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Pharmaceutical compositions for the treatment of rhinitis

Imported: 23 Feb '17 | Published: 22 Oct '02

Herman Van De Venne, Jean-Pierre Martin

USPTO - Utility Patents

Abstract

A pharmaceutical composition comprising a therapeutically effective amount of a mixture consisting essentially of

(i) pseudoephedrine, an individual optical isomer or a pharmaceutically acceptable salt thereof, and

(ii) at least one compound selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivatives, an individual optical isomer or a pharmaceutically acceptable salt thereof.

Claims

1. A pharmaceutical composition which comprises a therapeutically effective amount of a mixture consisting essentially of

2. A composition according to claim 1, wherein the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivative is a compound having the formula

wherein

3. A composition according to claim 2, wherein X and X′ are each independently selected from hydrogen, chlorine and fluorine atoms.

4. A composition according to claim 1, wherein the said compound (ii) is selected from:

5. A composition according to claim 1, wherein the said compound (ii) is selected from the racemate of 2-[2-[4[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid, its levorotatory and dextrorotatory enantiomers and their pharmaceutically acceptable salts.

6. A composition according to claim 1 wherein the said mixture consists essentially of about 1 to about 30 percent by weight of the compound (ii) and of about 60 to about 99 percent by weight of the compound (i).

7. A composition according to claim 6 wherein the said composition consists essentially of about 3 to about 15 percent by weight of the compound (ii) and of about 85 to about 97 percent by weight of the compound (i).

8. A composition according to claim 1, also containing at least one pharmaceutically acceptable carrier or excipient.

9. A method of treating a disorder selected from rhinitis, cold, flu, cold-like and flu-like symptoms in a human, which comprises administering to a human in need of such therapy, simultaneously or not, an effective amount of pseudoephedrine, an individual optical isomer or a pharmaceutically acceptable salt thereof, and an effective amount of at least one compound selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivatives, an individual optical isomer or a pharmaceutically acceptable salt thereof.

10. A method according to claim 9, wherein administration is effected simultaneously in the form of a pharmaceutical composition according to claim 1.

11. A method according to claim 10, wherein the said effective amount is from about 0.1 to about 6 milligram per kilogram of body weight per day.

12. A pharmaceutical composition according to claim 1, in the form of a dose containing about 15 mg to about 300 mg of the mixture of (i) and (ii).

13. A pharmaceutical composition according to claim 8, in the form of a coated tablet wherein the tablet coating comprises an effective amount of a compound (ii) and the tablet core comprises an effective amount of a compound (i) and a swellable hydrophilic polymer, and wherein the tablet coating and the tablet core further comprise pharmaceutically acceptable carrier materials.

14. A pharmaceutical composition according to claim 8, in the form of a capsule.