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 solid dosage form comprising at least one active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt thereof, at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system, wherein the at least one low molecular weight hydrophilic polymer has an average molecular weight of no more than 200,000 Daltons, the at least one high molecular weight hydrophilic polymer has an average molecular weight of at least 400,000 Daltons, and the solid dosage form has been heated at a temperature from about 50° C. to about 80° C. to plasticize and/or cure at least one of the low or high molecular weight hydrophilic polymers. 
     
     
         2 . The solid dosage 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, a poloxamer, or combination thereof; 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 solid dosage form. 
     
     
         3 . The solid dosage form of  claim 1 , wherein the at least one high molecular weight hydrophilic polymer is chosen from a polyalkylene oxide, a cellulose ether, a polysaccharide, or combination thereof; 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 solid dosage form. 
     
     
         4 . The solid dosage form of  claim 1 , wherein the effervescent system comprises an a) 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 solid dosage form. 
     
     
         5 . The solid dosage form 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 chosen from oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine. 
     
     
         6 . The solid dosage form of  claim 1 , wherein the solid dosage form further comprising a film coating. 
     
     
         7 . The solid dosage form of  claim 1 , wherein the solid dosage form has a hardness of at least about 15 kiloponds. 
     
     
         8 . The solid dosage form of  claim 1 , wherein the solid dosage form breaks into a plurality of particles having an average diameter of greater than about 250 microns when crushed, ground, or pulverized. 
     
     
         9 . The solid dosage form of  claim 1 , wherein the solid dosage form forms a viscous mixture or gel when in contact with about 3 mL to about 10 mL of an aqueous solvent. 
     
     
         10 . The solid dosage form of  claim 1 , wherein the 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. 
     
     
         11 . The solid dosage form of  claim 1 , wherein the at least one low molecular weight hydrophilic polymer is chosen from polyethylene oxide, hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose, polyethylene glycol, a Poloxamer, or combination thereof; the at least one high molecular weight hydrophilic polymer is chosen from polyethylene oxide, xanthan gum, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, or combination thereof; 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 at least one API is an opioid chosen from oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine. 
     
     
         12 . The solid dosage form of  claim 11 , wherein the at least one low molecular weight hydrophilic polymer is present an amount from about 15% to about 35% by weight of the solid dosage form; wherein the at least one high molecular weight hydrophilic polymer is present an amount from about 1% to about 55% by weight of the solid dosage form; and the effervescent system is present in an amount from about 50% to about 70% by weight of the solid dosage form. 
     
     
         13 . The solid dosage form of  claim 12 , wherein the solid dosage form has a hardness of at least about 20 kiloponds; and the 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. 
     
     
         14 . A process for preparing a solid dosage form, the process comprising:
 a. forming a mixture comprising at least one active pharmaceutical ingredient (API) or a pharmaceutically acceptable salt thereof, at least one low molecular weight hydrophilic polymer, at least one high molecular weight hydrophilic polymer, and an effervescent system, wherein the at least one low molecular weight hydrophilic polymer has an average molecular weight of no more than 200,000 Daltons, and the at least one high molecular weight hydrophilic polymer has an average molecular weight of at least 400,000 Daltons;   b. forming the mixture into a solid dosage unit; and   c. heating the solid dosage unit at a temperature of less than about 90° C. to yield the solid dosage form.   
     
     
         15 . The process of  claim 14 , further comprising coating the solid dosage unit at step (b) or the solid dosage form at step (c) with a film coating. 
     
     
         16 . The process of  claim 14 , wherein the at least one API is an opioid or a combination of an opioid and a non-opioid analgesic; and the opioid is chosen from oxycodone, oxymorphone, hydrocodone, hydromorphone, codeine, or morphine. 
     
     
         17 . The process of  claim 14 , wherein the at least one low molecular weight hydrophilic polymer is chosen from a polyalkylene oxide, a cellulose ether, a polyalkylene glycol, a poloxamer, or combination thereof; 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 solid dosage form. 
     
     
         18 . The process of  claim 14 , wherein the at least one high molecular weight hydrophilic polymer is chosen from a polyalkylene oxide, a cellulose ether, a polysaccharide, or combination thereof; 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 solid dosage form. 
     
     
         19 . The process of  claim 14 , 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 solid dosage form. 
     
     
         20 . The process of  claim 15 , wherein the mixture formed in step (a) further comprises a lubricant that is present in an amount from about 0.1% to about 2% by weight of the solid dosage form.