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Патент USA US3080302

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3,080,287
United States Patent 0 ” ICC
Patented Mar. 5, 1963
2
the above Example 1, whereby the individual ingredients
3,080,287
are used in the following ranges:
ANALGESIC COMPOSITIONS
Mozes Juda Lewenstein, 83-75 116th St,
Aspirin __________________________ __grains__ 2- 6
Kew Gardens, N.Y.
Phenacetin _________________________ __do_.__
No Drawing. Filed Aug. 5, 1957, Ser. No. 676,392
2 Claims. (Cl. 167-65)
Caffeine
_
_____
___
1- 4
do___ '1A- 1
Hexobarbital _________________ __milligrams__ 20-60
This invention relates to analgesic compositions and it
The resulting mixtures are formed to tablets, in conven
has particular relation to compositions in which anal
tional manner.
gesic compounds of the type described hereinafter are 10
Example 3
used in combination with a barbituric acid compound of
the type disclosed and under the conditions described
hereinafter.
Combinations of analgesics with barbituric acid com
pounds have been suggested previously. The purpose of 15
such combinations was not only to relieve pain, but also
to simultaneously calm down nervous patients by the
action of thereapeutic doses of the barbituric acid ingredi
ent in the combinations. The use of such doses renders
Mgm.
Acetylsalicylic acid ______________________ __ 224.00
Acetophenetidine
________________________ .__ 160.00
5-A’-cyclohexenyl-S-methyl
N-methyl-barbituric acid ________________ __
60.00
Ingredients used in ?rst granulation:
Starch added wet paste _______________ __
33.84
Certi?ed yellow #5 tartrazine, 91% _____ __
0.12
these compositions less suitable for daytime administra 20
Acacia
7.50
tion to patients who have to attend their work or other
activities, since therapeutic doses of most barbiturates tend
Sugar ______________________________ _._
__
____
..__
7.50
Ingredients used in second granulation:
Starch added wet paste _______________ .._
38.33
to induce sleep and make the patients drowsy. Another
disadvantage of such compositions is the cumulative effect
Certi?ed yellow #5 tartrazine, 91% ____ __
0.10
of repeated therapeutic doses of ba-rbituric acid com 25
Stearic acid _________________________ __
4.99
pounds when the compositions have to be repeatedly ad
ministered during a protracted period of time.
Talc
The use of mild analgesics, such as aminopyrine or
aspirin, in combination with barbiturates has also been
suggested, but the results were not encouraging, because 30
it has been found that little additional analgesia was con
Sta-rch q.s.
_____ __
____
5.99
7.94
Example 4
In any of the above Examples 1-3, an equal part by
weight of thiamylal sodium or three times in weight doses
of thiopental can be substituted for the hexobarbital. A
ferred by barbiturates in combination with such mild anal
mixture of these barbiturates can also be used. Further
gesics, neither were other advantages obtained.
more, instead of the respective barbituric acid a therapeu
It has now unexpectedly been discovered that improved
analgesic effects can be obtained by compositions in which 35 tically applicable salt thereof, e.g. the sodium salt, can be
used and instead of caffeine, an equivalent amount of a
the mild analgesics and the barbituric acid compounds de
therapeutically applicable caffeine salt, can be used.
scribed hereinafter are combined with each other under
According to the present invention the above named in—
the conditions of the present invention.
gredients, i.e. aspirin, phenacetin, caffeine are used in the
According to the present invention it has been found
that by using a therapeutic dose of (a) aspirin (acetyl 40 usual therapeutic doses, while a barbituric acid compound
which is rapid on onset and short in duration, is used in
salicylic acid) in combination with (b) phenacetin (ace
sub-therapeutic doses. In the above described propor
tophenetidine), (c) caffeine and (d) with a sub-therapeu
tions, due to co-action of these ingredients a substantially
tic dose of a barbituric acid compound, which is rapid on
increased synergistic analgesic effect results, which can
onset and short in duration of its effect, composiitons are
obtained in which the analgesic effect of the active ingredi 45 not be obtained in the absence of ingredients and propor
tions called for by the present invention. Thus, for exam
ents is accelerated, increased and prolonged in compari
ple the composition according to the above Example 1
son with the added effects of the individual ingredients,
yields a considerably increased analgesic effect in com
as well as in comparison with partial combinations, e.g.
(a), (c) and (d) or (b), (c) and (d), and which are 50 parison with a similar composition, in which the phen
acetin is omitted or substituted by aspirin, or in which the
practically free from undesired side-effects. In other
aspirin is omitted or substituted by phenacetin, or in
words, ‘this increase and improvement of the effect re
which the conditions called for by the present invention
quires the co-action of the ingredients (a), (b), (c) and
are not observed in other respects.
(d) and represents a novel and unexpected synergistic
The term “rapid on onset and short in duration” is used
effect of these ingredients.
55
in the present application to denote barbituric acid com
In the use of compositions embodying this invention
pounds, the therapeutic action of which is analogous to
drowsiness and hangover and other undesirable side-effects
that of the compounds described in the above Examples.
occurring in the use of known compositions, are usually
The parts mentioned above are parts by weight if not
not encountered.
otherwise stated.
Example 1
60
What is claimed is:
A mixture is prepared from‘ the following ingredients:
1. Analgesic compositions containing as active ingredi~
ents (a) 130-390 parts of acetyl salicylic acid; (b) 65-260
(a) Aspirin _______________________ __grains__
31/2
(11) Phenacetin ______________________ ___do___
(c) Caffeine ________________________ _._do___
parts of acetophenetidine; (0) 16-65 parts ‘of a compound
2%
% 65 selected from the group consisting of caffeine and
50
therapeutically applicable salts thereof; and at least one
compound selected from the group consisting of hexo
The above ingredients are incorporated in conventional
barbital, thioamylal, thiopental, analogous barbituric acid
(d) Hexobarbital ______________ __milligrams__
manner in each table for oral administration.
compounds rapid on onset and short in duration, and
70 therapeutically applicable salts of these compounds, the
Example 2
hexobarbital being used in an amount of 20-60 parts and
thioamylal, thiopental and said analogous barbituric acid
Mixtures are prepared from the ingredients named in
3,080,287
3
4
compounds, being used in amounts equivalent to 20-60
parts of hexobarbital.
2. Analgesic compositions containing as active ingredi
ents (a) aspirin, (b) acetophenetidine, (c) caffeine and
(d) hexobarbital, in the proportions of (a) 31/2 grains
(1)) 2% grains (0) 1/2 grain and (d) 50 milligrams.
Goodman et 211.: “Pharmacological Basis of Therapeu~
tics,” 2nd ed., (1955), Macmillan Co., N.Y., pp 125,
127, 138 and 141.
1957, pp. 11114117.
Orkin et al.: Survey of Anesthesiology, October 1957,
pp. 460-464.
References Cited in the ?le of this patent
Wilson et al.: The American Drug Index, Lippincott
Co., Philadelphia, 1956, pp. 4-5, 50.
Goodman et al.: Pharmacological Basis of Therapeutics
1st ed., 1941, Macmillan Co., N.Y., pp. 275-276 and
436, 438,
~
Friedman et al.: J.A.M.A., vol. 163, No. 13, Mar. 30,
Batterman: I.A.M.A., vol. 155, No. 11, July 10, 1954,
pp. 965-968.
10
Beecher: J.A.M.A., vol. 158, No. 5, June 4, 1955, pp.
399-401.
J.A.M.A., vol. 165, N0. 9, Nov. 2, 1957, pp. 1172
1173.
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