Details for Patent: 6,469,009
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Title: | Pharmaceutical compositions for the treatment of rhinitis |
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. |
Inventor(s): | Van De Venne; Herman (Lasne, BE), Martin; Jean-Pierre (Montigny-le-Tilleul, BE) |
Assignee: | UCB, S.A. (Brussels, BE) |
Filing Date: | Apr 08, 1996 |
Application Number: | 08/629,144 |
Claims: | 1. A pharmaceutical composition which comprises 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. 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 ##STR3## wherein Y is a hydroxyl group or an --NH.sub.2 group, X and X' represent independently a hydrogen atom, a halogen atom, a straight or branched chain lower alkoxy radical or a trifluoromethyl radical, m is 1 or 2, and n is 1 or 2. 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: 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or its dihydrochloride; potassium 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetate; 2-[2-[4-(diphenylmethyl)-1-piperazinyl]ethoxy]-acetic acid or its dihydrochloride; 2-[2-[4-[(4-fluorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or its hydrate; 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]-acetic acid; 2-[2-[4-(diphenylmethyl)-1-piperazinyl]ethoxy]-acetamide or its dihydrochloride; 2-[2-[4-[(2-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetamide or its dihydrochloride; 2-[2-[2-[4-[(4-methoxyphenyl)phenylmethyl]-1-piperazinyl]ethoxy]ethoxy]-ace tamide or its dihydrochloride; 2-[2-[2-[2-[4-(diphenylmethyl)-1-piperazinyl]ethoxy]ethoxy]-acetamide or its dihydrochloride; 2-[2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ethoxy]-acet amide or its dihydrochloride; 2-[2-[2-[4-(diphenylmethyl)-1-piperazinyl]ethoxy]ethoxy]-acetic acid or its dihydrochloride; and 2-[2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ethoxy]-acet ic acid or its dihydrochloride. 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. |