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|Title:||Sustained-release preparations of quinolone antibiotics and method for preparation thereof|
|Abstract:||The present invention relates to an orally administrable preparation comprising a quinolone antibiotic which releases the active compound with a delay.|
|Inventor(s):||Kanikanti; Venkata-Rangarao (Leverkusen, DE), Rupp; Roland (Bergisch Gladbach, DE), Weber; Wolfgang (Koln, DE), Deuringer; Peter (Koln, DE), Henck; Jan-Olav (Willich, DE), Sta.beta.; Heino (Koln, DE), Nishioka; Takaaki (Nabari, JP), Katakawa; Yoshifumi (Kusatsu, JP), Taniguchi; Chika (Nishinomiya, JP), Ichihashi; Hitoshi (Suita, JP)|
|Assignee:||Bayer Schering Pharma AG (Leverkussen, DE)|
1. Orally administrable preparation comprising ciprofloxacin as an active compound, characterized in that it contains a mixture of a) gel-forming polymer which is a
cellulose ether of a viscosity of 5 to 400 cP, measured as 2% polymer concentration by weight aqueous solution at 20.degree. C., and b) a mixture of a salt with the free base of ciprofloxacin at a salt-to-free base weight ratio of from about 1.3:1 to
about 1.8:1; wherein the preparation releases 80% of the active compound both in 0.1 N hydrochloric acid and in acetate buffer at pH 4.5 in the USP XXIV paddle test at 50 revolutions per minute / 37.degree. C. in the course of 1 to 4 hours.
2. The preparation according to claim 1, characterized in that the salt and the free base are ciprofloxacin hydrochloride and ciprofloxacin betaine, respectively.
3. The preparation according to claim 1, characterized in that the gel-forming polymer is hydroxypropylmethylcellulose of a viscosity of at most 75 cP, measured as a 2% polymer concentration by weight aqueous solution at 20.degree. C.
4. The preparation according to claim 3, characterized in that the hydroxypropylmethylcellulose has a viscosity of at most 50 cP, measured as a 2% polymer concentration by weight aqueous solution at 20.degree. C.
5. The preparation according to claim 3, characterized in that it contains 2 to 20 parts by weight of active compound mixture per part by weight of hydroxypropylmethylcellulose.
6. The preparation according to claim 1, wherein the gel-forming polymer is selected from the group consisting of alkylcellulose, hydroxyalkylcellulose, carboxyalkylcellulose, alkali metal salts of carboxyalkylcellulose, and crossliniked carboxymethylcellulose.
7. The preparation according to claim 6, wherein the gel-forming polymer is a hydroxyalkylcellulose.
8. The preparation according to claim 1, further comprising an organic acid having from 2 to 10 carbon atoms and from 1 to 4 carboxyl groups.
9. The preparation according to claim 8 wherein the organic acid is succinic acid.
10. The preparation according to claim 1, characterized in that the preparation is a combination preparation comprising a rapid-release (IR) part and a delayed release (CR) part.
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