Fexofenadine microcapsules and compositions containing them

• US 10,166,220 B2
• Filed: 12/02/2015
• Issued: 01/01/2019
• Est. Priority Date: 12/02/2009
• Status: Active Grant

• Current Assignee: Adare Pharmaceuticals S.R.L. (Adare Pharmaceuticals, Inc.)
• Original Assignee: Adare Pharmaceuticals S.R.L. (Adare Pharmaceuticals, Inc.)
• Inventors: Mapelli, Luigi, Fabiani, Flavio, Boltri, Luigi, Gatti, Paolo, Serratoni, Mauro, Cassanmagnago, Roberto
• Primary Examiner(s): Arnold, Ernst V
• Application Number:
  US14/956,786
• Publication Number:
  US 20160081991A1
• Time in Patent Office: 1,126 Days
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/5026 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5042 Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5047 Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5089 Processes
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• 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 37/00 Drugs for immunological or allergic disorders
• 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 present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Claims

1. A process for preparing a pharmaceutical composition comprising a water suspendable co-granulate of immediate release microcapsules and at least one inactive ingredient, wherein said microcapsules comprise fexofenadine coated with a water-insoluble polymer, wherein said process comprises the steps of:

(a) dissolving a water-insoluble polymer in an organic solvent;

(b) suspending fexofenadine in said organic solvent;

(c) applying a coating of said water-insoluble polymer onto said fexofenadine by phase separation to provide microcapsules;

(d) separating said microcapsules from said organic solvent and (e) co-granulating the microcapsules with at least one inactive ingredient to provide a water suspendable co-granulate.

2. The process of claim 1, wherein said fexofenadine is crystalline fexofenadine.

3. The process of claim 1, wherein said fexofenadine is fexofenadine hydrochloride.

4. The process of claim 3, further comprising drying the separated microcapsules provided by step (d) before the co-granulating step (e).

5. The process of claim 4, further comprising the step of adding a phase inducer agent to said organic solvent to promote step (c).

6. The process of claim 5, wherein said phase inducer agent is selected from the group consisting of polyethylene, polyisobutylene, butyl rubber, polybutadiene, organosilicon polymers, and paraffin.

7. The process of claim 6, wherein said phase inducer agent is polyethylene.

8. A process for preparing a taste-masked immediate release pharmaceutical composition in form of sachets comprising the following steps:

(a) dissolving a water-insoluble polymer in an organic solvent;

(b) suspending fexofenadine in said organic solvent;

(c) applying a coating of said water-insoluble polymer onto said fexofenadine by phase separation;

(d) separating said microcapsules from said organic solvent;

(e) optional wetting of microcapsules;

(f) co-granulating the microcapsules with at least one inactive ingredient;

(g) separately granulating at least one inactive ingredient;

h) mixing of co-granulate obtained in step (f) together with the granulated inactive ingredient obtained in step (g);

(i) filling the bulk mixture of step (h) in sachets.