Misuse preventative, controlled release formulation

摘要

Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a superabsorbent material. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material creates a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent.

主权项

1. A solid, compressed controlled release composition for oral administration of at least one pharmaceutically active agent, comprising:
(a) a first layer comprising a first population of controlled release microparticles having a pharmaceutically active agent disposed therein; (b) a second layer adjacent the first layer and comprising a superabsorbent material comprising a cross-linked acrylic acid polymer characterized in that the cross-linked acrylic acid polymer absorbs at least 15 times its own weight of water, the second layer comprising from about 10% to about 50% w/w of the superabsorbent material; (c) a controlled release agent disposed within the first layer, the second layer, or both the first layer and the second layer; and (d) the composition having a hardness from about 200 N to about 400 N, and wherein the composition,
(i) when intact and exposed to an aqueous medium, the pharmaceutically active agent is released from the formulation over a prolonged period of time,(ii) when crushed and exposed to 2 mL of water, the superabsorbent material absorbs all of the water and creates a hard gel that traps the microparticles, whereupon the hard gel and the microparticles provide controlled release of the pharmaceutically active agent disposed within the microparticles, and(iii) when broken and exposed to 900 mL of water in a U.S.P. Type I Apparatus with stirring at 100 rpm for 30 minutes at 37° C., less than about 50% by weight of the pharmaceutically active agent originally present in the formulation before it was broken is released into the water.