Abuse resistant capsule
The present invention is directed to an immediate release and extended release capsule or capsule fill which mitigates the abuse of abuse-susceptible active pharmaceutical ingredients by direct intravenous injection. The fill comprises a parenteral abuse resistant liquid formulation which when mixed with water and heated, results in a turbid, viscous or bubbling mixture that is not injectable with a standard insulin syringe. The abuse-susceptible active pharmaceutical ingredient is selected from the group consisting of opiates, opioids, tranquillizers, stimulants and narcotics.
1. An immediate release parenteral abuse resistant capsule comprising a parenteral abuse resistant liquid and a shell, the parenteral abuse resistant liquid comprising:
(a) an abuse-susceptible active pharmaceutical ingredient which is at least one stimulant;
(b) 2 to 5 wt. % xanthan gum;
(c) polysorbate 80 and optionally sorbitan monolaurate;
(d) 10 to 70 wt. % medium chain triglycerides; and
(e) 1 to 5 wt. % colloidal anhydrous silica; wherein the wt. % values are based on the total weight of the parenteral abuse resistant liquid;
such that a mixture of about 250 to about 1000 milligrams of the abuse resistant liquid with 5 milliliters of water at the mixture's boiling point forms a viscous phase, wherein about 33% or less of the pharmaceutically active ingredient can be recovered from the viscous phase drawn up into a 25 millimeter needle having an inner diameter of 0.60 millimeters,
wherein the capsule releases more than 80% of the active pharmaceutical ingredient within the gastrointestinal tract within 30 minutes of administration.
2. The parenteral abuse resistant capsule of claim 1 , wherein the viscous phase cannot pass through a 25 millimeter needle having an inner diameter of 0.60 millimeters.
3. The parenteral abuse resistant capsule of claim 1 , wherein the stimulant is an amphetamine, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof.
4. The parenteral abuse resistant capsule of claim 1 , that is resistant to alcohol dose dumping.
5. The parenteral abuse resistant capsule of claim 1 , that is resistant to solvent, acidic or aqueous extraction.
6. The parenteral abuse resistant capsule of claim 1 , wherein the capsule is a soft capsule.
7. The parenteral abuse resistant capsule of claim 1 , wherein the capsule is a hard gelatin capsule.
8. The parenteral abuse resistant capsule of claim 1 , wherein the parenteral abuse resistant liquid comprises 4 to 52.7 wt. % polysorbate 80, based on the total weight of the parenteral abuse resistant liquid.
9. The parenteral abuse resistant capsule of claim 8 , wherein the parenteral abuse resistant liquid further comprises sorbitan monolaurate.
10. The parenteral abuse resistant capsule of claim 1 , further comprising 40 to 70 wt. % hard fat based on the total weight of the parenteral abuse resistant liquid.