Pharmaceutical formulations of ciprofloxacin

• US 20020025964A1
• Filed: 09/06/2001
• Published: 02/28/2002
• Est. Priority Date: 01/21/1986
• Status: Abandoned Application

• Current Assignee: Bernd Streuff, Helmut Luchtenberg
• Original Assignee: Bernd Streuff, Helmut Luchtenberg
• Inventors: Luchtenberg, Helmut, Streuff, Bernd
• Application Number:
  US09/947,593
• Publication Number:
  US 20020025964A1
• Time in Patent Office: Days
• US Class Current: 514/253.08
• CPC Class Codes: A61K 31/495 having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazinesA61K31/48 takes precedence ; with three nitrogen atoms A61K31/53
• CPC Class Codes: A61K 9/2004 Excipients; Inactive ingredients
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds

Abstract

A pharmaceutical formulation comprising by weight 30 to 95% of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quin85 oline-3-carboxylic acid; 4.5 to 25% of a dry binder based on cellulose; 0 to 30% of a disintegration auxiliary based on starch; 0.5 to 10% of a disintegration auxiliary based on a cellulose derivative and/or a cross-linked polyvinyl-pyrrolidone; 0 to 2% of a flow-improving agent, and 0 to 3% of a lubricant. Tablets and capsules made from granules of the formulation, about 0.8 to 2 mm in size, exhibit high bioavailability and excellent storage stability.

Claims

1. A pharmaceutical formulation comprising by weight 30 to 95% of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid;

4.5 to 25% of a dry binder based on cellulose;

to 30% of a disintegration auxiliary based on starch;

0.5 to 10% of a disintegration auxiliary based on a cellulose derivative and/or a cross-linked polyvinylpyrrolidone;

0 to 2% of a flow-improving agent, and 0 to 3% of a lubricant.

2. A pharmaceutical formulation according to claim 1, wherein the 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid is present in 60 to 90% by weight as the HCl salt monohydrate.

3. A pharmaceutical formulation according to claim 1, comprising by weight 60 to 90% of 1-cyclopropyl-6-fluoro-1,4-dihyro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid HCl monohydrate, 3 to 15% of a dry binder based on cellulose;

5 to 16% of a disintegration auxiliary based on starch;

1 to 7% of a disintegration auxiliary based on a cellulose derivative and/or a cross-linked polyvinylpyrrolidone;

0.5 to 1% of a flow-improving agent; and

0.5 to 1% of a lubricant.

4. A pharmaceutical formulation according to claim 1, comprising by weight 72.4 to 78.8% of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid HCl monohydrate, 7 to 9% of a dry binder based on cellulose;

9 to 12% of a disintegration auxiliary based on starch;

4 to 5% of a disintegration auxiliary based on a cellulose derivative and/or a cross-linked polyvinylpyrrolidone;

0.6 to 0.8% of a flow-improving agent; and

0.6 to 0.8% of a lubricant.

5. A pharmaceutical formulation according to claim 1, comprising by weight 72.4 to 78.8% of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid HCl monohydrate;

7 to 9% of microcrystalline cellulose;

9 to 12% of coin starch;

4 to 5% of crosslinkid polyvinylpyrrolidone;

0.6 t 0.8% of cocoidal silicon chloride; and

0.6 to 0.8% of magnesium stearate.

6. A process for the preparation of a pharmaceutical formulation according to claim 1, comprising forming a mixture of the 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid with the dry binder based on cellulose;

adding to the mixture the disintegration agent based on starch and the flow-improving agent, if present, adding water to the mixture in an amount which will permit granulation, granulating the mixture, drying the granules, separating granules having a pore width of 0.8 to 2 mm, and then mixing such granules with the disintegration auxiliary based on a cellulose derivative and/or a cross-linked polyvinylpyrrolidone and with the lubricant, if present.

7. A formulation according to claim 1, in the form of granules of 0.8 to 2 mm in size.

8. Tablets formed of granules according to claim 7.

9. Capsules filled with granules according to claim 7.