COMPOSITION PHARMACEUTIQUE POUR TRAITER LES SYNDROMES RHUMATISMAUX, CONTENANT DU SOUFRE, DES GRAINES DE MOUTARDE ET UN SEL DE CUIVRE

PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF RHEUMATIC SYNDROMES CONTAINING SULFUR, MUSTARD SEEDS AND A COPPER SALT

Abrégé français

L'invention concerne une composition pharmaceutique pour traiter les syndromes rhumatismaux, tels que les rhumatismes, l'arthrite, la sciatique et/ou la goutte. Cette composition pharmaceutique est caractérisée en ce qu'elle contient, comme principes actifs, au moins du soufre et des graines de moutarde, ainsi qu'un sel de cuivre. Elle peut en outre contenir éventuellement de la camomille, du camphre et/ou de l'iodate de potassium. L'excipient utilisé de préférence est le talc. Cette composition se présente de préférence sous la forme d'une poudre, par exemple sous la forme d'une poudre pour les pieds. D'autres formes galéniques sont possibles, telles que des crèmes, pommades ou similaires.

Abrégé anglais

The invention relates to a pharmaceutical composition for the treatment of
rheumatic syndromes, especially rheumatism, arthritis, sciatica and/or gout,
characterized in that it contains at least the active substances sulfur,
mustard seeds and a copper salt. The pharmaceutical composition may optionally
contain camomile, camphor and/or potassium iodate. Talc is preferably used as
carrier substance. The composition is preferably available in the form of a
powder, e.g. a foot powder but other forms of administration such as creams,
ointments and the like are also possible.

Revendications

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Claims:
1. Pharmaceutical preparation for treating rheumatic syndromes, especially
rheumatism, arthritis, sciatica and/or gout, characterized in that it contains
at least
the following active agents:
Sulfur, mustard seed as well as a cupric salt.
2. Pharmaceutical preparation especially as per claim 1, characterized in that
the
cupric salt employed is copper sulfate.
3. Pharmaceutical preparation especially as per claim 1 or 2, additionally
containing
camomile and preferably camomile flowers.
4. Pharmaceutical preparation especially as per one of the claims 1 to 3,
containing
talc as its carrier substance.
5. Pharmaceutical preparation especially as per one of the claims 1 to 4,
additionally
containing camphor.
6. Pharmaceutical preparation especially as per one of the claims 1 to 5,
additionally
containing potassium iodate.
7. Pharmaceutical preparation especially as per one of the claims 1 to 5,
characterized in that the preparation is produced in powder form.
8. Pharmaceutical preparation especially as per one of the claims 1 to 7,
characterized by the following volume concentrations of the various
components:

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Sulfur: 30 - 50 % by weight, preferably 30 - 40 % by weight;
Camomile: 0 - 10 % by weight, preferably 5 - 10 % by weight;
Camphor: 0 - 25 % by weight, preferably 15 - 25 % by weight;
Mustard seed:0.5 - 2.5 % by weight, preferably 1 - 1.5 % by weight
Copper sulfate:0.05 - 0.3 % by weight, preferably 0.1 - 0.15 % by weight;
Potassium 0 - 0.15 % by weight, preferably 0.05 iodate: - 0.1 % by
weight;
Talc making up the remainder up to 100 % by weight.
9. Cutaneous form of administration employing a pharmaceutical preparation per
one
of the claims 1 to 8.
10. Cutaneous administration especially as per claim 9, characterized in that
it is in the
form of a foot powder suitable for application on the sole of the foot.
11. Process for producing a pharmaceutical preparation as in one of the claims
1 to 9,
characterized in that, in a first step, talc and sulfur are mixed in powder
form,
followed by a second step in which a small amount of a so-called "catalytic
powder" is added, said catalytic powder being a pulverulent mixture composed
of
talc, mustard seed and a cupric salt, especially copper sulfate.
12. Process especially as in claim 11, characterized in that in the first
phase, camphor
and/or camomile in the form of camomile flowers are optionally added and that
in
the second phase potassium iodate is further added to the "catalytic powder".

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13. Process especially as per claim 11 or 12, characterized in that in the
first phase
the components are first mixed in powder form in a mixer such as a 4-way
mixer,
following which the components to be added in the second step are screened and
added in powder form to, and thoroughly blended with, the mixture of the first
phase.
14. Application of the process per one of the claims 11 to 13 for producing a
foot
powder serving to treat rheumatic syndromes especially such as rheumatism,
arthritis, sciatica and/or gout.
15. Use of the pharmaceutical preparation per one of the claims 1 to 8 for
treating
especially one of the following disorders or ailments:
Sciatica, muscular rheumatism, arthritis, phlebitis (inflammation of a vein),
excessively high or low blood pressure, paralysis deformans (a degenerative,
chronic, not acutely inflammatory disease of a joint), paralysis post myelitis
(inflammation of the spinal cord), poliomyelitis (polio), paralysis cerebralis
(brain-
related paralysis), paralysis post nephritis vel uraemia (paralysis following
a kidney
infection or poisoning of the urinary tract), paralysis postlaesion cause
alicuia
mechanica (paralysis following injuries/lesions after surgical procedures, a
fall,
impact etc.), eczema, and/or x-ray-induced burns.

Description

CA 02358474 2001-07-19
WO 00143021 PCT/CH00100027
PHARMACEUTICAL PREPARATION, , CONTAINING SULFUR, MUSTARD SEEDS
AND A CUPRIC SALT, FOR TREATING RHEUMATIC SYNDROMES
This invention relates to a pharmaceutical preparation offering significantly
improved
properties in the treatment of rheumatic syndromes, especially rheumatism,
arthritis,
sciatica and/or gout, a cutaneous form of administration of a pharmaceutical
preparation,
a foot powder, as well as a method for producing a pharmaceutical preparation
and,
respectively, a foot powder.
Existing literature describes various active agents used in treating rheumatic
and
rheumatoid syndromes. For example, in a special supplement to "Zeitschrift fur
Arztliche
Fortbildung" (journal for advanced medical training), vol. XIII, 15 Nov 1959,
No. 150,
pages 798 to 802, titled "the practical physician", H. Seliger states that it
is especially
colloidal sulfur that has proved effective in treating rheumatism, arthritis
and sciatic,
among others. Beneficial additives mentioned by him include camphor and
camomile
flowers. H. Seliger makes special reference to a pharmaceutical preparation
marketed by
the N. Gschwend company of Herisau which contains the three active ingredients
mentioned together with talcum as the carrier substance.
The monograph D. IT07.10.4 referred to in the bibliography of the IKS Monthly
of 12/1994
describes mustard seed and camomile flowers as pharmaceutically effective
substances
in the cutaneous treatment of arthritis and rheumatic disorders.
Then there are a number of sulfur-containing preparations, indicated for
"rheumatism", in
the form of bath oils and additives with names such as "Soufrol", "Sulfur-Oil-
Bath" and
~Leukona Sulfomoor-Bath".

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This invention is aimed at introducing another pharmaceutical preparation with
good
and/or improved properties for the treatment of rheumatic syndromes.
The active agents contained in the pharmaceutical preparation according to
this invention
for the treatment of rheumatic syndromes and especially rheumatism, arthritis,
sciatica
and/or gout include at least sulfur, mustard seed and a cupric salt.
The characterizing features of other preferred pharmaceutical compositions are
specified
in the subclaims.
The invention also covers a cutaneous form of administration, for the
treatment of
rheumatic syndromes, of a pharmaceutical preparation per this invention. The
cutaneous
form of administration preferably employs a fine-particle foot powder
specially prepared
for application on the sole of the foot.
The preferred fine foot powder is sprinkled into shoes, socks, stockings or
liners
whereupon the active ingredients are absorbed into the blood stream through
the sole of
the foot. This is a unique form of applying a rheumatism antidote and
constitutes a
particular aspect directly associated with the special combination of the
individual active
ingredients as proposed by this invention. The functional mechanism is based
on the fact
that, as the substance makes contact with live and keratinous tissue (that
being the sole
of the foot), a number of chemical transformations take place, aided by the
effect of
natural aspiration, even natural perspiration, leading to corresponding
reactions in two

CA 02358474 2001-07-19
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ways, i.e. by way of both the blood stream and the nerve tissue. As an obvious
prerequisite, the active agents must be adequately resorbed by the skin, which
is assured
by the particular combination of active ingredients per this invention. By
virtue of the
above-mentioned transdermal absorption the organism will only take up exactly
the
amount of active substances that it needs.
Key components of the compounds introduced by this invention are such active
ingredients, present in trace amounts only, as cupric salt which preferably
consists of
copper sulfate, and potassium iodate, to both of which a certain catalytic
effect is
attributed. Correspondingly, these two substances, in conjunction with talc as
the carrier
substance, form a so-called "catalytic powder" which is added in minuscule
amounts to
the other active agents including in particular sulfur and mustard seed.
The process of producing the pharmaceutical preparation begins with a first
step in which
talc is mixed with sulfur as the active agent plus, as an option, camphor and
camomile
flowers. For the blending operation the active ingredients are prepowderized
and, of
course, the talc, or talcum, constituting the carrier substance, is
pulverulent on its part.
As the second step of the process, a minuscule amount of the above-mentioned
so-called
"catalytic powder" is added to the mixture. The catalytic powder again
consists of talc as
well as mustard seed, the cupric salt preferably in the form of copper
sulfate, and, as an
option, potassium iodate.

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The advantage of adding potassium iodate derives in particular from the fact
that it
stabilizes the pharmaceutical preparation for use in hot or tropical regions.
The talcum
carrier substance is known to be less than absolutely stable or suitable for
use in tropical
or hot zones, which makes the addition of potassium iodate necessary or
advisable.
The following explains this invention in more detail with the aid of the
production-process
examples given below and with reference to a sample composition.
As mentioned above, the production follows a bipartite process, i.e. the
pharmaceutical
preparation according to this invention is produced in two steps, dividing the
composition
into two parts.
Part 1:
Sulfur: Approx. 30 - 50 % by weight, preferably 30 - 40 % by weight;
Camomile: 0 -10 %, preferably 5 -10 %;
Camphor: 0 - 25 %, preferably 15 - 25 %;
Talcum (balance): 20 - 65 %.
Total, Part 1: 85 - 95
Part 2:
Mustard seed: 0.5 - 2.5 %, preferably 1 - 1.5 %;
Copper sulfate: 0.05 - 0.3 %, preferably 0.1 - 0.15 %;
Potassium iodate: 0 - 0.15 %, preferably 0.05 - 0.1
Talcum: 3 - 13
Total, Part 2: 5 -15

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The quantities expressed in percent by weight relate to the total weight of
the preparation
composed of Part 1 and Part 2.
For producing the preparation, the first step is to mix Part 1 for which
purpose the
individual components are ground into ultrafine~powder and screened, then
blended with
talc in a mixer, for instance a so-called 4-way mixer, for about 15 minutes.
Part 2 is produced by first grinding copper sulfate and, if applicable,
potassium iodate in a
mortar using a pestle until a homogeneous powder is obtained. These components
are
then sifted, together with talc and mustard seed, for instance through a 0.5mm-
mesh
screen and are then added to and blended with the mixture of Part 1. This can
again be
performed in a 4-way mixer, in this case for about 20 minutes.
Of course, the above quantities are indicated as examples only, subject to
variation and
modification depending on the application i.e. form of administration and on
the ailment to
be treated. Likewise, the mixtures can naturally be produced by methods
deviating from
that described above. It is important, however, that especially when a foot
powder is
produced, the different components making up the foot powder be thoroughly
mixed

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so as to result in a fine powder mixture.
It is also possible to administer the preparation in the form of a cream,
paste or the like,
containing the pharmaceutical preparation for instance as an ultrafine powder
together
with carrier substances and other additives.
Apart from the indications first above mentioned, the pharmaceutical
preparations
according to this invention have also been found to be suitable for
application in the case
of the following disorders or ailments:
Sciatic, muscular rheumatism, arthritis, phlebitis (inflammation of a vein),
excessively high
or low blood pressure, paralysis deformans, paralysis post myelitis,
poliomyelitis, paralysis
cerebralis, paralysis post nephritis vel uraemia, paralysis postlaesion cause
alicuia
mechanica, eczema, and x-ray burns.