# US 8,784,884 B2 · Pancreatic enzyme compositions and methods for treating pancreatitis and pancreatic insufficiency > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,784,884 B2 - Document ID: US8784884B2 - Status: Granted - Kind: B2 - Application number: 12/568,064 - Filed: 2009-09-28 - Published: 2011-03-17 - Granted: 2014-07-22 - Earliest claimed: 2009-09-17 - Applicants: Stephen Perrett; Ruth Thieroff-Ekerdt; Gopi Venkatesh; Konstantinos Efthymiopoulos - Inventors: Stephen Perrett; Ruth Thieroff-Ekerdt; Gopi Venkatesh; Konstantinos Efthymiopoulos - Web page: https://patentgrep.com/patent/US8784884B2 ## CPC - A61K 9/16: Agglomerates; Granulates; Microbeadlets {; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction (A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51)} - A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)} - A61K 9/5084: {Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs (tablets containing such a mixture A61K9/2077)} - A61K 38/465: {acting on ester bonds (3.1), e.g. lipases, ribonucleases} - A61K 38/48: acting on peptide bonds (3.4) - A61P 1/14: Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents - A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes - A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48) - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61K 9/2813: {Inorganic compounds} - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - 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 Compositions of the present invention, comprising the combination of enterically coated and uncoated pancreatic enzyme-containing beads are useful for treating or preventing pancreatitis pain, and optionally disorders associated with digestive enzyme deficiencies. ## Claims ### Claim 1 A multi-particulate digestive enzyme composition consisting essentially of coated digestive enzyme-containing beads, and uncoated digestive enzyme-containing beads, wherein: the enterically coated digestive enzyme-containing beads comprise a core and an enteric coating disposed over the core, wherein the core comprises a therapeutically effective amount of digestive enzymes, and the enteric coating comprises an enteric polymer; and the uncoated digestive enzyme-containing beads comprise a therapeutically effective amount of digestive enzymes, and is substantially free of an enteric polymer coating; wherein the digestive enzymes comprise lipase and protease, and the ratio of lipase and protease activities in the enterically coated digestive enzyme-containing beads to the lipase and protease activities in the uncoated digestive enzyme-containing beads ranges from about 5:95 to about 50:50. ### Claim 2 (depends on 1) The multi-particulate digestive enzyme composition of claim 1, wherein the digestive enzymes comprise lipase and protease, and the ratio of lipase and protease activities in the enterically coated digestive enzyme-containing beads to the lipase and protease activities in the uncoated digestive enzyme-containing beads ranges from about 5:95 to about 25:75. ### Claim 3 (depends on 1) The multi-particulate digestive enzyme composition of claim 1, wherein the digestive enzymes comprise lipase and protease, and each of the enterically coated and uncoated digestive enzyme-containing beads have substantially the same protease and lipase activity. ### Claim 4 (depends on 1) A dosage form comprising the multi-particulate digestive enzyme composition of claim 1. ### Claim 5 (depends on 4) The dosage form of claim 4, wherein the enterically coated digestive enzyme-containing beads have a total lipase activity ranging from about 2000 USP lipase units to about 10,000 USP lipase units. ### Claim 6 (depends on 4) The dosage form of claim 4, wherein the enterically coated digestive enzyme-containing beads have a total protease activity ranging from about 6800 USP protease units to about 34,000 USP protease units. ### Claim 7 (depends on 5) The dosage form of claim 5, wherein the enterically coated digestive enzyme-containing beads have a total protease activity ranging from about 6800 USP protease units to about 34,000 USP protease units. ### Claim 8 (depends on 4) The dosage form of claim 4, wherein the uncoated digestive enzyme-containing beads have a total lipase activity ranging from about 10,000 USP lipase units to about 18,000 USP lipase units. ### Claim 9 (depends on 4) The dosage form of claim 4, wherein the uncoated digestive enzyme-containing beads have a total protease activity ranging from about 34,000 USP protease units to about 62,000 USP protease units. ### Claim 10 (depends on 8) The dosage form of claim 8, wherein the uncoated digestive enzyme-containing beads have a total protease activity ranging from about 34,000 USP protease units to about 62,000 USP protease units. ### Claim 11 (depends on 4) The dosage form of claim 4, wherein the enterically coated digestive enzyme-containing beads have a total lipase activity ranging from about 2000 USP lipase units to about 4,000 USP lipase units. ### Claim 12 (depends on 4) The dosage form of claim 4, wherein the enterically coated digestive enzyme-containing beads have a total protease activity ranging from about 6800 USP protease units to about 13,600 USP protease units. ### Claim 13 (depends on 11) The dosage form of claim 11, wherein the enterically coated digestive enzyme-containing beads have a total protease activity ranging from about 6800 USP protease units to about 13,600 USP protease units. ### Claim 14 (depends on 4) The dosage form of claim 4, wherein the uncoated digestive enzyme-containing beads have a total lipase activity ranging from about 14,000 USP lipase units to about 18,000 USP lipase units. ### Claim 15 (depends on 4) The dosage form of claim 4, wherein the uncoated digestive enzyme-containing beads have a total protease activity ranging from about 47,000 USP protease units to about 62,000 USP protease units. ### Claim 16 (depends on 14) The dosage form of claim 14, wherein the uncoated digestive enzyme-containing beads have a total protease activity ranging from about 47,000 USP protease units to about 62,000 USP protease units. ### Claim 17 (depends on 4) The dosage form of claim 4, in the form of a capsule filled with the multi-particulate digestive enzyme composition. ### Claim 18 (depends on 1) A method of treating pancreatitis pain, comprising administering the composition of claim 1 to a patient in need thereof. ### Claim 19 (depends on 1) A method of treating pancreatitis pain and pancreatic insufficiency, comprising administering the composition of claim 1 to a patient in need thereof. ### Claim 20 (depends on 19) The method of claim 19, wherein said administering comprises administering, per meal, an amount of multi-particulate digestive enzyme composition such that the lipase activity of the enterically coated digestive enzyme-containing beads ranges from about 8000 to about 40,000 USP lipase units, and the lipase activity of the uncoated digestive enzyme-containing beads ranges from about 40,000 to about 72,000 USP lipase units. ### Claim 21 (depends on 1) A method of treating pancreatic exocrine insufficiency, comprising administering to a patient in need thereof a therapeutically effective dose of an enterically coated digestive enzyme composition of claim 1, wherein said dose ranges from about 100 to about 300 USP lipase units/kg/meal. ### Claim 22 (depends on 21) The method of claim 21, wherein the daily dose of said enterically coated digestive enzyme ranges from about 35,000 to about 90,000 USP lipase units. ### Claim 23 (depends on 21) The method of claim 21, wherein said the enterically coated digestive enzyme is in the form of a capsule comprising enterically coated digestive enzyme-containing beads; wherein the enterically coated digestive enzyme-containing beads comprise a core and an enteric coating disposed over the core, wherein the core comprises a therapeutically effective amount of one or more digestive enzymes, and the enteric coating comprises an enteric polymer.