Parasiticidal oral veterinary compositions comprising systemically-acting active agents, methods and uses thereof

Abstract

This invention relates to oral veterinary compositions for combating ectoparasites and endoparasites in animals, comprising at least one systemically-acting active agent in combination with a pharmaceutically acceptable carrier. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.

What is claimed is: 
     
         1 . A chewable tablet veterinary composition for treating and/or preventing a parasitic infection or infestation in an animal comprising:
 a) an effective amount of an isoxazoline active agent of the following formula:   
       
         
           
           
               
               
           
         
         
           wherein the asterisk signifies a chiral center; and 
         
         b) a pharmaceutically acceptable carrier that comprises a flavor, filler, a lubricant and a flow aid. 
       
     
     
         2 . The chewable tablet veterinary composition of  claim 1 , wherein the filler is a hydrated lactose. 
     
     
         3 . The chewable tablet veterinary composition of  claim 2 , wherein the filler is lactose monohydrate. 
     
     
         4 . The chewable tablet veterinary composition of  claim 1 , wherein the flavor is a pork flavor. 
     
     
         5 . The chewable tablet veterinary composition of  claim 1 , wherein the lubricant is magnesium stearate. 
     
     
         6 . The chewable tablet veterinary composition of  claim 1 , wherein the flow aid is silicon dioxide. 
     
     
         7 . The chewable tablet veterinary composition of  claim 6 , wherein the silicon dioxide is colloidal silicon dioxide. 
     
     
         8 . The chewable tablet veterinary composition of  claim 1 , wherein:
 i) the flavor is a pork flavor;   ii) the filler is lactose monohydrate;   iii) the lubricant is magnesium stearate; and   iv) the flow aid is colloidal silicon dioxide.   
     
     
         9 . The chewable tablet veterinary composition of claim,  2  or  3 , wherein the filler is present in a concentration of about 5 to about 80% (w/w). 
     
     
         10 . The chewable tablet veterinary composition of  claim 4 , wherein the flavor is present in a concentration of about 5 to about 40% (w/w). 
     
     
         11 . The chewable tablet veterinary composition of  claim 5 , wherein the lubricant is present in a concentration of about 1 to about 20% (w/w). 
     
     
         12 . The chewable tablet veterinary composition of  claim 6 , wherein the flow aid is present in a concentration of about 0.01 to about 25% (w/w). 
     
     
         13 . The chewable tablet veterinary composition of  claim 8  further comprising a disintegrant. 
     
     
         14 . The chewable tablet veterinary composition of  claim 13 , wherein the disintegrant is sodium starch glycolate or corn starch. 
     
     
         15 . The chewable tablet veterinary composition of  claim 1 , wherein the isoxazoline active agent is (R)-1-(5′-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3′H-spiro[azetidine-3,1′-isobenzofuran]-1-yl)-2-(methyl sulfonyl)ethanone. 
     
     
         16 . The chewable tablet veterinary composition of  claim 1 , wherein the isoxazoline active agent is (S)-1-(5′-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3′H-spiro[azetidine-3,1′-isobenzofuran]-1-yl)-2-(methyl sulfonyl)ethanone. 
     
     
         17 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises the isoxazoline active agent at a concentration of about 1% to about 20% by weight. 
     
     
         18 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises the isoxazoline active agent at a concentration of about 1% to about 10% by weight. 
     
     
         19 . The chewable tablet veterinary composition of  claim 1 , wherein the isoxazoline active agent is present at a concentration of about 1% to about 5% by weight. 
     
     
         20 . The chewable tablet veterinary composition of  claim 1 , wherein the isoxazoline active agent is present at a concentration of about 10% to about 20% by weight. 
     
     
         21 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises about 1 mg to about 150 mg of the isoxazoline active agent. 
     
     
         22 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises about 5 mg to about 50 mg of the isoxazoline active agent. 
     
     
         23 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises about 50 mg to about 150 mg of the isoxazoline active agent. 
     
     
         24 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises about 50 mg to about 100 mg of the isoxazoline active agent. 
     
     
         25 . The chewable tablet veterinary composition of  claim 1 , wherein the composition comprises about 75 mg to about 140 mg of the isoxazoline active agent. 
     
     
         26 . The chewable tablet veterinary composition of  claim 17 , wherein the composition provides an efficacy of at least about 95% against ticks for at least about 30 days. 
     
     
         27 . The chewable tablet veterinary composition of  claim 17 , wherein the composition provides an efficacy of at least about 95% against fleas for at least about 30 days. 
     
     
         28 . The chewable tablet veterinary composition of  claim 17 , wherein the composition provides an efficacy of at least about 95% against fleas for at least about 36 days. 
     
     
         29 . The chewable tablet veterinary composition of  claim 17 , wherein the composition provides an efficacy of about 100% against fleas for at least about 30 days. 
     
     
         30 . A method for the treatment and/or prevention of a parasitic infestation and/or infection in an animal comprising administering to the animal an effective amount of the soft chewable veterinary composition of  claim 1  to the animal. 
     
     
         31 . The method of  claim 30 , wherein the parasite are fleas or ticks. 
     
     
         32 . The method of  claim 30 , wherein the animal is a dog. 
     
     
         33 . The method of  claim 30 , wherein the animal is a cat. 
     
     
         34 . The method of  claim 30 , wherein the dose of the isoxazoline active agent is administered at a dose of about 1 to 5 mg per kilogram of bodyweight. 
     
     
         35 . The method of  claim 34 , wherein the composition provides an efficacy of at least about 95% against fleas for at least 30 days. 
     
     
         36 . The method of  claim 34 , wherein the composition provides an efficacy of at least about 95% against fleas for at least 36 days 
     
     
         37 . The method of  claim 34 , wherein the composition provides an efficacy of about 100% against fleas for at least about 30 days. 
     
     
         38 . The method of  claim 34 , wherein the composition provides an efficacy of at least about 95% against ticks for at least about 30 days.