; A61P 17/00 20180101; A61K 47/10 20130101; A61K
31/4045 20130101; A61M 35/003 20130101; Y10S 514/88 20130101; A61P
17/14 20180101; A61K 8/492 20130101; A61K 8/9771 20170801; A61Q
7/00 20130101; A61K 9/0014 20130101; A61J 1/067 20130101; A61K
47/46 20130101; A61K 2800/87 20130101; A61K 31/405 20130101; A61K
31/4188 20130101; A61K 31/47 20130101; A61Q 19/00 20130101; A61K
36/16 20130101; A61K 31/4045 20130101; A61K 2300/00 20130101; A61K
31/405 20130101; A61K 2300/00 20130101; A61K 31/4188 20130101; A61K
2300/00 20130101; A61K 36/16 20130101; A61K 2300/00 20130101 |
Class at
Publication: |
514/310 ;
514/419 |
International
Class: |
A61K 31/47 20060101
A61K031/47; A61K 31/405 20060101 A61K031/405 |
Foreign Application Data
Date |
Code |
Application Number |
Oct 30, 2002 |
DE |
102 50 646.9 |
Nov 18, 2002 |
DE |
202 17 814.5 |
Jan 29, 2003 |
US |
10/353,056 |
Claims
1. A disposable container for a medicament or cosmetic agent for
topical application, containing a single dose of melatonin or of a
melatonin derivative which corresponds to a locally effective dose
but which does not cause any systemic effect.
2. The container as claimed in claim 1, characterized in that the
single dose is 0.001 to 1.0 mg of melatonin or melatonin
derivative.
3. The container as claimed in claim 1, characterized in that the
single dose is 0.01 to 0.2 mg of melatonin or melatonin
derivative.
4. The container as claimed in claim 1, characterized in that the
single dose corresponds to a daily dose.
5. The container as claimed in claim 1, characterized in that the
agent is present as a liquid formulation.
6. The container as claimed in claim 5, characterized in that the
liquid formulation has a concentration of 0.001 to 0.01% (by
weight) of melatonin.
7. The container as claimed in claim 6, characterized in that the
liquid formulation has a concentration of 0.003 to 0.004% (by
weight) of melatonin.
8. The container as claimed in claim 1, characterized in that the
agent contains, as sole active substance, melatonin or a melatonin
derivative.
9. The container as claimed in claim 1, characterized in that the
agent contains, as active substances, a combination of melatonin or
a melatonin derivative together with biotin and/or gingko
biloba.
10. The container as claimed in claim 1, characterized in that the
agent contains, as active substance, a combination of melatonin or
a melatonin derivative and vitamin A, vitamin A acid, or another
derivative of vitamin A.
11. The container as claimed in claim 1, characterized in that it
contains 2.5 to 3.5 ml of the agent.
12. The container as claimed in claim 11, characterized in that it
contains 2.9 to 3.2 ml of the agent.
13. The container as claimed in claim 1, characterized in that the
agent is filled into the container under GMP conditions.
14. The container as claimed in claim 1, characterized in that it
is made of a plastic.
15. The container as claimed in claim 14, characterized in that it
is made of polyethylene, polypropylene, polyvinyl chloride,
polystyrene or a mixture of these.
16. The container as claimed in claim 1, characterized in that it
is colorless.
17. The container as claimed in claim 1, characterized in that it
is colored.
18. The container as claimed in claim 1, characterized in that it
is transparent.
19. The container as claimed in claim 1, characterized in that it
is non-transparent.
20. The container as claimed in claim 1, characterized in that it
has, on its head, a disposable closure piece which is opened by
turning it.
21. The container as claimed in claim 1, characterized in that,
after opening, the agent emerges only when pressure is applied.
22. The container as claimed in claim 1, characterized in that it
carries lettering either printed on or embossed and/or is provided
with a label.
23. An arrangement of several containers, as claimed in claim 1,
which are connected to one another in a detachable manner.
24. The arrangement as claimed in claim 23, characterized in that 5
containers are connected to one another in a detachable manner.
25. The arrangement as claimed in claim 23, characterized in that
10 containers are connected to one another in a detachable
manner.
26. The arrangement as claimed in claim 23, characterized in that
it is packed into an aluminum bag.
27. The arrangement as claimed in claim 26, characterized in that
the bag consists of an aluminum-containing laminated foil and
additionally includes polyethylene, polyester and/or paper.
28. The arrangement as claimed in claim 26, characterized in that
the aluminum bag is printed on and/or is provided with a label.
29. A package unit comprising several arrangements as claimed in
claim 23.
Description
[0001] The present invention relates to a disposable container for
a medicament or cosmetic agent for topical application, containing
a single dose of melatonin or of a melatonin derivative which
corresponds to a locally effective dose but which does not cause
any systemic effect.
[0002] Melatonin-containing agents can be used for various medical
and cosmetic purposes. For example, the document DE 101 10 418.9
discloses melatonin-containing compositions for topical application
on the skin and in the hair.
[0003] The subject of the present invention is a disposable
container for a medicament or cosmetic agent for topical
application, containing a single dose of melatonin or of a
melatonin derivative which corresponds to a locally effective dose
but which does not cause any systemic effect.
[0004] The disposable container according to the invention permits
application of a dose of melatonin or of a melatonin derivative
which is locally effective but which causes no undesired change in
the normal melatonin plasma level. The single dose of melatonin or
of melatonin derivative which is applied according to the invention
causes no significant elevation of the melatonin plasma level for
example.
[0005] The expression "melatonin or melatonin derivative", as it is
used in the context of this application, includes melatonin and/or
melatonin derivatives and salts, esters or complexes thereof.
Preferred melatonin derivatives include, for example,
5-methoxytryptamine, 5-methoxytryptophan, 5-methoxytryptophol,
5-methoxy-indole-3-acetic acid and 6-hydroxymelatonin.
[0006] The single dose according to the invention represents a dose
which permits a positive cosmetic and/or therapeutic effect without
significant changes in the plasma level. According to the
invention, a single dose of from approximately 0.001 to
approximately 1.0 mg of melatonin is preferred, and more preferably
a single dose of from approximately 0.01 to approximately 0.2 mg of
melatonin. Depending on the application area or the intended use of
the agent, a single dose can be applied once or several times
daily. In a preferred embodiment, the single dose corresponds to a
daily dose, particularly preferably a daily dose to be used in the
evenings.
[0007] The medicament or cosmetic agent is preferably present as a
liquid formulation. Examples of suitable formulations for topical
application of the agent are solutions, suspensions, emulsions,
microemulsions, nanosystems, creams, gels, lotions, sprays, foams
or ointments, and any other formulation which can be applied
topically. The agent is particularly preferably provided in the
form of a cosmetic solution.
[0008] Depending on its intended use, the medicament or cosmetic
agent contained in the disposable container according to the
invention can have different concentrations of melatonin or of a
melatonin derivative. The agent preferably contains a concentration
of approximately 0.001 to approximately 0.01% (by weight), more
preferably approximately 0.003 to 0.004% (by weight) of melatonin
or of a melatonin derivative. A particularly preferred
concentration is approximately 0.0033% (by weight).
[0009] In one embodiment, the therapeutic or cosmetic agent
contains melatonin or a melatonin derivative as sole active
substance. The agent can, however, also contain one or more further
active substances such as vitamin A, vitamin A acid or other
vitamin A derivatives, biotin and/or gingko biloba.
[0010] In a preferred embodiment, the medicament or cosmetic agent
contains a combination of the active substances melatonin or
melatonin derivative with biotin and/or gingko biloba. The active
substances in this embodiment can be in different dosages. A
particularly preferred dosage of this combination is from
approximately 0.05 to approximately 0.2 mg, particularly preferably
approximately 0.1 mg of melatonin or melatonin derivative, from
approximately 0.2 to approximately 0.4 mg, particularly preferably
approximately 0.3 mg of biotin, and from approximately 1.3 to
approximately 1.7 mg, particularly preferably approximately 1.5 mg
of gingko biloba. Gingko biloba can in this case be contained for
example as an extract, in particular as a dry extract, and/or in
the form of one or more ingredients.
[0011] In a further preferred embodiment, the agent contains a
combination of the active substances melatonin or melatonin
derivative and vitamin A, vitamin A acid or another derivative of
vitamin A. In this preferred active substance combination, the
dosage of melatonin or melatonin derivative is preferably from
approximately 0.05 to 0.2 mg, particularly preferably approximately
0.1 mg of melatonin.
[0012] The medicament or cosmetic agent can also contain one or
more cosmetic and/or pharmaceutical auxiliaries or additives, for
example thickeners, minerals or perfumes.
[0013] The composition according to the invention can be used to
promote hair growth, in particular to prevent and/or treat alopecia
in men or in women. Particularly preferred indications are male
pattern androgenetic alopecia, female pattern androgenetic
alopecia, male pattern diffuse alopecia and female pattern diffuse
alopecia.
[0014] Depending on the intended application or use, the disposable
container according to the invention can contain different volumes
of the medicament or cosmetic agent. In a preferred embodiment, the
disposable container contains approximately 2.5 to approximately
3.5 ml, preferably approximately 2.9 to approximately 3.2 ml of the
agent. A particularly preferred volume is approximately 3.0 ml.
[0015] The therapeutic or cosmetic agent can be filled into the
container using any suitable method known in the prior art. The
agent is preferably filled into the container under GMP conditions.
In this way it is possible to ensure that the agent is sterile and
that, when the agent is applied, no problems arise in respect of
bacterial contamination.
[0016] The disposable container according to the invention can in
principle be made of any desired material, in particular a material
approved for packaging of food products and pharmaceutical
products. Examples of preferred materials are plastics and mixtures
of plastics. Examples of particularly suitable plastics are
polyethylene, polyvinyl chloride, polystyrene, polypropylene,
polycycloolefins or mixtures or copolymers thereof, with particular
preference being given to polyethylene or polycycloolefins.
[0017] Depending on its desired outward appearance, the disposable
container can be transparent, non-transparent, colorless or
colored. Any desired dyes can for example be added to the plastic
in order to obtain a colored container. A non-transparent container
is preferred for use if the agent contains light-sensitive
substances, because a non-transparent container additionally
affords protection from light.
[0018] The disposable container according to the invention can in
principle have any desired shape. Examples of preferred containers
are shown in FIGS. 1 and 2. A suitable disposable container
preferably comprises a part in which the agent is contained, and a
disposable closure piece which is connected to the lower part via a
predetermined break line.
[0019] Simple and safe handling of the container is advantageously
ensured by the fact that it preferably has, on its head, a
disposable closure piece which is opened by turning it. The
container can thus be easily opened. In addition, after opening,
the agent can emerge only if pressure is applied. This pressure can
for example be exerted by hand during the application. This
property allows the user to correctly dose the agent and position
it in a targeted manner. If the agent is to be applied to the scalp
or hair, the opened container can be guided directly through the
hair like a comb. This permits straightforward and safe handling of
the container and correct dosing of the agent.
[0020] Depending on the intended use, the disposable container
carries lettering either printed on or embossed and/or is provided
with a label.
[0021] Two or more disposable containers can furthermore be
connected to one another in a detachable manner. For example, 5 or
10 containers are preferably connected to one another and form an
arrangement. A container or an arrangement of containers can also
be packed, preferably in a lightproof package, particularly
preferably in an aluminum bag for example.
[0022] The expression "aluminum bag", as it is used here, includes
bags made of aluminum and also bags which for example are coated
with aluminum on the outside or inside. For example, bags made of
one or more layers of plastic and/or paper can be coated with
aluminum. A preferred bag comprises, for example, an
aluminum-containing laminated foil which additionally includes
polyethylene, polyester and/or paper.
[0023] A package, in particular a lightproof package, permits
storage over a fairly long period of time without loss of efficacy
of the agent. Furthermore, such a package can provide protection
against gas loss.
[0024] Depending on the intended use, an aluminum bag in which one
or more disposable containers are packed can be printed on and/or
provided with a label.
[0025] In a further embodiment of the invention, a package unit
comprising several arrangements of disposable containers is
provided.
[0026] The invention is further explained by attached FIGS. 1 and 2
and examples.
[0027] FIG. 1 shows an arrangement of 5 disposable containers
connected to one another in a detachable manner and in a preferred
configuration. 1A shows a front view, 1B a plan view, 1C a side
view, and 1D a perspective view obliquely from above.
[0028] FIG. 2A shows a front view of an individual disposable
container in a preferred configuration. 2B shows a front view of an
arrangement of 10 disposable containers connected to one another in
a detachable manner, 2C shows a side view, and 2D shows a plan view
of said arrangement.
EXAMPLES
Example 1
Composition of a Formulation According to the Invention Containing
Melatonin, Gingko Biloba and Biotin as Active Substances
[0029] The composition contains 0.05% by weight of gingko biloba
dry extract, 0.01% by weight of biotin, 0.0033% by weight of
melatonin and other additives, water, and ethanol. The pH of the
composition is between 3.5 and 4.
Example 2
Clinical Study
[0030] The composition described in Example 1 was tested on 8
healthy female patients in a randomized double-blind study with
placebo control and a crossover design. The daily dose was 0.1 mg
of melatonin (3 ml of the composition) which was applied to the
scalp each day before bedtime, for a period of 14 days.
[0031] Urine and blood samples were taken from the patients and
were assayed for melatonin and the metabolite 6-hydroxymelatonin
sulfate.
[0032] It was found that the melatonin plasma profiles of the
patients treated with melatonin or placebo corresponded to the
concentration/time profiles described in the literature for
endogenous melatonin. This confirms that topical application of the
melatonin-containing composition for 14 days does not alter
endogenous melatonin secretion.
[0033] Administration of the composition for 14 days did not
increase the plasma concentration of melatonin, or the
concentration of 6-hydroxymelatonin sulfate in urine, above
physiological concentrations. Topical application of the
melatonin-containing composition was not associated with side
effects. Nor were any effects found on reaction times or on
cortical excitation parameters.
[0034] All things considered, it must be concluded that
administration of the composition does not induce any systemic
effects.
* * * * *