JP2016040307A5 - - Google Patents

Claims (24)

A pH-controlled pulsatile release system (PPRS) comprising a core surrounded by a coating layer, wherein the core comprises an active substance, and the coating layer comprises a swellable agent. A system comprising an embedded pH sensitive coating material, wherein the swelling agent can absorb at least 5 times its weight of water . The system of claim 1, wherein the active substance is a pharmaceutically active substance. The swelling agent, it is possible to suck at least 10 times the water weight of that, according to claim 1 or 2, wherein the system. The swelling agent is Ru is selected from the group consisting of sodium starch glycolate and cross-linked sodium carboxymethyl cellulose, of any one of claims 1 to 3 system. 5. The system of claim 4, wherein the swelling agent is sodium starch glycolate. The coating material is cellulose acetate trimellitate (cellulose acetate trimellitate), hydroxypropyl methylcellulose phthalate, polyvinyl acetate phthalate, and is selected from the group consisting of copolymerized methacrylic acid / methacrylic acid methyl ester, any one of claims 1 to 5 The system according to one item. 7. The system of claim 6, wherein the copolymerized methacrylic acid / methacrylic acid methyl ester is a material known under the trade name EUDRAGIT ™. 8. The system of any one of claims 1-7 , wherein the swelling agent is present in the coating layer in an amount that provides a coating having a non-leaching system in relation to its particle size and coating structure. It said coating layer further comprises an additive, of any one of claims 1-8 system. The system of claim 9, wherein the additive is a plasticizer. 11. The system of claim 10, wherein the plasticizer is selected from the group consisting of polyethylene glycol (PEG), triethyl citrate (TEC), and tributyl sebacate (TBS). The active substance, a neurotransmitter, hormone agonists or antagonists, anti-inflammatory agents steroidal or non-steroidal, stable isotope is selected from the group consisting of immunogenic substances, or mixtures thereof, according to claim 1 to 11 The system according to any one of the above. 13. The system according to claim 12, wherein the neurotransmitter is L-Dopa. 13. The system of claim 12, wherein the hormone agonist or antagonist is cetrorelix. 13. The system according to claim 12, wherein the immunogenic substance is a vaccine. A coating suspension for use in the manufacture of a pH controlled pulsed release system (PPRS) comprising a mixture of a pH sensitive coating material and a swelling agent in a solvent or solvent mixture, wherein the coating material is against the solvent A coating suspension wherein the swelling agent is soluble, the swelling agent is insoluble and non-swellable in the solvent, and the swelling agent can absorb at least 5 times its weight of water . A method of preparing a system for pH controlled pulsed release of a solid substrate comprising the following steps:
Providing a coating suspension according to claim 16 ;
Step of applying the suspension to a solid substrate; and,
evaporating the solvent of the suspension to form a coating layer in which the swelling agent is embedded in a matrix of pH sensitive coating material. 18. The method of claim 17, wherein the step of applying the suspension to a solid substrate is by spray coating. Use of a coating suspension according to claim 16 for the manufacture of a pH controlled pulsed release system. 20. Use according to claim 19, wherein the pH controlled pulsed release system is a drug delivery system. 21. Use according to claim 20, wherein the drug delivery system is a colon specific drug delivery system or a duodenum specific drug delivery system. 16. A pharmaceutical composition comprising a pulsed pH-controlled release system (PPRS) according to any one of claims 1 to 15 and a pharmaceutically acceptable carrier. Comprising the step of administering a suitable amount of the pharmaceutical composition to a subject in need thereof, for use in a method for site-specific intestinal delivery of drugs, according to claim 22 pharmaceutical composition. 24. A pharmaceutical composition according to claim 23 for use in a method for colon specific or duodenum specific drug delivery.