Orodispersible tablets containing fexofenadine

• US 6,723,348 B2
• Filed: 11/16/2001
• Issued: 04/20/2004
• Est. Priority Date: 11/16/2001
• Status: Expired due to Term

• Current Assignee: ETHYPHARM
• Original Assignee: ETHYPHARM
• Inventors: Faham, Amina, Chenevier, Philippe, Marechal, Dominique
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Bennett, Rachel M.
• Application Number:
  US09/995,975
• Publication Number:
  US 20030099700A1
• Time in Patent Office: 886 Days
• Field of Search: 424/490, 424/465, 424/458, 424/489, 424/495, 424/497
• US Class Current: 424/490
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• 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: A61P 11/00 Drugs for disorders of the respiratory system
• 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 concerns orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, preferably in less than 40 seconds, containing fexofenadine in the form of coated granules, and a mixture of excipients comprising at least one disintegrating agent, a soluble diluent agent, a lubricant and optionally a swelling agent, a permeabilizing agent, sweeteners, flavoring agents and colors; the process for obtaining such orodispersible tablets and the coated granules incorporated therein and the use of said orodispersible tablets in the treatment of seasonal allergic rhinitis.

Claims

1. Orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds containing:

(i) fexofenadine selected from the group consisting of fexofenadine base and at least one of its pharmaceutically acceptable salts, the form of coated granules, and

(ii) a mixture of excipients comprising at least one disintegrating agent, soluble diluent agent, and a lubricant.

2. Orodispersible tablets according to claim 1, which are able to disintegrate in less than 40 seconds.

3. Orodispersible tablets according to claim 1, wherein the mixture of excipients further comprises a swelling agent, an antistatic agent, a permeabilising agent, sweeteners, flavoring agents or colors.

4. Orodispersible tablets according to claim 1, wherein the weight ratio of the mixture of excipients to the coated granules is 0.4 to 9.

5. Orodispersible tablets according to claim 4, wherein the weight ratio of the mixture of excipients to the coated granules is 1.5 to 5.

6. Orodispersible tablets according to claim 5, wherein the weight ratio of the mixture of excipients to the coated granules is 2 to 3.

7. Orodispersible tablets according to claim 1, wherein disintegrating agent is selected from the group consisting of croscarmellose, crospovidone, and mixtures thereof.

8. Orodispersible tablets according to claim 1, wherein the soluble diluent agent has binding properties and consists of a polyol having less 13 carbon atoms and being either in the form of the directly compressible product with an average particle size of 100 to 500 μ

m, or in the form of a powder with an average particle size of less than 100 μ

m, it being understood that sorbitol cannot be used alone and that, in the case where there is only one soluble diluent agent with binding properties, it is used in the form of the directly compressible product, whereas in the case where there are at least two soluble diluent agents with binding properties, one is present in the directly compressible form and the other is present in powder form, it then being possible for the polyols to be the same, the ratio of directly compressible polyol to powder polyol being 99/1 to 20/80.

9. Orodispersible tablets according to claim 1, wherein the proportion of disintegrating agent is from 3 to 15% by weight, and the proportion of soluble diluent agent is 30 to 90% by weight, the percentages being based on the weight of the tablet.

10. Orodispersible tablets according to claim 9, wherein the proportion of disintegrating agent is from 5 to 15% by weight, and the proportion of soluble diluent agent is from 40 to 60% by weight, the percentages being based on the weight of the tablet.

11. Orodispersible tablets according to claim 1, wherein the lubricant is selected from the group consisting of magnesium stearate, stearic acid, sodium stearyl fumarate, micronised polyoxyethyleneglycol, leukine, sodium benzoate and mixtures thereof.

12. Orodispersible tablets according to claim 3, wherein the sweetener is selected from the group consisting of aspartam, potassium acesulfame, sodium saccharinate, neohesperidin dihydrochalcone, sucralose, monoammonium glycyrrhizinate, and mixtures thereof.

13. Orodispersible tablets according to claim 11, wherein the lubricant is in powder form and is, at least in part, disposed on the surface of the tablets.

14. Method of treatment of symptoms associated with seasonal allergic rhinitis wherein orodispersible tablets according to claim 1 is orally administered to patients.

15. Orodispersible tablet of fexofenadine or one of its pharmaceutically acceptable salts, according to claim 1, which is bioequivalent to Allegra®

tablet in a bioavailability study in humans.

16. Orodispersible tablets according to claim 8, wherin the polyol is selected from the group consisting of mannitol, xylitol, sorbitol and maltitol.

17. Orodispersible tablets according to claim 8, wherin the ratio of directly compressible polyol to powder polyol is 80/20 to 20/80.