Palatable formulations

Patent metadata

Field	Value
Publication number	US-12544336-B2
Application number	US-202118043743-A
Country	US
Kind code	B2
Filing date	Sep 2, 2021
Priority date	Sep 4, 2020
Publication date	Feb 10, 2026
Grant date	Feb 10, 2026

Abstract

Palatable oral dosage formulations are provided including an effective amount of an isoxazoline parasiticidal agent, an avermectin, and a pyrazinoisoquinoline, and optionally one or more additional active ingredients, such as a tetrahydropyrimidine.

First claim

What is claimed is:

1 . A palatable veterinary dosage form comprising an isoxazoline class parasiticide selected from the group consisting of lotilaner, sarolaner, afoxolaner, and fluralaner;
and a first granulate comprising granules, wherein the granules of the first granulate comprise a macrocyclic lactone class parasiticide; and a pyrazinoisoquinoline class parasiticide, wherein the pyrazinoisoquinoline class parasiticide comprises praziquantel, and the macrocyclic lactone class parasiticide comprises moxidectin.

2 . The palatable veterinary dosage form of claim 1 , further comprising a tetrahydropyrimidine class parasiticide.

3 . The palatable veterinary dosage form of claim 1 , wherein the first granulate comprises physiologically acceptable polymer matrix-coated granules.

4 . The palatable veterinary dosage form of claim 1 , wherein the palatable veterinary dosage form is a hard chewable tablet.

5 . The palatable veterinary dosage form of claim 1 , wherein the palatable veterinary dosage form disintegrates in less than or equal to 15 minutes in water at 37° C., as determined by the disintegration method 2.9.1 (Test A and B) of the European Pharmacopoeia 8.0.

6 . The palatable veterinary dosage form of claim 1 , wherein the palatable veterinary dosage form has a friability of 1% or less as measured according to USP <1216>.

7 . The palatable veterinary dosage form of claim 1 , comprising 20-40% (wt/wt) lotilaner, 0.020% to 0.045% (wt/wt) moxidectin, and 5-10% (wt/wt) praziquantel, based on total weight of the dosage form.

8 . The palatable veterinary dosage form of claim 1 , further comprising at least one of a diluent; an antioxidant; a disintegrant; a wetting agent; a binder; a taste-masking polymer; a plasticizer; a flavoring agent; a glidant; or a lubricant.

9 . The palatable veterinary dosage form of claim 8 , comprising microcrystalline cellulose; lactose monohydrate; butylated hydroxytoluene; croscarmellose sodium; sodium lauryl sulfate; polyvinylpyrrolidone K30; ammonia methacrylate copolymer type A; a 20% aqueous emulsion comprising glycerol monostearate, triethyl citrate, and polysorbate 80; a flavorant; colloidal silicon dioxide; and magnesium stearate.

10 . The palatable veterinary dosage form of claim 9 , comprising 25% to 30% (wt/wt) microcrystalline cellulose; 3% to 6% (wt/wt) lactose monohydrate; 0.05% to 0.06% (wt/wt) butylated hydroxytoluene; 3% to 5% (wt/wt) croscarmellose sodium; 0.4% to 0.6% (wt/wt) sodium lauryl sulfate; 1% to 3% (wt/wt) polyvinylpyrrolidone; 1% to 2% (wt/wt) ammonia methacrylate copolymer type A; 0.1% to 0.5% (wt/wt) 20% aqueous emulsion comprising glycerol monostearate, triethyl citrate, and polysorbate 80; 5% to 20% of a flavorant; 0.5% to 1.5% (wt/wt) colloidal silicon dioxide; and 0.5% to 1.5% (wt/wt) magnesium stearate.

11 . The palatable veterinary dosage form of claim 1 , produced by a process comprising providing a first granulate comprising praziquantel and moxidectin; optionally coating the first granulate with a physiologically acceptable polymer matrix optionally a polymethacrylate-based copolymer matrix to provide a coated first granulate; providing a second granulate comprising the isoxazoline class parasiticide; combining the first granulate or coated first granulate with the second granulate and at least one pharmaceutically acceptable excipient to provide a final blend; and compressing a ready-to-press mixture into a tablet.

12 . The palatable veterinary dosage form of claim 11 , wherein the first granulate or coated first granulate comprises praziquantel, moxidectin, a diluent, an antioxidant, a disintegrant, a wetting agent, and a binder; the physiologically acceptable polymer matrix comprises a polymethacrylate-based copolymer; the second granulate comprises lotilaner, a diluent, a wetting agent, a disintegrant, and a binder; and the at least one pharmaceutically acceptable excipient comprises a diluent, a flavoring agent, a disintegrant, a glidant, and a lubricant.

13 . The palatable veterinary dosage form of claim 12 , wherein the first granulate or coated first granulate comprises praziquantel, moxidectin, lactose monohydrate, microcrystalline cellulose, butylated hydroxytoluene, croscarmellose sodium, sodium lauryl sulfate, and polyvinylpyrrolidone; the physiologically acceptable polymer matrix comprises ammonia methacrylate copolymer type A and a 20% aqueous emulsion comprising glycerol monostearate, triethyl citrate, and polysorbate 80; the second granulate comprises lotilaner, microcrystalline cellulose, sodium lauryl sulfate, croscarmellose sodium, and polyvinylpyrrolidone; and the at least one pharmaceutically acceptable excipient comprises microcrystalline cellulose, a flavoring agent, croscarmellose sodium, colloidal silicone dioxide, and magnesium stearate.

14 . The palatable veterinary dosage form of claim 1 , wherein the first granulate is formed by co-granulating the macrocyclic lactone class parasiticide and the pyrazinoisoquinoline.

15 . The palatable veterinary dosage form of claim 1 , comprising a second granulate, the second granulate comprising the isoxazoline class parasiticide.

16 . The palatable veterinary dosage form of claim 15 , wherein the second granulate further comprises the tetrahydropyramidine class parasiticide.

17 . The palatable veterinary dosage form of claim 16 , wherein the tetrahydropyramidine class parasiticide is pyrantel.

Assignees

• Elanco Us Inc

Inventors

• Patil Rajesh

Classifications

• A61K31/4985

  Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K31/422

  not condensed and containing further heterocyclic rings · CPC title

• A61K31/365

  Lactones · CPC title

• A61K9/0056

  Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals · CPC title

• A61K2300/00

  Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00 · CPC title