Note: Descriptions are shown in the official language in which they were submitted.
CA 022~7~9 1998-12-04
WO 97/46Z46 PCT/EP97/028q9
COMPLEX PREPARATIONS CHARACTERIZED BY A aETAINE CONTENT
The invention relates to complex preparations for topical, intracorporal,
or oral treatment, affecting, maintaining, and improvinq cellular function,
cellular metabolism, physiological processes, microcirculation, immunity,
homeostasis, and/or prevention, healing, care of various tissue damaging
manifestations, changes in and deformation of tissue, caused by/arising due to
exogenic and/or endogenic factors in humans and animals.
It is known that agents and preparations for treating and/or improving
cellular function, physiological processes, or immunity already exist. It is also
known that there are topical agents for surface stimulation of blood circulation
or for healing and care of the human or animal body. The bases of these agents,
especially where dermatics are concerned, are as a rule antibiotics, cortisones,
antimycotics, and other often very dangerous materials. 8ecause of their side
effects, they are often contraindicated, for example during pregnancy or for
infants. These agents are also associated with other disadvantages because, if
they are effective at all, they are therapeutically effective only after extended
use or when used in conjunction with other agents, or with a special diet. None
of these known agents contain ionic preparations, which, under high osmotic
pressure, can introduce the physiologically necessary materials such as amino
acid-containing substances, enzymes, mineral substances, vitamins, etc. into the
cell interior and blood plasma by its effect on the cell membrane.
CA 022~7~9 1998-12-04
WO 97/46246 ~ PCT/EP97/02849
It is an object of this invention to provide preparations with natural
materials on a phytobiological basis, especially for topical use for fast,
effective treatment, affecting, and maintaining of cellular function, cellular
metabolism, physiological processes, microcirculation, immunity, resistance~
homeostasis, and/or prevention, healing, care of various tissue damaging
manifestations, changes in and deformation of tissue, caused by/arising due to
exogenic and/or endogenic influences in humans and animals, which, under high
osmotic pressure, bring the ions and active ingredients to the cellular layer,
selectively make the cell membrane porous, and introduce themselves into the cell
interior and blood plasma and, with the necessary substances, mineral materials,
amino acids, enzymes, vitamins, proteins, acid, and/or other components, provide
for and significantly contribute to supporting and encouraging physiological
processes and to reestablishing the equilibrium in the organism.
This object is achieved according to the principles of the invention. A
topical agent for treatment of mycotic, microbic tissue damage is known in the
prior art (Patent DE 3816442 C2). [handwritten: INSERT PA OE 2a]
The invention is based on special compositions of the preparations. The
preparations according to the invention comprise ion-containing compounds, salts,
astringent components, amphoterics,
[stamp:l CHANGED PAGE
CA 022~7~9 1998-12-04
NO 97/46246 2a pcT/Ee97/o2849
In addition, UK patent application no. 2 106 386 relates to a preparation
for scalp and hair treatment that contains a mixture of metals ~especially iron
salts, magnesium salts, manganese salts, calcium salts, zinc salts, and copper
salts), phosphates, carbohydrates, amino acids, vitamins, and oils.
[stamp:] CHANGED PAGE
CA 022~7~9 1998-12-04
~O 9?/46246 PCT/EP97/02849
moisturizing agents, bonding and adhesive agents, etheric oils, to which, if
necessary, one or more appropriate materials such as enzymes, vitamins, proteins,
and auxiliary components can be added. The preparations according to the
invention are characterized not only by the presence of ion-containing compounds,
but also by the presence of lipotropic active agents, preferably betaine. Ion-
containing compounds and salts with Na, Cl, K, Mg, Ca, and phosphate are
preferred; preferred astringents are tannin, aspartic acid, and/or sandalwood
oil; a preferred moisturizing agent is qlycerin and a preferred etheric oil is
peppermint oil. Preferred bonding agents include preferably pectin and/or a
hydrogel such as agar gel.
The preparations according to the invention have a comparatively low to
physiologically normal pH value and a comparatively high osmotic pressure. The
components combined according to the invention have a surprisingly effective
synergistic effect, whereby cellular function, metabolism, physiological
processes, and microcirculation are promoted while all tissues are simultaneously
supplied and provided with important substances such as mineral substances, amino
acids, dextrose, enzymes, vitamins, and proteins, which is especially
advantageous in the case of physical stress and disturbed physiological
equilibrium.
If necessary, the preparations according to the invention can also
contain, among other ingredients, plant extracts, emulsifiers, amino acids,
lanolin, glycine, choline, eucerin,
_ . . . ~
CA 022~7~9 1998-12-04
.
W0 97/96296 PCT/EP97/02899
dyes, waxes, bacteriostatics, oils, starches, tin, iron, fats, gelatins,
preservatives, vaseline, camphor, carbamide, tensides, paraffins. The amount for
the components is variable and can be 0.01% for one component and 20% or more for
another.
The examples provided explain this further.
In their consistency or administration, the preparations according to the
invention can be an infundible and/or topical solution, salve, cream, gel,
lotion, powder, spray, foam, emulsion, tablets, capsules, textile wound bandages,
bandages, or can be mixed partially/completely with other agents or other
materials. In the preparations according to the invention, the quantities
provided can increase or decrease and/or components can be omitted and/or
exchanged.
The preparations according to the invention vary in their composition and
the resulting principle and effect of its function, period of effect, methods of
use, interaction, and affordability based upon other comparable prior art agents,
especially agents which are for topical use for affecting, encouraging,
maintaining, and/or restoring cell function, physiological processes,
microcirculation, immunity in human or animal tissue.
As a lipotropic active ingredient, betaine is known as a component in
pro~ucing soothing, surface-active, infection-inhibiting body cleansing agents.
CA 022~7~9 1998-12-04
.
WO 97/46246 PCT/EP97/02~99
Put it is to be regarded as highly surprising that betaine reaches the
deep cellular layer as a lipotropic, amino acid-containing substance in the ion-
containing preparations according to the invention by way of the ions and under
high osmotic pressure and brings about an unexpectedly high cell and nutrient
exchange, an improved microcirculation, and extensive physiological processes.
It is to be regarded as highly surprising that only in the indicated preparations
according to the invention does the betaine reach the deep tissue and display an
effective influence on the cellular and physiological processes.
It is to be regarded as surprisinq that effective substances such as
betaine, but also enzymes, vitamins, and other essential materials and elements
can be quickly and accurately administered in topical form by way of the ion-
contai ni ng preparations according to the invention and under high osmotic
pressure.
The clinical results confirm these surprising effects and show a
significantly improved microcirculation and improved, increased physiological
processes, which especially manifest themselves in skin and muscle tissues,
fibers, joints, and healing processes. These surprising results can also open up
new advantages and opportunities in the immunological, hematological, and
metabolic fields.
The surprising effect of the betaine-containing c ,,u..ds according to the
invention was confirmed by the following clinical tests:
. . . _ , ,
CA 022~7~9 l998-l2-04
WO 97/462q6 PCT/Ee97/02849
~ ifteen female subjects ages 20-58 were divided into three groups of five
each ~A, 8, and C). All subjects exhibited a characteristic manifestation of
cellulitis in the second or third stage on the thigh: pincer test positive,
mattress-shaped bulges visible to the naked eye when standing ~second stage) or
when lying down as well as when standing (third stage), slack skin tone. These
symptoms are the result of deficient, interrupted cellular function and
microcirculation, which leads to a collection of water and fat in the tissue.
During the text period, the subjects were required to change nothing about their
lifestyle and not to begin any diets or aerobics/sport activities.
Group A applied the ion-containing preparation according to the invention
to the affected skin area (right thigh) once a day for 14 days, applying it in
a thin layer and massaging it into the skin until completely absorbed. The
circumference of the thigh was measured at a marked location on the first and
last day of treatment. A tightening and smoothing of the skin was already visible
after four days. After eight days of treatment, a clearly visible reduction of
the protrusion on the skin surface could be observed. After fourteen days, the
treated skin surface was smooth, supply, elastic, and tight. A reduction in thigh
circumference of up to three centimeters was measured in all five subjects.
Group B went through the same treatment with an ion-cont~i ni ng preparation
as group A, but without
CA 022~7~9 1998-12-04
W0 97/46246 PCT/EP97/02849
the inclusion of betaine. After approximately ten days, a liqht smoothing and
tightening of the skin was ascertained in four of the five subjects. However,
after the fourteen-day treatment, there were no further changes or improvements
in the manifestation of cellulitis.
Group C went through the same treatment with a betaine-containing body
cleansing agent. After fourteen days, none of the subjects displayed an
improvement or a positive change, either in the condition of the skin or in the
circumference of the thigh.
Example 1
Component Content in grams Approx. content in %
~etaine 1.0 0.1
Hamamelis 1.0 0.1
Glycerin 20.0 2.0
NaCl 10.0 1.0
MgCl 0.8 0.08
KCl 0.8 0.08
Na~HPO~12H2O 6.0 0.6
Agar 2.0 0.2
Tannin 10.2 1.0
Peppermint oil 0.5 O.OS
Calendula 1.0 0.1
H2O ad 100.0
CA 02257559 1998-12-04
W0 97/46246 PCT/EP97/028qg
Example 2
Component Content in grams Approx. content in %
Petaine 3.0 o 3
Lanolin S0 S.S
Eucerin S0 5.5
Almond oil 100 10.0
Paraffin 100 10.0
NaCl 10.2 1.0
MgCl 0.8 0.08
KCl 0.8 0.08
Tannin 10.0 1.0
Glycerin 20.0 2.0
Vitamins A ~ D 0.13 0.01
H2O ad 100.0
CA 02257559 l998-l2-04
.
.
WO 97/46246 PCT/EP97/02849
Example 3
Component - Content in grams Approx. content in
Betaine lO.0 1.0
Carbamide 3.0 0.3
Ca3(P0~)2 80.0 8.0
Glycerin 80.0 8.0
Na~HPO~ 12H20
NaCl 6.5 0.6
MgCl 0.2 0.02
~Cl 0.2 0.02
Tannin 12.0 1.2
MgO2 2.5 0.25
Pectin 80.0 8.0
Peppermint oil 1.0 0.1
Benzalkonium chloride 0.002 0.0002
H2O ad 100.0
CA 02257559 1998-12-04
.
WO 97/46246 . PCT/Ee97/02849
Example q
Component Content in grams Approx. content in %
Betaine 20.0 2.0
Calendula 0.5 0.05
Hamamelis 0-5 0-05
Pectin 30.0 3.0
Tannin 10.0 1.0
Glycerin 20.0 2.0
Na,HPO~12H2O 6.0 0.6
MgC~ 1.0 0.1
KCl 1.0 0.1
NaCl 10.0 1.0
Peppermint oil 0.5 0.05
H2O ad 100.0
.
CA 02257559 1998-12-04
WO 97/46246 11 PCT/EP97/02849
Example 5
Component Content in grams Approx. content in %
Betaine 20.0 2.0
Avena sativa 1.0 0.7
Echinacea angustifolia 1.0 0.1
Urtica dioica 1.0 0.1
Pectin 1.5 0.15
NaCl 0.3 0.03
KCl 0 3
MgCl 0.3 0.03
Peppermint oil ~ 2.0 0.2
CaHPO~ 2H20
Tannin 0.2 0.02
FeSO, . 0.02 0.002
H2O ad 100.0
CA 02257559 1998-12-04
WO 97/46246 PCT/EP97/02049
12
Example 6
Component Content in grams Approx. content in %
Betaine 60.0 6.0
Pectin 110.0 11.0
Tannin 15.0 1.5
CaH(PO~)2 100.0 10.0
Glycerin 115.0 11.5
NaCl 14.0 1.4
MgCl 1.0 0.1
KCl 1.0 0.1
Na~HP0~12HzO 12.0 1.2
MgO2 2.0 0.2
Peppermint oil 1.0 0.1
Benzalkonium chloride 0.002 0.0002
H2O ad 100.0
, _
