Immediate release, abuse deterrent pharmaceutical compositions

Abstract

The present disclosure provides pharmaceutical compositions and processes for making solid dosage form pharmaceutical compositions that provide immediate release of active ingredients and have abuse deterrent properties. The pharmaceutical compositions provided herein comprise at least one pharmaceutically active ingredient, at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system.

What is claimed is: 
     
         1 . A pharmaceutical composition comprising:
 at least one active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt thereof;   at least one low molecular weight hydrophilic polymer, the at least one low molecular weight hydrophilic polymer having an average molecular weight of no more than 200,000 Daltons;   at least one high molecular weight hydrophilic polymer, the at least one high molecular weight hydrophilic polymer having an average molecular weight of at least 400,000 Daltons; and   an effervescent system;   
       wherein the pharmaceutical composition is a cured solid dosage form that was heated at a temperature of less than about 90° C., wherein the cured dosage form has a hardness value that is higher than that of an uncured solid dosage form, and wherein the cured solid dosage form deters abuse and provides immediate release of the at least one API. 
     
     
         2 . The pharmaceutical composition form of  claim 1 , wherein the at least one low molecular weight hydrophilic polymer is chosen from a polyalkylene oxide, a cellulose ether, a polyalkylene glycol, or a poloxamer; and the at least one low molecular weight hydrophilic polymer is present in an amount from about 5% to about 50% by weight of the pharmaceutical composition. 
     
     
         3 . The pharmaceutical composition of  claim 1 , wherein the at least one high molecular weight hydrophilic polymer is chosen from a polyalkylene oxide, a cellulose ether, or a polysaccharide; and the at least one high molecular weight hydrophilic polymer is present in an amount from about 0.1% to about 30% by weight of the pharmaceutical composition. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein the effervescent system comprises a) an acid component chosen from an organic acid, an inorganic acid, or combination thereof and b) a base component chosen from an alkali metal bicarbonate, an alkaline earth metal bicarbonate, an alkali metal carbonate, an organic carbonate, or combination thereof; and the effervescent system is present in an amount from about 20% to about 90% by weight of the pharmaceutical composition. 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein the at least one API is an opioid or a combination of an opioid and a non-opioid analgesic; and the opioid is oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine. 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the cured and uncured solid dosage forms are tablets, compacts, pellets, caplets, or pills. 
     
     
         7 . The pharmaceutical composition of  claim 1 , wherein the cured solid dosage form further comprises a film coating. 
     
     
         8 . The pharmaceutical composition of  claim 1 , wherein the cured solid dosage form deters abuse by breaking into a plurality of particles having an average diameter of greater than about 250 microns when crushed, ground, or pulverized. 
     
     
         9 . The pharmaceutical composition of  claim 1 , wherein the cured solid dosage form releases at least about 80% of the at least one API within about 30 minutes when measured using an USP-approved in vitro release procedure. 
     
     
         10 . The pharmaceutical composition of  claim 1 , wherein the at least one API is oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine; the at least one low molecular weight hydrophilic polymer is chosen from polyethylene oxide, hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose, polyethylene glycol, or a poloxamer; the at least one high molecular weight hydrophilic polymer is chosen from polyethylene oxide, xanthan gum, hydroxypropyl cellulose, or hydroxypropylmethyl cellulose; and the effervescent system comprises a) an acid component chosen from an organic acid, an inorganic acid, or combination thereof and b) a base component chosen from an alkali metal bicarbonate, an alkaline earth metal bicarbonate, an alkali metal carbonate, an organic carbonate, or combination thereof. 
     
     
         11 . The pharmaceutical composition of  claim 10 , wherein the at least one low molecular weight hydrophilic polymer is present in an amount from about 10% to about 40% by weight of the pharmaceutical composition; the at least one high molecular weight hydrophilic polymer is present in an amount from about 1% to about 15% by weight of the pharmaceutical composition; and the effervescent system is present in an amount from about 40% to about 80% by weight of the pharmaceutical composition. 
     
     
         12 . The pharmaceutical composition of  claim 11 , which comprises at least two low molecular weight hydrophilic polymers and at least two high molecular weight hydrophilic polymers. 
     
     
         13 . The pharmaceutical composition of  claim 12 , further comprising at least one lubricant, at least one antioxidant, or combination thereof. 
     
     
         14 . The pharmaceutical composition of  claim 13 , wherein the cured solid dosage form further comprises a film coating. 
     
     
         15 . The pharmaceutical composition of  claim 13 , wherein the at least one API is oxycodone hydrochloride, oxymorphone hydrochloride, or morphine sulfate. 
     
     
         16 . The pharmaceutical composition of  claim 13 , wherein the cured and uncured solid dosage forms are tablets. 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein the hardness value of the cured solid dosage form is at least about three-fold higher than that of the uncured solid dosage form. 
     
     
         18 . The pharmaceutical composition of  claim 16 , wherein the cured solid dosage form deters abuse by breaking into a plurality of particles having an average diameter of greater than about 250 microns when crushed, ground, or pulverized. 
     
     
         19 . The pharmaceutical composition of  claim 16 , wherein the cured solid dosage form deters abuse by forming a viscous mixture or gel when in contact with about 3 mL to about 10 mL of an aqueous solvent. 
     
     
         20 . The pharmaceutical composition of  claim 16 , wherein the cured solid dosage form releases at least about 80% of the at least one API within about 30 minutes when measured using an USP-approved in vitro release procedure.