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Патент USA US2050558

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Patented Aug. 11, 1936
.
x, 2,050,558
[UNITED .SATES PATENT oFFicE
.
’\
2,050,558
STABLE HORMONE DRY PREPARATIONS
IN A SOLID ‘CONDITION AND A PROCESS
_ OF PREPARING THEM
'
.
Max Bockmiihl and Fritz Lindner, Frankfort-on
. the-Main, and Otto Schaumann, Wiesbaden,
’ Germany, assignors to Winthrop Chemical
Company Inc., New_York, N. Y., a corpora-.
' tion of New York
No Drawing.
Application March 16, 1934, Serial '
No. 115,996. In Germany March 18, 1933
.
r
(Cl. 167—74) ~
11 Claims.
The present invention relates to’ stable hor
rated and dried hormonerpreparations may be
mone dry preparations in a solid condition andv
mixed in any desired manner with an extender,
to a process of preparing them.
such as urea, lactose or the like.
I
ply hormones parenterally in the form of a dry
5
,
The following examples serve to illustrate the
Many attempts have already been made to ap
substance. Preparations from the posterior lobes
‘of the hypophysis have for instance been ad
ministered in diabetes insipidus in the form of
a snuff. Owing to their extraordinary efficacy the
hormones
in question can be administered in small
10
quantities only and consequently in highly di
lected state. It is, therefore, necessary to tritu
rate the hormones with indifferent powders.
This process requires a stability of the-hormones
It has been
found that the mixture of many hormones with
the usual extenders, such as lactose, urea, or the
15 in the solid diluents in question.
like are not stable. It, therefore, has been sug
gested that the total glands containing the
invention:
-
5
_.
'(1) 20 milligrams of the pulverized hormone
of the posterior lobe of the hypophysis having ~
a tonic e?ect on the intestine and an ‘action pre
venting diuresis and containing ' 100 units per
milligram are dissolved in 2 cc. of glacial acetic 10
acid. There is added a solution of -2 grams of
the sodium salt of protalbinic acid in 10 cc. of
glacial acetic acid and subsequently asv a pre;
cipitant, a mixture "of 100 cc. of acetone and 200
cc. of ether. The precipitate is centrifuged.‘ 15
washed with ether and dried. The dry powder I
is trituratedywith 5 times its weight of lactose.
(2) 20 milligrams of the pulverized hormone '" " '
of the. posterior lobe of the hypophysis having
hormone or hormones should be used in a dried atonic e?ect on‘ the intestine and an action 20
20 or pulverized conditionx Indeed, for some time preventing diuresis and containing 100 units per
‘the total posterior lobe of the cerebral gland has milligram are dissolved in 2 cc. of water and
been used, in the dried form. This expedient,‘ the solution is mixed with 30 cc. of. normal
however, has the drawback that it involves thev serum. The active substance is then precipitated,
administration not only of the hormones desired united with the serum albumen by the addition 25
for each particular case, but of the whole of the of a mixture of 300 cc. of absolute alcohol and
300 cc. of ether, separated, washed with ether
hormones and accompanying substances con
tained in the portion of the gland.
80
'
‘
f
and
dried.
'
'
'
'
'
‘
We have now found that stable dilutions of the
‘hormones, such as the hormone of the posterior
('3) 2o-milligrams of the pulverized hormone
of the-‘posterior lobe of the hypophysis having a 30
lobe of the hypophysis which has a tonic effect
on the intestine and prevents diuresis, the blood
tonic effect on the intestine and an action pre
venting diuresis and containing 100 units per
milligram are dissolved in 2 cc. of glacial acetic
acid and the solution is mixed with a solution of‘
Zgrams of gelatin in 10 cc. of glacial acetic'acid. 35
The active substance is precipiated, united with
the gelatin by pouring the mixed solution into ; a
300 cc. of ether, and is further treated as de
- sugar reducing hormone of pancreas, the sexual
hormone of the anterior lobe of the hypophysis
can be obtained in a solid form by uniting the
hormones obtained according to known ‘meth
ods
with
high-molecular,
albumen-like , sub
stances, the high-molecular decomposition prod
ucts thereof, such as serum albumen, gelatin, . scribed in Example 2.
. (4) 100 milligrams of the blood-su'gar-reducing 40
' ‘o casein, ‘the sodium salt of lysalbinic acid, the
hormone of pancreas in a pure state are dissolved
sodium salt of protalbinic acid, etc. The proc
ess is, for instance, conducted as follows: the in 5 cc. of glacial acetic acid. The solution isv
hormones are dissolved together with the carrier mixed with a solution of 5 grams of gelatin in
substances named above in a solvent suitable for 25 cc. of glacial .acetic acid and the hormone
45 both components, such as water, dilute alkalies,
for instance dilute caustic soda solution, dilute
and- gelatin are precipitated by introducing the
solution, while stirring, into 1 liter of ether. The
caustic potash solution, d?utesodium carbonate
further treatment is carried out as described in
solution; furthermore, organic acids, such as
Example
;
__
'
45
'
(5) 20 milligrams of the pure preparation of "
tions thus'obtained are mixed witha precipitant. the sexual hormone of the anterior lobe of‘the 60
hypophysis ‘from the urine ‘of pregnant women
which will precipitate the hormones and the car
rier ‘substances.- As precipitants there may be are dissolved in 2 cc. of water and the solution
acetic acid. formic acid or the like. The solu
used organic solvents miscible with the solvent
in the solution and in which the hormone and
55 the”carrie1f substance are insoluble. The sepa
1
is mixed with 30 cc. of normal serum. The active
principle is then precipitated together with the
serum albumen by means [of a mixture of 500 cc. to
.
‘ 2
2,050,658
of alcohol and 500 cc. of ether. The i'urther
treatment is carried out as describedin Exam
diuresis-hindering action together with the so
ple 2.
stance in glacial acetic acid, precipitating the
hormone together with the carrier substance ,by
adding a mixture of acetone and ether and drying l
We claim:
_
,
-
1. The process which comprises dissolving a
hormone together with a high molecular albumen
decomposition product as a carrier substance in
a. solvent, precipitating the hormone together
with the carrier substance and drying the pre
10
cipitate.
,
,
-
i
2. The process which comprises dissolving a.
hormone together with a high molecular albumen
decomposition product as a carrier substance in
a solvent, precipitating ‘the hormone together
16 with the carriersubstance by adding an organic
solvent in which both the hormone and the car
, rier substance are insoluble and drying the pre
cipitate.
3. The process which comprises dissolving the
20 hormone of the posterior lobe of the hypophysis
having a tonic effect on the intestine and a
dium salt of protalbinic acid as a carrier sub
the precipitate.
,
6. The process which comprises dissolving the i
‘hormone or the posterior lobe of the hypophysis
having a tonic e?ect on the intestine and a
diuresis-hindering action together with gelatin 10
in glacial acetic acid, precipitating the hormone
together with the carrier substance by adding
ether and drying the precipitate.
'7. A composition of matter comprising a hor-.
mone bound to a high molecular albumen de 15
composition product as a carrier substance.
8. A composition of matter comprising a hor
mone bound to a high moleculargalbumen de
composition product as a carrier substance and
an indiiferent extender.
20
diuresis-hindering action together with a high
9. 'A composition- of matter comprising the hor
mone of the ‘posterior lobe of the hypophysis
molecular albumen decomposition product as a
having a tonic e?ect on the intestine and a
carrier substance in a solvent, precipitating the‘ diuresis-hindering action bound to ‘a high mo
25 hormone together with the carrier substance‘ and lecular albumen decomposition product as a car- 25
drying the precipitate.
_
rier substance.
4. The process which comprises dissolving the
hormone of the posterior lobe of the hypophysis
having a tonic effect on the_intestine and a
30 diuresis-hindering action together with a high
molecular albumen decomposition product as a
carrier substance in a solvent, precipitating the >
'
10. A composition of matter comprising the
hormone of the posterior lobe of the hypophysis
having a tonic effect on the intestine and a
diuresis hindering action bound to protalbinic 3°
acid.
-
11. A composition of matter. comprising the
hormone of the posterior lobe of the hypophysis
hormone together with the carrier substance by
adding an organic solvent in which both the having a tonic e?ect on the intestine and a
35 hormone and the carrier substance are insoluble, ‘diuresis hindering action bound to gelatin.
35
and drying the precipitate;
.
I
‘
5. The process which comprises dissolving the
hormone oi! the posterior lobe of the hypophysis
having a tonic e?ect on the intestine‘. and a
MAX BocKMtiHL.
FRITZ LINDNER.
o'rro sermon/rm.
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