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Патент USA US2410949

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Patented Nov. 12, 1946
2,410,949
UNITED STATES PATENT OFFICE
2,410,949
LIQUID PHARMACEUTICAL PREPARATION
Walter Karrer, Riehen, near Basel, Switzerland,
assignor to Hoifmann-La Roche Inc., Nutley,
N. J ., a corporation of New Jersey
No Drawing. Application February 5, 1943, Serial
No. 474,878. In Switzerland April 1, 1942
4 Claims.
(01. 1.67-—65) ,
1
Since it was ascertained that citrin causes an
increase of capillary resistance (Deutsche Medizi
nische Wochenschrift, year 1936, page 1325), it
is not probable that the same physiological ac
tion also appertains to various pure and nat
2
that may have remained undissolved. A clear,
light yellow solution with a neohesperidin con
tent of about 2 per cent is obtained. The solu
tion can be sterilised.
Example 3
urally occurring glucosides of the ?avon group
and their aglucones (Klinische Wochenschrift,
year 1941, page 1265). However, these pure
?avon glucosides and their aglucones in ques
tion are hardly soluble in water so that there is
7 parts by weight of hesperetin are shaken for
3 hours with 1000 parts by weight of a 30 per
cent aqueous solution of sarcosin anhydride. The
product is ?ltered and a clear, yellowish solution
no possibility of preparing aqueous solutions
with a hesperetin content of 0.6 to 0.7 per cent
thereof for clinical testing by injection. The ad
is obtained. The solution can be sterilised.
ministration of these substances was,v therefore,
I claim:
limited to the oral application, and demonstra
1. An aqueous solution of a substance of the
tion of the therapeutic e?ect has not been 15 group consisting of ?avon glucosides and aglu
de?nitely established.
cones thereof, said solution containing said sub
It has now been found that on using sarcosin
anhydride as material for increasing the solu
stance in an amount greater than that soluble
by itself in the aqueous solution, and sarcosin
bility, su?iciently concentrated and stable solu
anhydride present in an amount effective to
tions can be prepared, not only of the glucosides 20 maintain said solubility.
‘in question but also of ‘the aglucones, which are
2. A liquid pharmaceutical preparation con
thus made available for experimental injection.
taining water, sarcosin anhydride, and quercit
Sarcosin anhydride, in comparison with other
rin, said quercitrin being present in an amount
materials which might be considered for in
greater than that soluble by itself in the prepara
creasing the solubility, has the great advantage 25 tion, and said sarcosin anhydride being present
that it is well tolerated even in concentrated
aqueous solutions and that even in high doses
in an amount effective to maintain said solu
bility.
it is absolutely harmless.
»3. A liquid pharmaceutical preparation con
Example 1
30 taining water, sarcosin anhydride, and neohes
peridin, said neohesperidin being present in an
15 parts by weight of quercitrin are shaken for
amount greater than that soluble by itself in the
3 hours with 1000 parts by weight of a 30 per cent
preparation, and said sarcosin anhydride being
aqueous solution of sarcosin anhydride. The
present in an amount effective to maintain said
product is ?ltered, whereby a clear, yellow solu
solubility.
.
tion with a quercitrin content of 1.4 to 1.5 per 35
_4. A liquid pharmaceutical preparation con
cent is obtained. It can be ?lled into ampuls
taining water, sarcosin anhydride, and hesper
and sterilised.
etin, said hesperetin being present in an amount
Example 2
greater than that soluble by itself in the prepara
20 parts by weight of neohesperidin are shaken
tion,
and said sarcosin anhydride being present
for 3 hours with 1000 parts by weight of a 20 40 in an amount e?ective to maintain said solu
per cent aqueous solution of sarcosin anhydride.
bility.
The product is ?ltered on‘ from any substance
WALTER KARRER.
1
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