Long-acting spiro-isoxazoline formulations
View Patent ↗The invention describes a long-acting injectable veterinary composition comprising a spirocyclic isoxazoline, at least one biopolymer, and optionally, at least one veterinary acceptable-carrier, -solvent, -excipient, or any mixture thereof. The invention also includes a method of treating an animal with a parasitic infestation by administering the biopolymeric composition to the animal in need thereof, and a process for preparing the biopolymeric composition.
1. A long-acting veterinary injectable microsphere composition wherein the microsphere comprises:
a) a 38% to 63% drug load consisting of (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-(methylsulfonyl)ethanone;
b) and a poly(D,L-lactide-co-glycolide) biopolymer that is 50% polylactide and 50% polyglycolide or 75% polylactide and 25% polyglycolide or a poly(D,L-lactide); and
c) at least one veterinary acceptable-carrier selected from water or triacetin; and optionally, at least one veterinary acceptable excipient, and wherein long-acting is at least 3 to 6 months.
2. The composition of claim 1 wherein the veterinary acceptable carrier is water.
3. The composition of claim 2 wherein the (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-(methylsulfonyl)ethanone is about 20 mg/mL.
4. The composition of claim 1 wherein the composition further comprises at least one veterinary acceptable excipient.
5. The composition of claim 1 , wherein the injectable composition is a subcutaneous injectable composition.
6. The long-acting injectable veterinary microsphere composition of claim 1 , comprising
a poly(D,L-lactide-co-glycolide).
7. The composition of claim 6 wherein the veterinary acceptable carrier is water.
8. The composition of claim 7 , wherein the composition is administered by subcutaneous injection.
9. A method of treating an animal with a parasitic infestation comprising administering a long-acting veterinary injectable microsphere composition wherein the microsphere comprises:
a) a 38% to about 63% drug load consisting of (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-(methylsulfonyl)ethanone;
b) and a poly(D,L-lactide-co-glycolide) biopolymer that is 50% polylactide and 50% polyglycolide or 75% polylactide and 25% polyglycolide or a poly(D,L-lactide);
c) at least one veterinary acceptable carrier selected from water or triacetin; and
d) optionally, at least one veterinary acceptable excipient.
10. The method of claim 9 wherein the veterinary acceptable carrier is water.
11. The method of claim 9 or 10 wherein said animal is a companion animal and the composition is administered by subcutaneous injection.
12. The composition of claim 6 wherein the poly(D,L-lactide-co-glycolide) is 75% polylactide and 25% polyglycolide and the veterinary acceptable carrier is water.
13. The composition of claim 12 wherein the biopolymer is poly(D,L-lactide) and the veterinary acceptable carrier is water.
14. The method of claim 9 wherein the biopolymer is a poly(D,L-lactide-co-glycolide) and the veterinary acceptable carrier is water.
15. The method of claim 14 wherein the composition further comprises a veterinary acceptable excipient.