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Claims for Patent: 3,933,999

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Claims for Patent: 3,933,999

Title: Organic compounds
Abstract:The invention concerns novel combinations of active agents a) 1-methyl-2-[2-(.alpha.-methyl-p-chlorodiphenylmethyloxy)ethyl]pyrrolidine and b) a non-toxic sympathicomimetic agent having a peripheral vasoconstrictive effect, useful in the treatment of rhinitis.
Inventor(s): Craps; Lucien (Basel, CH)
Assignee: Sandoz Ltd., (Sandoz AG) (Basel, CH)
Application Number:05/425,121
Patent Claims: 1. A pharmaceutical composition useful for the treatment of Rhinitis comprising as active agents

a. 1-methyl-2-[2-(.alpha.-methyl-p-chloro-diphenylmethyloxy)ethyl]pyrrolidine in free base form or in pharmaceutically acceptable acid addition salt form, and b) a compound selected from the group consisting of 2-amino-1-phenylalkan-1-ol of 2 to 4 alkanol carbon atoms, wherein the phenyl is unsubstituted or mono- or disubstituted by hydroxy and the amino is unsubstituted or mono- or disubstituted by alkyl of 1 to 4 carbon atoms and imidazoline substituted in the 2-position by phenylalkyl of 1 to 3 carbon atoms, wherein the weight ratio of active agent a) to active agent b) is from about 1:10 to about 1:60, and a pharmaceutically acceptable carrier therefor.

2. A composition according to claim 1, wherein active agent b) is 2-amino-1-phenylpropanol, 2-methylamino-1-phenylpropanol, 1-(3'-hydroxyphenyl)-2-methylaminoethanol or 1-phenyl-2-diethylaminopropanol.

3. A composition according to claim 1, wherein active agent b) is naphazoline, xylometazoline or tetryzoline.

4. A composition according to claim 1, wherein active agent b) is in retard form with respect to active agent a).

5. A composition according to claim 1, wherein said ratio is from about 1:25 to about 1:50.

6. A composition according to claim 5, wherein said ratio is from about 1:30 to about 1:50.

7. A composition according to claim 1, in unit dosage form having about 1 mg of active agent b) and from about 30 to about 50 mg of active agent b).

8. A composition according to claim 7, having a core containing active agent b) and a layer outside the core containing active agent a).

9. A coated tablet comprising the composition of claim 1 and having a kernel containing active agent b) and a coating surrounding the kernel and containing active agent a).

10. A method of treating Rhinitis in animals, which comprises orally administering to an animal in need of said treatment a anti-histaminic effective amount of active agent a) and active agent b) of the composition of claim 1.

11. The method of claim 10 which comprises orally administering a weight ratio of active agent a) to active agent b) of from 1:10 to 1:60.

12. The method of claim 11, wherein active agent a) is orally administered in an amount of from 0.02 to 0.15 mg. per kg. animal body weight a day.

13. The method of claim 12, wherein active agent a) is orally administered in an amount of from 2 to 6 mg. daily.

14. A composition according to claim 1 wherein active agent b) is 2-amino-1-phenylalkan-1-ol of 2 to 4 alkanol carbon atoms, wherein the phenyl is unsubstituted or mono- or disubstituted by hydroxy and the amino is unsubstituted or mono- or disubstituted by alkyl of 1 to 4 carbon atoms.

15. A composition according to claim 14 wherein active agent b) is 2-amino-1-phenylpropanol.
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