초록 ▼

The present invention relates to microcapsules for the oral administration of medicinal and/or nutritional active principles (AP), which are smaller than or equal to 1000 .mu.m in size. These microcapsules consist of particles which are coated with a coating material consisting of a mixture of a fil

The present invention relates to microcapsules for the oral administration of medicinal and/or nutritional active principles (AP), which are smaller than or equal to 1000 .mu.m in size. These microcapsules consist of particles which are coated with a coating material consisting of a mixture of a film-forming polymer derivative, a hydrophobic plasticizer, a functional agent and a nitrogen-containing polymer. These microcapsules are also characterized by their ability to remain in the small intestine for a long time (at least 5 hours) and to allow, during the residence, release and absorption of the AP. The invention also relates to a process for the production of the said microcapsules.

대표청구항 ▼

[ We claim:] [1.] Microcapsules of reservoir kind containing at least one medicinal nd nutritional active principle (AP), with the exclusion of acetylsalicylic acid (ASA), which are intended for oral administration, characterized:in that they consist of particles of AP each coated with at least one

[ We claim:] [1.] Microcapsules of reservoir kind containing at least one medicinal nd nutritional active principle (AP), with the exclusion of acetylsalicylic acid (ASA), which are intended for oral administration, characterized:in that they consist of particles of AP each coated with at least one coating film of specific following composition:1- at least one film-forming polymer (P1) which is insoluble in the liquids of the digestive tract, present in a quantity of 50 to 90%, preferably 50 to 80% by weight of dry matter of the whole coating composition, and consisting of at least one non-hydrosoluble cellulose derivate, ethylcellulose and/or cellulose acetate being prefered;2- at least one nitrogen-containing polymer (P2), present in a quantity of 2 to 25, preferably 5 to 15% by weight of dry matter of the whole coating composition, and consisting of at least one polyacrylarnide and/or one poly-N-vinylamide and/or one poly-N-vinyl-lactame, the polyacrylamide and/or the polyvinylpyrrolidone being prefered;3- at least one plasticizer present in a quantity of 2 to 20%, preferably 4 to 15% by weight of dry matter of the whole coating composition, and consisting of at least one of the following compounds: glycerol esters, phtalates, citrates, sebacates, cetylalcohol esters, castor oil and cutin, castor oil being particularly prefered;4- at least one surface-active and/or lubricating agent, present in a quantity of 2 to 20%, preferably 4 to 15% by weight of dry matter of the whole coating composition, and chosen from anionic surfactants, preferably the alkali metal or alkakine-earth metal salts of fatty acids, stearic acid and/or oleic acid being preferred, and/or from nonionic surfactants, preferably polyoxyethylenated esters of sorbitan and/or polyoxyethylenated esters of sorbitan and/or polyoxyethylenated derivatives of castor oil, and/or from lubricants such as stearates, preferably calcium, magnesium, aluminium or zinc stearate, or such as stearylfumarate, preferably sodium stearylfimarate, and/or glyceryl behenate, said agent comprising only one or a mixture of the above products;in that they have a particle size of between 50 and 1000 microns, preferably of between 100 and 750 microns and, more preferably, of between 100 and 500 microns;in that they are designed so as to be able to remain in the small intestine for a period of at least about 5 hours, preferably of at least about 7 hours and, even more preferably, for a period of between about 8 hours and about 24 hours, and permitting so the absorption of the AP during at least part of their residence in the small intestine.