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| Cell lines and their use for the production plasminogen activators |
| OF THE INVENTION Production of serum-independent human cell lines The present invention provides ... |
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Time-release
| Details |
Inventors: Horvath, Tibor; Udvardy, Agnes; David, Agoston; Marmarosi nee Kellner, Katalin;
Assignee: CHINOIN Gyogyszer es Vegyeszeti Termekek Gyara Rt. (Budapest, HU)
Primary Examiner: Rose; Shep K.
Assistant Examiner:
Attorney, Agent or Firm: Ross; Karl F., Dubno; Herbert
Time-release pharmaceutical compositions, suitable for oral administration, are disclosed, which comprise as active ingredient 50 to 70% by weight of a compound of the formula (I) ##STR1## or the formula (Ia) ##STR2## wherein R is hydrogen or --CH.sub.2 COOH, R.sup.1 is hydrogen or alkyl having 1 to 4 carbon atoms, R.sup.2 is alkyl having 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 5 carbon atoms, carbamoly or ureido, R.sup.3 is hydrogen or methyl, and the dotted line stands for two hydrogens or another bond, or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, and which further include 4 to 8% by weight of a hydrophobic substance with a great specific surface; 7 to 12% by weight of a lipoid; 8 to 12% by weight of a polyoxy compound; 4 to 9% by weight of a binding agent; and 0.5 to 4% by weight of an acid stabilizer. |
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DETAILED DESCRIPTION We claim: 1.
A tablet or dragee core for a time-release pharmaceutical composition, suitable for oral administration, which comprises as active ingredient 50 to 70% by weight of a compound of the formula (I) ##STR5## or the formula (Ia) ##STR6## wherein R is hydrogen or --CH.
sub.
2 COOH, R.
sup.
1 is hydrogen or alkyl having 1 to 4 carbon atoms, R.
sup.
2 is alkyl having 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 5 carbon atoms, carbamoyl or ureido, R.
sup.
3 is hydrogen or methyl, and the dotted line stands for two hydrogens or another bond, or a pharmaceutically acceptable acid addit ion or quaternary ammonium salt thereof, and which further comprises by weight 1% colloidal silicic acid, 6.
5% hydrophobic colloidal silicic acid, 7 to 12% fatty acid, 8 to 12% microcrystalline cellulose, 4 to 9% polyvinylpyrrolidone-vinyl acetate, and 0.
5 to 4% of an acid stabilizer selected from the group consisting of betaine in hydrochloric acid tartaric acid and citric acid.
2.
The table or dragee core defined in claim 1 wherein the fatty acid is stearic acid present in the amount of 10.
5%, the microcrystalline cellulose is present in an amount of 10%, the polyvinylpyrrolidone-vinyl acetate is present in an amount of 7% and the acid stabilizer is selected from the group consisting of 0.
6% betaine in hydrochloric acid and 3.
5% citric acid.
3.
The dragee core defined in claim 1 coated by a shell which comprises 55% by weight talc, 17% by weight polyvinylpyrrolidone-vinyl acetate, 17% by weight cellulose, 9% by weight titanium dioxide, and 2% by weight polyoxyethylene 6000.
4.
The time-release pharmaceutical composition defined in claim 1 further comprising an inert filling agent or diluent.
5.
The time-release pharmaceutical composition defined in claim 1 which comprises 1,6-dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidzaolium metosulfate of the formula (I) as active ingredient.
6.
The time-release pharmaceutical composition defined in claim 1 which comprises 6-methyl-9-carboxymethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2-a)pyrimidi ne of the formula (I) as active ingredient
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Semiconductor manufacture 
