Pharmaceutical composition for piperidinoalkanol compounds

• US 5,932,247 A
• Filed: 10/09/1997
• Issued: 08/03/1999
• Est. Priority Date: 02/28/1995
• Status: Expired due to Term

• Current Assignee: Aventisub II, Inc. (Sanofi )
• Original Assignee: Hoechst Marion Roussel Incorporated (Sanofi )
• Inventors: Schoeneman, Aaron W., Schnitz, Joseph M., Attarchi, Faraneh, Mitchell, Kristen C., Ortyl, Thomas T., Pierce, Marguerite L., Phadke, Deepak S., Skultety, Paul F.
• Primary Examiner(s): JORDAN, KIMBERLY R
• Application Number:
  US08/948,005
• Time in Patent Office: 663 Days
• Field of Search: 424/452, 424/465, 514/777, 514/781
• US Class Current: 424/452
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.

Claims

1. A pharmaceutical composition in solid unit dosage form prepared by a process comprising blending together a compound of the formula:

##STR10## wherein X is a number ranging from about zero to 5, and the individual optical isomers thereof, with microcrystalline cellulose, lactose and pregelatinized starch;

adding a solution of gelatin in water mixing;

drying and milling the mixture; and

adding croscarmellose sodium with mixing, wherein the resulting mixture is filled into capsules.

2. A pharmaceutical composition in solid form wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are present in amounts of about 4.8%, 33.7%, 33.7%, 9.6%, 3.5% and 0.5%, respectively, by weight of the composition, wherein the final mixture is pressed into a tablet from which the quantity of compound of the formula:

##STR11## wherein X is a number ranging from about zero to 5, and the individual optical isomers thereof, dissolved in 45 minutes, is not less than 75% of label in water at about 37°

C. and about 50 rpm when measured using USP Apparatus 2.

3. A pharmaceutical composition in solid form wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starach, gelatin and magnesium stearate are present in amounts of about 4.8%, 25.7%, 25.7%, 9.6%, 3.5% and 0.75% respectively, by weight of the composition wherein the final mixture is pressed into a tablet from which the quantity of compound of the formula:

##STR12## wherein X is a number ranging from about zero to 5, and the individual optical isomers thereof, dissolved in 45 minutes, is not less than 75% of label in 0.001 N aqueous hydrochloric acid at abaout 37°

C. and about 50 rpm when measured using USP Apparatus 2.

4. A pharmaceutical composition in solid form wherein croscarmellose sodium, microcrystalline cellulose, pregelatinized starch, and magnesium stearate are present in amounts of about 6%, 33.3%, 30% and 0.75% respectively, by weight of the composition wherein the final mixture is pressed into a tabalet from which the quantity of compound of the formula:

##STR13## wherein X is a number ranging from about zero to 5, and the individual optical isomers thereof, dissolved in 45 minutes, is not less than 75% of label in 0.001 N aqueous hydrochloric acid at about 37°

C. and about 50 rpm when measured using USP Apparatus 2.