Oral dosage form comprising an antimisuse system

摘要

An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents.;Said oral solid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.

主权项

1. An oral solid dosage form comprising:
(a) at least one salt of at least one analgesic active principle, (b) an anti-misuse system comprising at least one quenching agent, said dosage form comprising a first population of microparticles for the modified release of said analgesic active principle, each microparticle of the first population of microparticles individually comprising (1) a core comprising said at least one analgesic active principle salt, and (2) a coating on said core, wherein the coating controls the modified release of said analgesic active principle, wherein said first population of microparticles is in a non-complexed form relative to said quenching agent, said dosage form further comprising a second population of microparticles containing said quenching agent, wherein said quenching agent is a salt comprising ion having the opposite polarity to the polarity of the analgesic active principle salt in solution, wherein said quenching agent comprises a salt of an ion exchange resin or a salt selected from the group consisting of: sodium dodecyl sulfate, sodium docusate, anionic methacrylic copolymers, methyl methacrylate and methacrylic acid copolymers, crosslinked acrylic polyacids, carboxymethylcelluloses, carboxymethycellulose derivatives, crosslinked carboxymethylcellulose, crosslinked carboxymethylcellulose derivatives, alginates, xanthane, arabic gum, alginate (sulfonate)propylene glycol, glucuronates, carbonates, gluconates, succinates, phosphates, glycerophosphates, lactates, trisilicates, fumarates, adipates, benzoates, tartrates, sulfonamides, acesulfames, metallic salts of Ca, metallic salts of Fe, metallic salts of Mg, metallic salts of Zn, trimethyl tetradecyl ammonium bromide, benzethonium chloride, chitosan, cationic methacrylic copolymers, Eudragit™ RS, Eudragit™ RL, copolymer based on dimethylaminoethyl methacrylate and neutral methacrylic esters and mixtures thereof, wherein said salt comprises an ion capable of forming a complex with said analgesic active principle salt when said analgesic active principle salt is extracted in vitro in solution, wherein said complex is poorly soluble in common solvents selected from the group of water-ethanol mixtures, alcohol, alcoholic beverages, sodas, vinegar, hydrogen peroxide, and mixtures thereof.