Abuse resistant pharmaceutical compositions

#The present invention relates to a composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The composition of the invention is adapted to be abuse resistant so as to reduce or eliminate such abuse.

#It is widely known that certain categories of drugs such as analgesics (e.g. opioids), sedatives (e.g. benzodiazepines) and stimulants (e.g. amphetamines) have potential to be misused or abused if they are not used as intended or as prescribed.

#In the case of intentional misuse or abuse a person may attempt to extract the active ingredient from the commercial dosage form in order to concentrate it and take a larger amount than prescribed or to take the drug in a different manner to that prescribed, the object being to produce a euphoric “high” or some other pharmacological effect other than that produced when the product is used as intended.

#FIG. 1 is a schematic representation of a gelling agent-containing, abuse deterrent bead according to the invention.

#FIG. 2 is a graph illustrating the in vitro release of drug from two compositions of the invention compared to that of two comparator compositions which do not contain a gelling agent component.

#FIG. 3 is a graph illustrating the in vivo release of drug (mean plasma concentrations) from a composition according to the invention compared to that of a comparator composition which does not contain a gelling agent component.

#The term “bead” as used herein means a discrete unit such as a particle, particulate, pellet, granule or the like, and the terms “population of beads” and “bead population” each mean a plurality (two or more) of said beads.

#The term “gel” as used herein means a three dimensional network or structure formed from a synthetic and/or natural polymer which can absorb and retain a significant amount of water (relative to the amount of polymer) upon exposure to an aqueous environment. Gels are essentially dilute cross-linked systems which may be classified as ‘weak’ or ‘strong’ depending on their flow behaviour at steady state (weak—meaning more free flowing or relatively less viscous; strong—meaning less free flowing or relatively more viscous). The term “gelling agent” is construed accordingly as a material which forms, or is capable of forming, a gel upon hydration.

#The term “permeable” as used herein means the ability of a coating to allow another substance, particularly water or other solvents, to pass through it. The term “semi-permeable” as used herein means a coating with selective permeability, allowing some substances (such as solvents) to pass through it, whilst not allowing the passage of others (especially solutes). Permeable coatings are taken to include semi-permeable and porous (having interstices or passages that enable liquid to pass though) coatings. By contrast, the term “impermeable” as used herein means a coating which does not allow other substances to pass through it.