DE1900124A1 - New pharmaceutical compositions based on polystyrene polymers - Google Patents

Description

DR. F. ZUMSTEIN - DR. E. ASSMANN DR. R. KOENIGSBERQER - DIPU-PHYS. R. HOLZBAUER

TELEPHONE: 22 84 70 and S21911

TELEGRAMS! ZUMPAT
CHECK ACCOUNT: MDNOHEN 011 * 0

BANK ACCOUNT i
BANKHAU8 H. AufHÄU8ER

8 MDNOHEN S, ^ RAUHAUSSTRASSE 4 / III

1227 / B

ROUBSEL-UCIAP, PariB / France

New pharmaceutical compositions based on sa == ssssa & ssss = ssssa = s3ss = 3ss = 3s == ss = ssssssss = ss = ss:

of polystyrene polymers

8sssassasss3S3S3sa == sss

The invention relates to new pharmaceutical compositions on the Polystyrene polymer base.

The invention relates in particular to pharmaceutical compositions, which contain polystyrene polymers as the active ingredient, which are commercially available under the registered trademark "Amberlite XAD1" and "Amberlite XAD2" (Rohm & Haas) are available.

The "Amberlite XAD1" and the "Anberlite XAD2" are in Porm small balls with a grain size between 0.35 and 0.44 mro (Sieve 20 to 50). Each of these little balls consists of a multitude of tiny 'grains of uniform size, the porosity of each ball and the very large Ensure that the surface of the pattern has a considerable absorption capacity.

The new pharmaceutical compositions according to the invention have interesting pharmacological properties. she have in particular towards molecules with lipophilic

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Orientation, like dew cholesterol and een fatty acids, one adsorbing effect which it used to treat hyperoholeaterinemia and the atheroaatosis thereby suitable n things, that they adsorb the intestinal bile acids and from there subsequently reduce the cholesterol and fat levels in the blood.

They can be used to treat hypereholesteremia and at arterial diseases can be used as a preventive agent or curative agent.

The new pharmaceutical compositions according to the invention can be administered orally. They can be in the form of lozenges, coated tablets, tablets, sachets, capsules, Granules, suspensions, jellies and jams are available.

The useful dosage ranges from 5 to 30 g of the active ingredient per day, based on 2 to 10 g per ingestion for an adult. The pharmaceutical forms, "such as lozenges, coated tablets, tablets, sachets, capsules, granules, suspensions, jellies and jams herds according to the usual traversing m produced.

Manufacture of a preferred pharmaceutical form

Polymer ¹¹ XADI "or ^η 1ΑΏ2 ^η 20 g

Fruit puree (in solid form:. * M) * 9 to 12.5 g

Apple pectin 1 to 2 g

Citric acid 2 to 4 g

Bucker - 20 to 35 g

Water ad 100 g

A resin XAD1 XAD2 or is obtained as 100 g of a jam with $ 20.

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8AD ORfGIMAL

Adaorptiana digestion of sodium cholate on other polymers:

Kan puts 30 g of the washed polish * Xä $ i2 " (moisture ag rad 41» 4? 'Corresponding to 17 »58 g of dry polymer) in a column with a diameter of 1.5 cm; 200 micrometers of a fig sodium cholate solution are passed inside the ball } 30 minutes over the polymer and 'determines the cfaolaic acid at the outflow of the column quantitatively; the concentration of the sodium cholate solution is then 0.695 *, which corresponds to a 30.5 Hg adsorption of the sodium cholate on the polymer.

One wins under the same experimental conditions after once and for all leading a 0.95 £> igen I; cholate Over 30 g of the polymer "XADI" C Moisture content 38 # corresponding to 18.6 g of dry polymers) 192 ecm one 0.60 # strength sodium hydroxide solution, waa an adsorption of 39 »5 V» sodium cholate corresponds to the polyasera "XABI".

Pharmacological experiment Kypocholesterolämlsche Uirkunk in "Kulms

Male »a 'lay old chicks are on a bypereholesterinemic diet containing 250 ^ sucrose and 2 ^ cholesterol, administered,

The animals are divided into three groups. The first group or comparative group is only hyper-

cholesterolemiaches putter administered.

The second group is puttered with 1.5 fv of polymer em "XAD1 ^M

attached, nourishes what a mean administration of corresponds to about 200 to 250 mg per kg of body weight.

The third group is fed with putters, the 1.5 f ^ framycetin

sulfate are included.

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BATH ORIGINAL.

Some of the animals will after a 14 Sage with the diet were fed, the other part killed after 30 days.

lipids

The level of cholesterol in the serum, the ./fat content, is determined

in the serum and choleeterin in the liver; increasing the The weight of the animals and the weight of the liver are noted

The results are summarized in the following tables

Table It After a fortnight of diet

Group Weight Liver Cholesterol Fats in cholesterol increased in serum Serum in the liver (body) g $ g in g / liter in g / l in g %

comparison 267 II: 4th , 38 2 , 83 13, diet 98 6th , 31 polymer
^W XAD1 " 241 4th 2
(»20 , 27
*) 14, 14th 4th
(-36 , 02 Framycetin
sulfate 3 , 95 2
(-20 , 27 12t
(-14 08 (-35 • 09
V) Tabel To 30 day

Group Weight Liver Cholesterol Fats in Cholesterol

increased in serum serum in the liver

(Body) g fo g in g / liter in g / l in g ^ o

Compare 651 # 3.14 2.53 11.78 7.72

588; < 3.62 2.24 11.24 5.59

(-12V) (-5 ίβ) (»28? Ί)

Fratnycetin- _fiRA ^ " _{R #} . ₉ - 9.91 7.00 sulfate ⁶⁸⁴ "° ² x ^{86 2} x ⁵⁴ (-16 Ji) (-9V)

From these results, it is found that the polymer "XAD1" at a dosage of 200 to 250 mg / kg a clear one has hypocholesterolemic effect and that this

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BAD OWGiNAU

Effect similar to that of framyeetin sulfate after 4 days of treatment is comparable; after 30 days of treatment it is clearly superior to that of the antibiotic.

Male rats, yiistar, weighing about 200 g come with a complete food composition (UAR) nourishes; the amount of food administered per day and per rat is 20 g.

The animals are divided into two groups.

Me first group or comparison group only receives the Food·

The second group is nourished with the putt to which 10 $> of the polymer "XAD1" or the polymer "XAD2" have been added ·

You determine the level of cholesterol after 8 days, 15-day and 21-day treatment.

The results obtained are in the following tables summarized:

Table I: Treatment with polymers »" XAD1 "

Duration of treatment group cholesterol in mg

100 cc serum

8 days comparison
Treated 90.7
78.5 15 days comparison
Treated 84.7
73.0 21 days comparison
Handled 66.7
61.0

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gabeile lit treatment with polymer em ^tf 'KXD2 ^t>

Treatment adaia he group cholesterol in mg

100 cc serum

8 saga comparison
Treated 82.0
63.0 15 pounds age comparison
treated 89.0
75.0 21! 'Age comparison
Treated 77.0
74.0

These results show that the two products show a significant reduction in cholesterol after 8 and 15 days Induce treatment.

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Claims (3)

Patents ns ρ r tt q h β tSSS B? SS 38 ItQ 1. Pharmaceutical compositions * marked with a content of polystyrene polymers "Awfeerlite XA3) 1 * and" Amberllte XA3> 2 ⁿ as an active beat and part euteamsisn »with a pharmaceutically acceptable agent. 2 · Pharmacist laughs β ZueacsmsiiaetBURgen according to Artßprtxoh 1 »characterized in that all active Beatand parts" Amberlite XABI * and contain a pharmaceutical OfrSger · 3. Fharnasentlache ßuB COMMERCIAL SETS according to claim 1, characterized in that all as the active ingredient "Aniberlite XAD2" and a phanaaceatic carrier included · 4 · Use of the pharmaceutical compositions naoh one of the preceding claims as an agent for the treatment of hyperoholeatorinemia and atherotnatosis. 909836 / U15