Controlled-Release Oral Formulations of Lipophilic Drugs

An oral drug delivery device for controlled delivery of at least one lipophilic drug, the device comprising

• a drug-containing polymeric component comprising at least one pharmaceutically acceptable film-forming hydrophilic polymeric component, optionally at least one pharmaceutically acceptable plasticizer, and at least one lipophilic drug emulsified in at least one emulsifying agent, wherein said emulsified drug is embedded in said drug-containing polymeric component,
• a controlled release (CR) polymeric component comprising at least one pharmaceutically acceptable film-forming hydrophilic polymer, at least one pharmaceutically acceptable release-modifying agent, and optionally at least one pharmaceutically acceptable plasticizer,
• wherein said hydrophilic film-forming polymer and said optional plasticizer in said drug-containing polymeric component and in said CR polymeric component may be the same or different;
• and
• wherein the oral drug delivery device is configured for being integrated into an orally administrable dosage unit form, and
• wherein said oral drug delivery device is configured for enabling said at least one release-modifying agent, upon ingestion of said dosage unit form and contact with gastric medium and/or intestinal medium, to form a viscous gel that is configured for gradually eroding concurrently with passage through the stomach and the intestinal tract, and for controllably releasing said emulsified drug into surrounding environment in the form of micelles, optionally wherein said release-modifying agent is a hydrophilic polymer which when dissolved in water at 2% w/w gives a solution with viscosity of at least 150 mPa*sec,
• optionally, wherein said release modifying agent is comprised in an amount of at least about 30 mg per said dosage unit form and wherein said at least one emulsifying agent is a lipid excipient having HLB (Hydrophilic Lipophilic Balance) greater than 6, optionally wherein said emulsifying agent is a mixture of lipid excipients of which at least 50% have HLB greater than 6, and remaining lipid excipients are any one of oils, fatty acids, glycerides, polyoxyglycerides, polyglyceryl and polyalcohol esters or water insoluble surfactants, or any mixture of at least two thereof, wherein each said remaining lipid excipients has HLB lower than, equal to or higher than 6.