MEDICAMENT ANALGESIQUE ET ANTI-INFLAMMATOIRE

ANALGESIC AND INFLAMMATION-INHIBITING MEDICAMENT

Abrégé français

On décrit l'utilisation du médicament à effet analgésique et anti-inflammatoire, à base végétale et renfermant les constituants ci-après: Populus tremula, Solidago virgaurea, Fraxinus excelsior, comme excipient unique de l'efficacité, en tant qu'agent thérapeutique de base.

Abrégé anglais

The use is described of the medicament with analgesic and inflammation-
suppressing action based on
plants and containing populus tremula, solidago virgaurea and fraxinus
excelsior as the sole active vehicle as
a basic therapeutic.

Revendications

-6-
Claims
1. Use of the medicament having analgesic and
inflammation-inhibiting action on a plant basis and
containing the constituents
Populus tremula
Solidago virgaurea
Fraxinus excelsior
as the sole carrier of the activity as a basic
therapeutic.
2. Use of the medicament according to Claim 1,
containing about
50 - 70 vol.-% of Populus tremula
- 30 vol.-% of Solidago virgaurea
10 - 30 vol.-% of Fraxinus excelsior
as a basic therapeutic.
3. Use of the medicament according to Claim 1 or 2,
containing about
60 vol.-% of Populus tremula
vol.-% of Solidago virgaurea
20 vol.-% of Fraxinus excelsior
as a basic therapeutic.
4. Use of the medicament according to one of Claims
1 to 3, in which bark and leaves are present in the ratio
1 : 2 in the constituent Populus tremula, as a basic
therapeutic.

Description

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0 407 634 A1
Analgesic and inflammation-inhibiting medicament
The use of the medicament having analgesic and
inflammation-inhibiting action on a plant basis and
containing the constituents
Populus tremula
Solidago virgaurea
Fraxinus excelsior
as the sole carrier of the activity as a basic therapeu-
tic is described.

~ v a x
.._ - 2 -
EP 0 407 634 A1
Analgesic and inflammation-inhibiting medicament
The invention relates to an analgesic and
inflammation-inhibiting medicament.
In the therapy of inflammatory rheumatological
diseases, in particular rheumatoid arthritis, two
different medicinal principles are used side by side. The
first consists in the reduction of the pain and the
inflammatory symptoms in the joint concerned. Various
classes of substance, for example salicylic acid ~leriva-
Lives, acetic and propionic acid derivatives or oxicams
are used for this purpose. A summarising expression is
"non-steroidal antirheumatics" (NSAR). Their activity is
evaluated in the joint concerned itself. The effects
occur rapidly (hours to days). The dose is suited to the
immediate situation. A change in course of the. inflam~
matory rheumatic disease does not occur as a result of
these medicaments.
The medicament purely on a plant basis described
in the WTPO document (T~TO, 87/02248) likewise has the
effects of the non-steroidal antirheumatics (NEAP,)
together with better tolerability.
In addition to the activity described, agents are
known and are intensively additionally sought, which
favourably influence the entire course of incurable
chronic diseases (so-called disease-modifying drugs).
They influence pain and inflammation only after long
administration ( over a period of months ) ~,aith maintenance
doses and are afflicted with considerable side effects-
(about a third of the patients have to discontinue this
treatment). Their activity is initially recognised in an
improdement in the signs of systemic inflammation. This
is in particular an improvement in the erythrocyte
sedimentation test, which is generally used as a method
for the assessment of an inflammatory event. Other tests,

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which, in principle, give no other evidence, are, for
example, C-reactive protein (CPR). The long-term ai.m in
this treatment is the reduction or avoidance of joint
destruction by rheumatic inflammation. This therapy is
familiar today under the name basic therapy.
Because of frequent and occasionally critical
side effects, there are carefully worked out rules for
treatment with basic therapeutics. For example, results
from a 20-week double blind study should be quoted for
the change in the erythrocyte sedimentation test
(Ward, J.R. et al., Arthritis and Rheumatism Vol. 26,
No. 11, 1983, pages 1303 - 1315).
Medicament ESR before ESR after 20
therapy weeks
Placebo 55 51
Auranofin 63 22
Gold Na thioma- 58 33
late
ESR =
Erythrocyte sedimentation
rate in min/h
only
for the first
hour
Surprisingly,
it has
now been
found
in an
inves-
tigation
in various
research
centres
that basic
therapeutic
effects
were also
achieved
using
the medics--
went disclosed
in WO
87/02248.
This medicament
having
analgesic
and
inflammation-inhibiting
action
on a.
plant
basis
is
distinguished
by the
constituents
Populus
tremula,
Solidago
virgaurea
and Fraxinus
excelsior
as the
sole
carriers
of the
activity.
Tt has
proved
advantageous
if the
medicament
"..
according
to the
invention
contains
50 - 70
vol.-~
of
Populus
tremula,
10 - 30
vol.-~
of Solidago
virgaurea
and
10 - 30
vol.--~
of Fraxinus
excelsior.
A particularly
preferred
composition
of the
medicament
according
to. the
invention
contains
about

v .' J ~' 1 . "7
- 4 - ~d~~~;'x~
60 vol.-~ of Populus tremula, 20 vol.-~ of Solidago
virgaurea and 20 vol.-~ of Fraxinus excelsior.
It is finally in the scope of the invention that
bark and leaves are present in the ratio 1 . 2 in the
constituent Populus tremula.
The present invention consists in the surprising
discovery that this medicament can be employed not only
for the immediate treatment of rheumatic diseases, but
rather, in particular, also as a basic therapeutic.
As an example of the basic therapeutic action of
the medicament identified according to the invention,
results of investigations in the rheumatological depart-
ment of a hospital are reproduced, in particular by means
of the CRP values of the medicament according to
WO 87/02248. A clear reduction in these values is shown.
It can be safely said that owing to the administration of
the medicament of WO 87/02248, the inflammatory activity
of the rheumatological diseases - expressed by C-reactive
protein - was clearly lowered. Some results are given
below in tabular form:
CRP Values
Time interval Average value Standard
deviation
Before WO 87/02248 i 46.2 32.1
After 3 months 37.4 30.9
After 6 months 32.9 26.4
After 9 months ~ 29.4 21.8
After 12 months 27 . 9 21 > 3
r ~ ~
Care has to be taken i,n this case that the
patients in both groups investigated here have addi-
- tionally received a long-term basic therapy which has
already beers, carried out for a long time at the beginning
of the test. This was not changed, as the discovery was
unforeseeable. The effects as a result of the medicament
on a plant basis according to WO 87/02248 consequently go
beyond effects already achieved. 7Cn this case; the group
of the medicaments on a plant basis according t~

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WO 87/02248 starts out from more unfavourable values than
the placebo group.
Under these conditions, a reduction in the
erythrocyte sedimentation test of 31 ~ is a considerable
effect.
During monitoring of 5 patients with rheumatoid
arthritis who had already been treated, it turned out
that as a result of additional administration of the
medicament on a plant basis according to WO 87/02248,
downward changes, i.e, in the therapeutic direction,
occur (lacuna) the starting values in three out of five
cases in the erythrocyte sedimentation test and in four
out of five cases- with C-reactive protein within four
weeks. This clear effect is surprising for several
reasons:
1. The dosages used here have not been determined
with respect to the basic therapeutic activity.
They correspond, rather, to the dose on symptoma~.
tic therapy.
2. The effects observed are additional effects in
the basic therapy already carried out. In the
case of the discovery, it would be ethically
unjustifiable to withhold a known effective
therapy from the seriously ill. It was completely
unexpected that a further increase in the basic
therapeutic activity could occur over and above
this traditional therapy.
3. For the appreciation of the discovery, it has
to be considered that the medicament on a plant .
basis according to WO 87/02248 is essentially
better tolerated compared to other antirheunaa-.
tics. From this, there is the possibility
3:1 both to achieve greater effects by means of
h~.gher doses and .
3.2 to increase their effectiveness further by
additional use of the medicamewt according to
WC) 87/02248 in addition t~ traditional basic
therapy .