WO2019021191A1 – January 31, 2019 – STARCH-FREE SOFT CHEW FOR VETERINARY APPLICATIONS

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Inventors :

MCDONNELL, Kevin - 3725 Concession Road 1, Lefaivre, Ontario K0B 1J0; ROSSI, Joanna - 1213 des Genevriers, Pincourt, Québec J7W 0A3; ECCLES, Scott - 1025 Ronsard, Deux Montagnes, Québec J7R 6N2; PUCHKAROV, Gueorgui - 3330 rue Lauriault, Saint-Laurent, Québec H4K 1T6

Owner :

TGX SOFT CHEW, LLC

Application Number :

WOIB18055519

Document Number :

WO2019021191A1

Priority Date :

July 26, 2017

Filing Date :

July 24, 2018

Date of Grant/ Publication :

January 31, 2019

Class :

A61K9 / 20

Abstract

The present invention relates to a starch-free soft chew formulation for oral delivery of at least one active ingredient to an animal, and a starch-free soft chew containing the formulation and at least one active ingredient. The starch-free soft chew includes one or more active ingredients and excipients, such as a bulking agent, a flavoring agent, a humectant, a preservative, an antioxidant, and a lubricant, but no added water. In addition, the invention relates to a composition of starch-free, non-water excipients for use in the final dosage form of a soft chew for oral administration of at least one active ingredient to an animal. Also provided are processes for making the starch-free soft chew formulation and the starch-free soft chew.

Claim(s)

1. A starch-free soft chew formulation for oral delivery of at least one active ingredient to an animal.;
2. The soft chew formulation of claim 1 , which comprises a plurality of starch-free excipients.;
3. The soft chew formulation of claim 1, which comprises a plurality of starch -free excipients consisting essentially of non-starch solid excipients and non-water liquid excipients.;
4. The soft chew formulation of claim 2 or 3, wherein the plurality of starch-free excipients include at least two non-starch solid excipients and at least two non-water liquid excipients.;
5. The soft chew formulation of claim 4, wherein the plurality of starch -free excipients comprise at least one filler, a humectant, a solvent, a softening agent, and a lubricant.;
6. The soft chew formulation of claim 5, wherein the plurality of starch-free excipients comprise at least two fillers.;
7. The soft chew formulation of claim 5 or 6, wherein the plurality of starch-free excipients further comprise flavoring.;
8. The soft chew formulation of claim 5 or 6, wherein the plurality of starch-free excipients further comprise a binder.;
9. The soft chew formulation of claim 5 or 6, wherein the plurality of starch-free excipients further comprise a disintegrant.;
10. The soft chew formulation of claim 5 or 6, wherein the plurality of starch-free excipients further comprise a surfactant.;
11. The soft chew formulation of claim 4, wherein the at least two non-starch solid excipients comprise dibasic calcium phosphate and microcrystalline cellulose.;
12. The soft chew formulation of claim 11, wherein the dibasic calcium phosphate is hydrous.;
13. The soft chew formulation of claim 12, wherein the dibasic calcium phosphate is dibasic calcium phosphate dihydrate.;
14. The soft chew formulation of claim 4, wherein the at least two non-starch solid excipients comprise dibasic calcium phosphate, microcrystalline cellulose, and lactose.;
15. The soft chew formulation of claim 14, wherein the lactose is lactose monohydrate.;
16. The soft chew formulation of any one of claims 11-15, wherein the weight ratio of dibasic calcium phosphate to microcrystalline cellulose is about 1 : 1-4: 1.;
17. The soft chew formulation of claim 16, wherein the weight ratio of dibasic calcium phosphate to microcrystalline cellulose is about 2: 1-3: 1.;
18. The soft chew formulation of any one of claims 4 and 11-17, wherein the at least two non-water excipients comprise glycerin and triglycerides of fatty acids with carbon chain lengths of C6- C12.;
19. The soft chew formulation of claim 18, wherein the triglycerides of fatty acids are caprylic/capric triglycerides or medium-chain triglycerides.;
20. The soft chew formulation of claim 18 or 19, wherein the weight ratio of glycerin to the triglycerides of fatty acids is about 4: 1 to 7: 1.;
claim 21: 21. The soft chew formulation of claim 20, wherein the weight ratio of glycerin to the triglycerides of fatty acids is about 5: 1 to 6: 1.;
claim 22: 22. The soft chew formulation of any one of claims 1-21, which comprises croscarmellose sodium.;
claim 23: 23. The soft chew formulation of any one of claims 1-22, which comprises magnesium stearate, stearic acid, or sodium stearyl fumarate.;
claim 24: 24. The soft chew formulation of any one of claims 1-23, which comprises citric acid.;
claim 25: 25. The soft chew formulation of claim 24, wherein the citric acid is citric acid anhydrous.;
claim 26: 26. The soft chew formulation of any one of claims 1-25, which comprises potassium sorbate.;
claim 27: 27. The soft chew formulation of any one of claims 1-26, which comprises a-tocopherol.;
claim 28: 28. The soft chew formulation of claim 27, wherein the a-tocopherol is DL-a-tocopheryl acetate.;
claim 29: 29. The soft chew formulation of any one of claims 1-28, which comprises povidone, hydroxyl propyl cellulose, or hydroxyl methyl cellulose.;
claim 30: 30. The soft chew formulation of any one of claims 2-4, wherein the plurality of starch-free excipients include dibasic calcium phosphate dihydrate, microcrystalline cellulose, glycerin, and medium-chain triglycerides.;
claim 31: 31. The soft chew formulation of claim 30, wherein the weight ratio of dibasic calcium phosphate dihydrate to microcrystalline cellulose is about 2: 1 to about 3: 1.;
claim 32: 32. The soft chew formulation of claim 30 or 31 , wherein the weight ratio of glycerin to medium-chain triglycerides is about 5: 1 to 6: 1.;
claim 33: 33. The soft chew formulation of any one of claims 1-32, wherein the plurality of starch-free excipients further comprise flavoring.;
claim 34: 34. The soft chew formulation of any one of claims 2-4, which comprises: dibasic calcium phosphate dihydrate; microcrystalline cellulose; flavoring; croscarmellose sodium; glycerin; medium-chain triglycerides; and magnesium stearate or sodium stearyl fumarate.;
claim 35: 35. The soft chew formulation of claim 34, which comprises dibasic calcium phosphate dihydrate, microcrystalline cellulose, flavoring, croscarmellose sodium, glycerin, medium-chain triglycerides, and magnesium stearate in a weight ratio of about 25:8:30:5:25:5:2.;
claim 36: 36. The soft chew formulation of claim 34, which comprises dibasic calcium phosphate dihydrate, microcrystalline cellulose, flavoring, croscarmellose sodium, glycerin, medium-chain triglycerides, and magnesium stearate in a weight ratio of about 30: 10:23:5:25:5:2.;
claim 37: 37. The soft chew formulation of any one of claims 34-36, which further comprises: citric acid anhydrous; potassium sorbate; and DL-a-tocopheryl acetate.;
claim 38: 38. A starch-free soft chew for oral delivery of at least one active ingredient to an animal, comprising the soft chew formulation of any one of claims 1 -37 and at least one active ingredient.;
claim 39: 39. The soft chew of claim 38, wherein the at least one active ingredient includes an active pharmaceutical ingredient.;
claim 40: 40. The soft chew of claim 39, wherein the active pharmaceutical ingredient is an antiparasitic.;
claim 41: 41. The soft chew of claim 40, wherein the active pharmaceutical ingredient is an anthelmintic.;
claim 42: 42. The soft chew of claim 41, wherein the active pharmaceutical ingredient is milbemycin oxime, ivermectin, moxidectin, abamectin, selamectin, pyrantel, febantel, fenbendazole, oxibendazole, emodepside, piperazine, mebendazole, levamisole, praziquantel, or oxantel.;
claim 43: 43. The soft chew of claim 42, wherein the active pharmaceutical ingredient is milbemycin oxime, praziquantel, ivermectin, or pyrantel.;
claim 44: 44. The soft chew of any one of claims 39-43, wherein the at least one active ingredient further includes a second active pharmaceutical ingredient.;
claim 45: 45. The soft chew of claim 44, wherein the second active pharmaceutical ingredient is an antiparasitic.;
claim 46: 46. The soft chew of claim 45, wherein the second active pharmaceutical ingredient is an anthelmintic.;
claim 47: 47. The soft chew of any one of claims 44-46, wherein the at least one active ingredient includes: milbemycin oxime or ivermectin; and praziquantel or pyrantel.;
claim 48: 48. The soft chew of claim 47, wherein the at least one active ingredient includes milbemycin oxime and praziquantel.;
claim 49: 49. The soft chew of claim 47, wherein the at least one active ingredient includes ivermectin and pyrantel.;
claim 50: 50. The soft chew of claim 49, wherein the pyrantel is pyrantel pamoate.;
claim 51: 51. The soft chew of claim 38, wherein the at least one active ingredient is moisture – sensitive.;
claim 52: 52. The soft chew of claim 51 , wherein the at least one active ingredient includes clavulanic acid, nitenpyram, milbemycin oxime, or ivermectin.;
claim 53: 53. The soft chew of claim 41, wherein the active pharmaceutical ingredient is moisture – sensitive.;
claim 54: 54. The soft chew of claim 53, wherein the active pharmaceutical ingredient is milbemycin oxime or ivermectin.;
claim 55: 55. The soft chew of claim 38, wherein the at least one active ingredient includes a cannabinoid.;
claim 56: 56. The soft chew of claim 55, wherein the cannabinoid is a phytocannabinoid or a synthetic cannabinoid.;
claim 57: 57. The soft chew of claim 56, wherein the cannabinoid is tetrahydrocannabinol, cannabidiol, cannabinol, cannabichromene, cannabigerol, 2-arachidonoylglycerol, or anandamide.;
claim 58: 58. The soft chew of claim 38, wherein the at least one active ingredient includes an active nutritional ingredient.;
claim 59: 59. The soft chew of claim 58, wherein the active nutritional ingredient is glucosamine, enzymes, fish oils, or herbal ingredients.;
claim 60: 60. The soft chew of any one of claims 38-57, wherein the soft chew formulation comprises: 15-90% w/w dibasic calcium phosphate dihydrate; 5-30% w/w flavoring; 5-40% w/w microcrystalline cellulose; 0-15% w/w croscarmellose sodium; 0-5% w/w sodium stearyl fumarate or magnesium stearate; 15-50% w/w glycerin; 15-50% w/w medium-chain triglycerides; 0-5% w/w citric acid anhydrous; 0.01-3% w/w potassium sorbate; and 0.01-3% w/w DL-a-tocopheryl acetate.;
claim 61: 61. The soft chew of any one of claims 38-57, wherein the soft chew formulation comprises: 10-60% w/w dibasic calcium phosphate dihydrate; 5-35% w/w flavoring; 5-40% w/w microcrystalline cellulose; 0-15% w/w croscarmellose sodium; 0-5% w/w sodium stearyl fumarate or magnesium stearate; 15-50% w/w glycerin; 2-20% w/w medium-chain triglycerides; 0-5% w/w citric acid anhydrous; 0.01-3% w/w potassium sorbate; and 0.01-3% w/w DL-a-tocopheryl acetate.;
claim 62: 62. The soft chew formulation of any one of claims 1-37, or the soft chew of any one of claims 38-61, which is made without adding water as an excipient.;
claim 63: 63. A composition of starch-free, non-water excipients for use in the final dosage form of a soft chew for oral administration of at least one active ingredient to an animal, said composition consisting essentially of non-starch solid excipients and non-water liquid excipients, said starch-free, non-water excipients comprising: dibasic calcium phosphate; microcrystalline cellulose; glycerin; and triglycerides of fatty acids with carbon chain lengths of C6-C12.;
claim 64: 64. The composition of claim 63, wherein the dibasic calcium phosphate is dibasic calcium phosphate hydrous.;
claim 65: 65. The composition of claim 64, wherein the dibasic calcium phosphate is dibasic calcium phosphate dihydrate.;
claim 66: 66. The composition of any one of claims 63-65, wherein the weight ratio of dibasic calcium phosphate to microcrystalline cellulose is about 1 : 1 to about 4: 1.;
claim 67: 67. The composition of any one of claims 63-65, wherein the weight ratio of dibasic calcium phosphate to microcrystalline cellulose is about 2: 1 to about 3: 1.;
claim 68: 68. The composition of any one of claims 63-67, wherein the triglycerides of fatty acids are caprylic triglycerides, capric triglycerides, or a mixture thereof.;
claim 69: 69. The composition of any one of claims 63-67, wherein the triglycerides of fatty acids are medium chain triglycerides.;
claim 70: 70. The composition of any one of claims 63-69, wherein the weight ratio of glycerin to the triglycerides of fatty acids is about 4: 1 to 7: 1.;
claim 71: 71. The composition of any one of claims 63-69, wherein the weight ratio of glycerin to the triglycerides of fatty acids is about 5: 1 to 6: 1.;
claim 72: 72. The composition of any one of claims 63-71, wherein the starch-free, non-water excipients further comprise a filler.;
claim 73: 73. The composition of claim 72, wherein the filler is lactose.;
claim 74: 74. The composition of claim 73, wherein the lactose is lactose monohydrate.;
claim 75: 75. The composition of any one of claims 63-74, wherein the starch-free, non-water excipients further comprise a flavoring agent.;
claim 76: 76. The composition of any one of claims 63-75, wherein the starch-free, non-water excipients further comprise a disintegrant.;
claim 77: 77. The composition of claim 76, wherein the disintegrant is croscarmellose sodium.;
claim 78: 78. The composition of any one of claims 63-77, wherein the starch-free, non-water excipients further comprise a lubricant.;
claim 79: 79. The composition of claim 78, wherein the lubricant is magnesium stearate, stearic acid, or sodium stearyl fumarate.;
claim 80: 80. The composition of any one of claims 63-79, wherein the starch-free, non-water excipients further comprise a preservative.;
claim 81: 81. The composition of claim 80, wherein the preservative is citric acid or potassium sorbate.;
claim 82: 82. The composition of any one of claims 63-81, wherein the starch-free, non-water excipients further comprise an antioxidant.;
claim 83: 83. The composition of claim 82, wherein the antioxidant is citric acid or a-tocopherol.;
claim 84: 84. The composition of claim 81 or 83, wherein citric acid is a citric acid anhydrous.;
claim 85: 85. The composition of claim 83, wherein the a-tocopherol is DL-a-tocopheryl acetate.;
claim 86: 86. The composition of any one of claims 63-85, wherein the starch-free, non-water excipients further comprise a binder.;
claim 87: 87. The composition of claim 86, wherein the binder is povidone.;
claim 88: 88. The composition of claim 87, wherein the povidone is povidone K30.;
claim 89: 89. The composition of any one of claims 63-88, wherein the at least one active ingredient includes at least one active pharmaceutical ingredient or at least one active nutritional ingredient.;
claim 90: 90. The composition of any one of claims 63-89, wherein the at least one active ingredient includes an active pharmaceutical ingredient.;
claim 91: 91. The composition of claim 90, wherein the active pharmaceutical ingredient is an antiparasitic.;
claim 92: 92. The composition of claim 91, wherein the active pharmaceutical ingredient is an anthelmintic.;
claim 93: 93. The composition of claim 90, wherein the active pharmaceutical ingredient is a cannabinoid.;
claim 94: 94. The composition of any one of claims 63-89, wherein the at least one active ingredient includes an active nutritional ingredient.;
claim 95: 95. A process for making a starch -free soft chew for oral delivery of at least one active ingredient to an animal, said process comprising the steps of: a) dry-mixing at least two non-starch dry excipients in a mixer; and b) mixing the dry excipients into a dough-like material by adding into the mixer at least two non-water liquid excipients.;
claim 96: 96. The process of claim 95, further comprising the step of: c) forming the dough-like material into ribbon.;
claim 97: 97. The process of claim 96, further comprising the step of: d) portioning the ribbon into soft chew portions.;
claim 98: 98. The process of claim 97, further comprising the step of: e) packaging the soft chew portions.;
claim 99: 99. The process of any one of claims 95-98, further comprising the step of dry-mixing the at least one active ingredient with the starch-free dry excipients.;
claim 100: 100. The process of any one of claims 95-99, wherein step b) is performed by adding into the mixer the at least two non-water liquid excipients in a sequential manner.;
claim 101: 101. The process of claim 100, wherein the at least two non-water liquid excipients comprise a humectant and a solvent.;
claim 102: 102. The process of claim 101, wherein the humectant is glycerin and the solvent is medium chain triglycerides.;
claim 103: 103. The process of claim 101 or 102, wherein the humectant is added into the mixer first and the solvent is added into the mixer thereafter.;
claim 104: 104. The process of any one of claims 95-103, further comprising the step of mixing the at least one active ingredient with one of the non-water liquid excipients.;
claim 105: 105. The process of any one of claims 101-103, wherein the at least one active ingredient is mixed with the solvent.;
claim 106: 106. The process of claim 95, wherein the mixer is a low-shear mixer.;
claim 107: 107. The process of claim 95, wherein the mixer is a high-shear mixer.;
claim 108: 108. The process of claim 97, wherein the portioning step is carried out using a portioning tool.;
claim 109: 109. The process of any one of claims 95-108, where the process is carried out under ambient room-temperature conditions.

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