# US 12,005,053 B2 · Veterinary pharmaceutical compositions for direct systemic introduction > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,005,053 B2 - Document ID: US12005053B2 - Status: Granted - Kind: B2 - Application number: 17/148,236 - Filed: 2021-01-13 - Published: 2021-05-06 - Granted: 2024-06-11 - Earliest claimed: 2012-05-02 - Assignees: NewMarket Pharmaceuticals LLC - Applicants: NewMarket Pharmaceuticals LLC - Inventors: Mark Ridall; David Rock - Web page: https://patentgrep.com/patent/US12005053B2 ## CPC - A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465) - A61K 9/0056: {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} - A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2063: {Proteins, e.g. gelatin} - A61K 9/2095: {Tabletting processes} - A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters - A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin - A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34) - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Veterinary pharmaceutical compositions for direct systemic introduction, also known as DSI pharmaceutical compositions. One veterinary pharmaceutical composition for direct systemic introduction includes about 10-17 dry mass % bovine gelatin; about 10-17 dry mass % mannitol; about 0-1 dry mass % of a surfactant; and about 65-80 dry mass % of the active pharmaceutical ingredient which is a proton pump inhibitor. A method of manufacturing a veterinary pharmaceutical composition for direct systemic introduction includes combining one or more pharmacologically inactive compounds to form a first solution; using one or more surfactants to form a second solution; adding an active pharmaceutical ingredient to the second solution to form a first mixture; adding the first solution to the first mixture to form a pre-formulation; freezing the pre-formulation; and lyophilizing the pre-formulation. ## Claims ### Claim 1 A veterinary pharmaceutical composition for direct systemic introduction, comprising: about 10-17 dry mass % bovine gelatin; about 10-17 dry mass % mannitol; about 0-1 dry mass % of a surfactant; and about 65-80 dry mass % of the active pharmaceutical ingredient which is a proton pump inhibitor; wherein the veterinary pharmaceutical composition further comprises an H2 receptor antagonist. ### Claim 2 (depends on 1) The veterinary pharmaceutical composition according to claim 1, comprising: about 10-13 dry mass % of the bovine gelatin; about 12-15 dry mass % of the mannitol; and about 0.1-0.3 dry mass % of the surfactant. ### Claim 3 (depends on 1) The veterinary pharmaceutical composition according to claim 1, wherein the proton pump inhibitor is omeprazole or esomeprazole. ### Claim 4 (depends on 3) The veterinary pharmaceutical composition according to claim 3, wherein the proton pump inhibitor comprises micronized omeprazole having an average particle diameter of about 1 to about 10 microns. ### Claim 5 (depends on 1) The veterinary pharmaceutical composition according to claim 1, having a disintegration time of 7 seconds or less in deionized water maintained at 37.0° C.±0.5° C. ### Claim 6 (depends on 1) The veterinary pharmaceutical composition according to claim 1, having a disintegration time of 4 seconds or less in deionized water maintained at 37.0° C.±0.5° C. ### Claim 7 (depends on 1) The veterinary pharmaceutical composition according to claim 1, wherein the veterinary pharmaceutical composition further comprises about 0-0.5 dry mass % of a flavorant or sweetener. ### Claim 8 (depends on 1) The veterinary pharmaceutical composition according to claim 1, wherein the veterinary pharmaceutical composition is characterized by a pH adjusted to about 8.3±0.2. ### Claim 9 (depends on 1) The veterinary pharmaceutical composition according to claim 1, wherein the H2 receptor antagonist comprises at least one compound selected from the group consisting of famotidine, cimetidine, ranitidine, and nizatidine. ### Claim 10 A method of manufacturing a veterinary pharmaceutical composition for direct systemic introduction, the method comprising: combining one or more pharmacologically inactive compounds to form a first solution; using one or more surfactants to form a second solution; adding an active pharmaceutical ingredient to the second solution to form a first mixture; adding the first solution to the first mixture to form a pre-formulation; freezing the pre-formulation; and lyophilizing the pre-formulation; wherein the veterinary pharmaceutical composition comprises: about 10-17 dry mass % bovine gelatin; about 10-17 dry mass % mannitol; about 0-1 dry mass % of a surfactant; and about 65-80 dry mass % of the active pharmaceutical ingredient which is a proton pump inhibitor. ### Claim 11 (depends on 10) The method according to claim 10, wherein the method further comprises reducing the pressure surrounding the pre-formulation prior to lyophilizing the pre-formulation. ### Claim 12 (depends on 10) The method according to claim 10, wherein the veterinary pharmaceutical composition further comprises about 0-0.5 dry mass % of a flavorant or sweetener. ### Claim 13 (depends on 10) The method according to claim 10, wherein the first solution comprises at least the bovine gelatin and the mannitol. ### Claim 14 (depends on 10) The method according to claim 10, wherein the second solution comprises at least the surfactant. ### Claim 15 (depends on 10) The method according to claim 10, wherein the method further comprises adjusting the pH of the pre-formulation using Sodium Hydroxide. ### Claim 16 (depends on 15) The method according to claim 15, wherein the pH is adjusted to about 8.3±0.2. ### Claim 17 (depends on 10) The method according to claim 10, wherein the active pharmaceutical ingredient comprises omeprazole or esomeprazole. ### Claim 18 (depends on 10) The method according to claim 10, wherein the active pharmaceutical ingredient comprises micronized omeprazole having an average particle diameter of about 1 to about 10 microns. ### Claim 19 (depends on 10) The method according to claim 10, wherein the veterinary pharmaceutical composition further comprises an H2 receptor antagonist.