# US 2014/0154315 A1 · Hydrophobic Preparations > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0154315 A1 - Document ID: US20140154315A1 - Status: Published application - Kind: A1 - Application number: 14/115,922 - Filed: 2012-05-04 - Published: 2014-06-05 - Earliest claimed: 2011-05-06 - Assignees: Vaxcine Ltd. - Inventors: Roger New - Web page: https://patentgrep.com/patent/US20140154315A1 ## CPC - A61K 39/0008: {Antigens related to auto-immune diseases; Preparations to induce self-tolerance} - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)} - A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} - A61K 31/00: Medicinal preparations containing organic active ingredients - A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61K 2039/55566: {Emulsions, e.g. Freund's adjuvant, MF59} - Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change - 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 - Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE ## Abstract The present invention relates to preparations of substances in hydrophobic solvents in which they would not normally be soluble and to processes for obtaining these preparations. In particular, the invention relates to preparations of hydrophilic species in hydrophobic solvents such as oils. The use of these preparations as vaccines and in pharmaceutical compositions is also described. ## Claims ### Claim 1 A single phase hydrophobic preparation comprising a hydrophilic species, and an amphiphilic component comprising sodium docusate, a phospholipid and a nonionic amphiphile, in an oil phase, wherein the moieties of the hydrophilic species are surrounded by the amphiphilic component with the hydrophilic head groups of the amphiphilic component orientated towards the hydrophilic species and wherein there is no chemical interaction between the amphiphilic component and the hydrophilic species; characterised in that said non-ionic amphiphile has a lipophilic chain comprising 10 to 20 carbons, and a head group comprising 2 to 10 oxyethylene groups or 1 to 3 hydroxyl groups. ### Claim 2 (depends on 1) The preparation of claim 1 wherein said hydrophilic species is selected from peptides, proteins, lipids, sugars, nucleic acids, steroids and/or conjugates of one or more of these agents in combination, and/or a conjugate with at least one medium- or long-chain hydrocarbon tail. ### Claim 3 A method of manufacture of a hydrophobic preparation containing a hydrophilic species which includes the following steps: (i) mixing a solution of sodium docusate, a phospholipid and a non-ionic amphiphile dissolved in a hydrophobic solvent with a solution of a hydrophilic species dissolved in an aqueous phase to form an emulsion; (ii) removing the aqueous phase and hydrophobic solvent; and (iii) adding an oil phase to the dry residue obtained in (ii). ### Claim 4 (depends on 3) A method as claimed in claim 3 wherein said hydrophobic solvent is selected from cyclohexane, cycloheptane, cyclooctane or mixtures thereof and optionally tertiary butanol. ### Claim 5 (depends on 3) A method as claimed in claim 3 wherein step (ii) is carried out by lyophilisation. ### Claim 6 (depends on 3) The method of claim 3 wherein said hydrophilic species is selected from peptides, proteins, lipids, sugars, nucleic acids, steroids and/or conjugates of one or more of these agents in combination, and/or a conjugate with at least one medium- or long-chain hydrocarbon tail. ### Claim 7 (depends on 3) A method of claim 3 wherein said hydrophilic species is collagen or fragments, derivatives and analogues thereof, which is dissolved in a mixture of acetic acid and dimethyl sulfoxide. ### Claim 8 (depends on 1) A two phase composition comprising an aqueous phase and a single phase hydrophobic preparation of claim 1. ### Claim 9 (depends on 8) A two phase composition of claim 8 wherein said two phase composition is an oil-in water emulsion. ### Claim 10 (depends on 8) A two phase composition of claim 8 wherein said aqueous phase comprises gelatin or albumin. ### Claim 11 (depends on 10) A two phase composition of claim 10 wherein said two phase composition is a microcapsule. ### Claim 12 (depends on 1) A method of forming a two phase composition comprising contacting a preparation of claim 1. ### Claim 13 (depends on 12) The method of claim 12 wherein said aqueous phase comprises gelatin or albumin. ### Claim 14 (depends on 1) A preparation of claim 1 for use in medicine. ### Claim 15 (depends on 1) A composition comprising a preparation of claim 1 and optionally one or more pharmaceutical excipients, diluents or carriers. ### Claim 16 (depends on 15) A vaccine comprising a composition of claim 15. ### Claim 17 (depends on 16) A vaccine of claim 16 adapted for oral administration. ### Claim 18 (depends on 17) A vaccine of claim 17 comprising a capsule. ### Claim 19 (depends on 18) A vaccine of claim 18, wherein said capsule is enterically coated. ### Claim 20 (depends on 16) The vaccine of claim 16 wherein said composition comprises a malaria antigen or an influenza antigen, or an enteric disease pathogen antigen. ### Claim 21 (depends on 15) The pharmaceutical composition of claim 15 adapted for oral, intramuscular or subcutaneous administration. ### Claim 22 (depends on 15) An enterically coated capsule comprising a pharmaceutical composition of claim 15. ### Claim 23 (depends on 15) A composition of claim 15 comprising collagen for use in treating rheumatoid arthritis. ### Claim 24 (depends on 1) A cosmetic formulation comprising preparation of claim 1 and optionally one or more excipients, diluents or carriers.