Pharmaceutical Composition Containing An N-Phenylpyrazole Derivative, And Use Thereof For Preparing A Topical Veterinary For Flea Control

• US 20120029043A1
• Filed: 12/15/2008
• Published: 02/02/2012
• Est. Priority Date: 12/16/2008
• Status: Active Grant

• Current Assignee: Virbac
• Original Assignee: Virbac
• Inventors: Derrieu, Guy
• Granted Patent: US 8,501,799 B2
• Time in Patent Office: Days
• US Class Current: 514/407
• CPC Class Codes: A01N 2300/00 Combinations or mixtures of active ingredients covered by classes A01N27/00 - A01N65/48 with other active or formulation relevant ingredients, e.g. specific carrier materials or surfactants, covered by classes A01N25/00 - A01N65/48
• CPC Class Codes: A01N 25/02 containing liquids as carriers, diluents or solvents
• CPC Class Codes: A01N 47/02 the carbon atom having no bond to a nitrogen atom
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 33/14 Ectoparasiticides, e.g. scabicides

Abstract

The invention relates to a liquid pharmaceutical composition that contains an N-phenylpyrazole derivative as an active principle, benzyl alcohol, and an appropriately selected organic solvent, and to the use of such a composition for preparing a topically applied antiparasitic veterinary drug for preventing and/or treating flea infestation in pets, in particular in dogs and cats.

Claims

1. A liquid pharmaceutical composition, comprising:

as active principle, 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-(trifluoromethylsulfinyl)-1H-pyrazole-3-carbonitrile (fipronil),

at least 5% (weight/volume) of benzyl alcohol, and

at least 50% (weight/volume) of an organic solvent chosen from propylene glycol monomethyl ether, dipropylene glycol n-butyl ether, ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, diethylene glycol monoethyl ether and propylene glycol, and mixtures thereof,

it being understood that said composition is free of C₁-C₄ alcohol.

2. The composition as claimed in claim 1, wherein the fipronil represents from 1% to 20% (weight/volume).

3. The composition as claimed in claim 2, wherein the fipronil represents from 5% to 15% (weight/volume).

4. The composition as claimed in claim 1, wherein the benzyl alcohol represents from 25% to 35% (weight/volume).

5. The composition as claimed in claim 1, wherein the organic solvent is diethylene glycol monoethyl ether.

6. The composition as claimed in claim 1, wherein it the composition also contains one or more excipients chosen from surfactants, thickeners, dyes, fragrances and antioxidants.

7. The composition as claimed in claim 6, wherein the antioxidants are chosen from butylhydroxyanisole, butylhydroxytoluene, propyl gallate, ascorbyl palmitate and rosemary extracts, and mixtures thereof.

8. The composition as claimed in claim 6, wherein, when they are present, the antioxidant(s) represent from 0.005% to 2% (weight/volume).

9. The composition as claimed in claim 1, wherein it the composition comprises one or more additional antiparasitic active principles.

10. The composition as claimed in claim 9, wherein the additional antiparasitic active principles are chosen from acaricides, flea and tick growth inhibitors, endoparasiticides and active principles against pet ectoparasites and sand flies.

11. The use of a liquid pharmaceutical composition as described in claim 1, for the preparation of an antiparasitic veterinary medicament for topical use for the prevention and/or treatment of pet flea infestations.

12. The use as claimed in claim 11, wherein said medicament is intended for cats or dogs.

13. The use as claimed in claim 11, wherein said medicament is intended to be administered in an amount ranging from 0.3 to 1.5 ml to cats.

14. The use as claimed in claim 11, wherein said medicament is intended to be administered in an amount ranging from 0.3 to 6 ml to dogs.

15. The use as claimed in claim 11, wherein said medicament is intended for administering a unit dose of fipronil ranging from 5 to 15 mg per kg of body weight.

16. A method for the prevention and/or treatment of pet flea infestations comprising topically applying a liquid pharmaceutical composition as described in claim 1 to an animal in need thereof.

17. The method of claim 16, wherein the animal is a cat or a dog.

18. The method of claim 16, wherein said pharmaceutical composition is administered in an amount ranging from 0.3 to 1.5 ml to cats.

19. The method of claim 16, wherein said pharmaceutical composition is administered in an amount ranging from 0.3 to 6 ml to dogs.

20. The method of claim 16, wherein said pharmaceutical composition is administered in a unit dose of fipronil ranging from 5 to 15 mg per kg of body weight.