# US 6,720,002 B2 · Antihistamine formulations for soft capsule dosage forms > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 6,720,002 B2 - Document ID: US6720002B2 - Status: Granted - Kind: B2 - Application number: 09/909,313 - Filed: 2001-07-20 - Published: 2003-05-08 - Granted: 2004-04-13 - Earliest claimed: 2001-07-20 - Assignees: R.P. Scherer Technologies, LLC - Inventors: Jing Lin; Hung Truong - Web page: https://patentgrep.com/patent/US6720002B2 ## CPC - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - 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 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine - A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection - 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 The invention herein relates to a pharmaceutical composition containing loratadine and derivatives thereof which is suitable for use in soft capsule dosage forms. A pharmaceutical composition according to the invention comprises loratadine and derivatives thereof in a pharmaceutically effective amount; and a solvent system comprising a mixture of medium chain fatty acids. The loratadine compositions exhibit good solubility and storage stability while maintaining bioavailability of the drug. The compositions also permit high concentrations of solubilized loratadine per total fill volume and thereby permit the use of smaller capsules to deliver the same dosage of drug. ## Claims ### Claim 1 A pharmaceutical composition for use in soft capsule dosage forms comprising: a) loratadine and derivatives thereof in a pharmaceutically effective amount; and b) a solvent system comprising a mixture of medium chain fatty acids; wherein said loratadine and derivatives thereof is present in an amount of about 6.3% by weight of the total composition. ### Claim 2 A pharmaceutical composition for use in soft capsule dosage forms comprising: a) loratadine and derivatives thereof in a pharmaceutically effective amount; and b) a solvent system comprising a mixture of medium chain fatty acids; wherein the mixture of medium chain fatty acids is present in an amount of about 89.0% by weight or less of the total composition; and wherein said loratadine and derivatives thereof is present in an amount of about 6.3% by weight of the total composition. ### Claim 3 A pharmaceutical composition for use in soft capsule dosage forms comprising: a) loratadine and derivatives thereof in a pharmaceutically effective amount; and b) a solvent system comprising a mixture of medium chain fatty acids; and further comprising a dispersant; and wherein said loratadine and derivatives thereof is present in an amount of about 6.3% by weight of the total composition. ### Claim 4 (depends on 1) The composition of claim 1 wherein said loratadine derivatives are decarbalkoxylated forms of loratadine. ### Claim 5 (depends on 4) The composition of claim 4 wherein the decarbalkoxylated loratadine derivative is descarboethoxyloratadine. ### Claim 6 (depends on 1) The composition of claim 1 wherein said loratadine and derivatives thereof is present in an amount of less than 6.3% of the total composition. ### Claim 7 (depends on 1) The composition of claim 1 wherein said mixture of medium chain fatty acids is a mixture of mono- and diglycerides of medium chain fatty acids. ### Claim 8 (depends on 7) The composition of claim 7 wherein said mixture of mono- and diglycerides of medium chain fatty acids comprises a mixture of caprylic acid and capric acid. ### Claim 9 (depends on 2) The composition of claim 2 wherein the mixture of medium chain fatty acids is present in an amount of from about 89.0% to about 80.0% by weight of the total composition. ### Claim 10 (depends on 3) The composition of claim 3 wherein the dispersant is present in an amount of about 8.0% by weight or less of the total fill composition. ### Claim 11 (depends on 10) The composition of claim 10 wherein the dispersant is present in an amount ranging from about 7.5% to about 7.0% by weight of the total composition. ### Claim 12 (depends on 10) The composition of claim 10 wherein the dispersant comprises povidone and polyoxyethylene sorbitan fatty acid ester. ### Claim 13 (depends on 12) The composition of claim 12 wherein the povidone to polyoxyethylene sorbitan fatty acid ester ratio is from about 10:1 to about 15:1. ### Claim 14 (depends on 13) The composition of claim 13 wherein the ratio of povidone to polyoxyethylene sorbitan fatty acid ester is about 10:1. ### Claim 15 (depends on 1) The composition of claim 1 wherein said soft capsule dosage form is a soft gelatin capsule. ### Claim 16 A pharmaceutical composition for use in soft capsule dosage forms consisting essentially of: a) loratadine and derivatives thereof present in an amount of about 6.3% by weight of the total composition; b) mono- and di-glycerides of medium chain fatty acids present in an amount of about 87% by weight of the total composition; c) povidone present in an amount of about 6.3% by weight of the total composition; and d) polyoxyethylene sorbitan fatty acid ester present in an amount of about 0.8% by weight of the total composition. ### Claim 17 A pharmaceutical composition for use in soft gelatin dosage forms consisting essentially of: a) decarboalkoxylated loratadine derivative in a pharmaceutically effective amount; b) a mixture of mono- and d-glycerides of medium chain fatty acids comprising a mixture of caprylic and capric acid; c) povidone; and d) polyoxyethylene sorbitan fatty acid esters; wherein said loratadine derivative is present in an amount of about 6.3% by weight of the total composition. ### Claim 18 (depends on 17) The composition of claim 17 wherein the decarbalkoxylated loratadine derivative is descarboethoxyloratadine. ### Claim 19 A soft capsule dosage form comprising a fill composition consisting essentially of: a) loratadine and derivatives thereof in a pharmaceutically effective amount; b) a mixture of mono- and diglycerides of medium chain fatty acids; c) povidone; d) polyoxyethylene sorbitan fatty acid ester; and wherein said loratadine and derivatives thereof is present in an amount of about 6.3% by weight of the total composition, and wherein said soft capsule has a capsule size of 5 minim or less. ### Claim 20 (depends on 19) The soft capsule of claim 19 wherein the capsule size is a 3 minim oval.