DE1139236B - Process for the production of therapeutically valuable stitosterol preparations - Google Patents

Description

GERMAN

PATENT OFFICE

B 65853 IVa / 30 h

ANME LDETAG:

NOTICE THE REGISTRATION AND ISSUE OF EDITORIAL:

FEBRUARY 8, 1962

NOVEMBER 8, 1962

The subject of patent application B 62020 IVa / 30h (German Auslegeschrift 1 131 845) is a method for the production of therapeutically valuable sitosterol preparations, which is characterized by that one commercially available, coarsely present sitosterol in the presence of sufficient amounts of Mills fillers to a particle size below 30 microns and the millbase in the presence of Gelatin suspended in water, whereupon from the suspensions thus obtained, if necessary, the Part or all of the water removed.

As detailed in the main patent application, sitosterol only has a good anti-sclerotic effect Effectiveness when it is supplied to the organism in very fine distribution. The administration of sitosterol of the required degree of division, however, stand the high specific volume of a such a product as well as its extremely strong hydrophobicity in the way. More difficulties arise when grinding the commercial product and when compacting the high volume, which (as is also explained in more detail in the main patent application) only by suspension in Water can be effected. The thixotropy is particularly annoying, the aqueous suspensions or Show pastes of finely divided sitosterol.

According to the process of the main patent application, the thixotropy of the Sitosterol suspensions lifted. Since gelatin is commonly used as a thickener, This finding was very surprising, especially since it turned out that alginates and various Cellulose derivatives (carboxymethyl cellulose, ethyl cellulose) do not have such an effect. It was now found that instead of gelatin, methyl cellulose can also be used to neutralize the thixotropy of Can use sitosterol suspensions; Mixtures of these two substances can also be used. the Preparations produced with it have compared to the preparations containing only gelatin increased stability.

To produce the new sitosterol preparations - as in the process of the main patent application - commercially available or otherwise specified coarsely dispersed sitosterol in the presence of suitable fillers, eg. B. crystalline sugars such as cane sugar or milk sugar, comminuted in grinding devices of sufficient dividing power to a particle size below 30 microns, preferably about 5 to 10 microns. The so-called jet mills are particularly suitable for this. Then the grinding method of preparation becomes therapeutic
valuable sitosterol preparations

Addition to patent application B 62020 IVa / 30 h
(Interpretation document 1 131 845)

Applicant:

CF Boehringer & Soehne G. mb H.,
Mannheim-Waldhof

Dr. Peter Rieckmann, Mannheim-Waldhof,
has been named as the inventor

good - in modification of the procedure of the main patent application - made into a paste in the presence of methylcellulose, whereby (depending on the amount of water) Thin suspensions to pastes are obtained which no longer show any noteworthy thixotropy. In general, an addition of about 0.1 to 2% methyl cellulose, based on the amount used, is sufficient Amount of sitosterol. In addition, any desired flavor corrections and preservatives can be added to the pasting or the like. Be added.

Particularly advantageous forms of administration of the sitosterol suspensions to be produced according to the invention or pastes are obtained by lyophilizing the same.

example

40 kg of commercially available sitosterol are added (if necessary after sufficient pre-shredding) 10.0 kg of crystalline cane sugar mixed. The mixture is made on a so-called jet mill ground to a particle size of about 10 microns. The grist is heated with a (warm prepared and cooled again) solution of 0.5 kg methyl cellulose, 12.5 kg sugar, 100 g sorbic acid and 300 g of a 1% alcoholic vanillin solution in 36.6 kg of water to form a homogeneous mass stirred.

The product obtained can be administered directly as "sitosterol juice", although in the case of bottling same in bottles to avoid later sticking of the bottle closures in the In the preparation of the juice, it is advisable to replace about 10% of the above-mentioned amount of water with glycerine are.

209 680/317

By lyophilizing the juice one obtains a therapeutic application in some cases particularly suitable »sitosterol granules«.

Claims (1)

PATENT CLAIM: Process for the production of therapeutically valuable sitosterol preparations according to patent application B 62020 IVa / 30h (German Auslegeschrift 1 131 845), in which one grinds commercially available, coarsely present sitosterol in the presence of sufficient amounts of fillers to a particle size below 30 microns and the millbase in the presence of Suspended gelatin in water, whereupon the water is removed from the suspensions thus obtained, if necessary, in whole or in part, characterized in that the gelatin used to make the ground material is completely or partially replaced by methylcellulose.