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|Title:||Sustained-release preparations of quinolone antibiotics|
|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 (Cologne, DE), Deuringer; Peter (Cologne, DE), Henck; Jan-Olav (Willich, DE), Stab; Heino (Cologne, DE), Nishioka; Takaaki (Nabari, JP), Katakawa; Yoshifumi (Kusatsu, JP), Taniguchi; Chika (Nishinomiya, JP), Ichihashi; Hitoshi (Suita, JP)|
|Assignee:||Bayer Schering Pharma AG (Leverkusen, DE)|
1. An orally administrable antibiotic matrix preparation comprising a quinolone active compound, wherein the preparation comprises a rapid-release part containing a quinolone active
compound and a disintegrant, and a delayed-release part containing a mixture of a salt with the free base of the quinolone active compound at a salt-to-free base weight ratio of from about 1:10 to about 10:1 and an organic acid having from 2 to 10 carbon
atoms and from 1 to 4 carboxyl groups.
2. The preparation of claim 1, wherein the salt and free base are ciprofloxacin hydrochloride and ciprofloxacin betaine, respectively.
3. The preparation of claim 1, wherein the rapid-release part contains ciprofloxacin hydrochloride, ciprofloxacin betaine, or a mixture thereof.
4. The preparation of claim 1, wherein the disintegrant is crosslinked polyvinyl pyrrolidone.
5. The preparation of claim 1, wherein the organic acid is selected from the group consisting of acetic acid, malonic acid, succinic acid, fumaric acid, tartaric acid and citric acid.
6. The preparation of claim 1, wherein the organic acid is succinic acid.
7. The preparation of claim 1, wherein the delayed-release part further comprises a gel-forming polymer selected from the group consisting of alkylcellulose, hydroxyalkylcellulose, and carboxyalkylcellulose and its alkali metal salts.
8. The preparation of claim 7, wherein the gel-forming polymer is a hydroxyalkylcellulose.
9. The preparation of claim 7, wherein the gel-forming polymer is a crosslinked carboxymethylcellulose or an alkali metal salt thereof.
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