Patent ID: 8652523

Claim:
Orally administered microcapsules for modified release of at least one active principle with low solubility, wherein the mean diameter of the microcapsules are less than 1000 microns; wherein each microcapsule has a core comprising at least one active principle and at least one solubilizing agent, wherein said solubilizing agent increases the solubility of said active principle by more than 50% when said solubilizing agent is placed in an aqueous solution at a concentration of 20% w/w at 37° C.; wherein the at least one solubilizing agent is selected from the group consisting of hydrophilic polymers, polyvinyl pyrrolidone, polyvinyl alcohol, hydrophilic derivatives of cellulose, hydroxypropylcellulose, carboxymethylcellulose, maltodextrins, polyethylene glycol, surfactants, polyoxyethylene-polyoxypropylene copolymers, polyoxyethylenated hydrogenated castor oil, sodium dodecyl sulfate, esters of sucrose or sorbitan, phospholipids, polyethylene glycol stearate, disodium palmoate, polyoxyethylenated oils, polysorbates, sequestering agents, cyclodextrins, and mixtures thereof; wherein the mass fraction [solubilizing agent]×100/[solubilizing agent+AP] is greater than or equal to 5%; wherein said solubilizing agent confers properties upon the core such that in a dissolving test (TD) a non-coated core releases 80% of said active principle in less than two hours; wherein the core is coated with a coating film which controls the modified release of the active principles; wherein the coating film is at least 3% dry weight/dry weight of the microcapsule mass; wherein the coating film comprises at least one film-forming polymer (P1) insoluble in gastrointestinal tract fluids, at least one water-soluble polymer (P2), and at least one plasticizer, (PL), wherein the mass fraction by dry weight of P1 relative to the total mass of the coating is between 40 and 90%; Wherein the mass fraction by dry weight P2/(P1+P2) is between 15 and 60%; and Wherein the mass fraction by dry weight PL/(P1+PL) is between 1 and 30%.