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 process for preparing a solid dosage form, the process comprising:
 a) forming a mixture comprising at least one active pharmaceutical ingredient (API) susceptible to abuse 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 90° C. to form the solid dosage form;   wherein the solid dosage form deters abuse and provides immediate release of the at least one API.   
     
     
         2 . The process of  claim 1 , wherein the at least one low molecular weight hydrophilic polymer is a polyalkylene oxide, a cellulose ether, a polyalkylene glycol, a poloxamer, or combination thereof. 
     
     
         3 . The process of  claim 1 , wherein 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. 
     
     
         4 . The process of  claim 1 , wherein the at least one high molecular weight hydrophilic polymer is a polyalkylene oxide, a cellulose ether, a polysaccharide, or combinations thereof. 
     
     
         5 . The process of  claim 1 , wherein 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. 
     
     
         6 . The process of  claim 1 , wherein the effervescent system comprises i) an acid component chosen from an organic acid, an inorganic acid, or combinations thereof and ii) a base component chosen from an alkali metal bicarbonate, an alkaline earth metal bicarbonate, an alkali metal carbonate, an organic carbonate, or combinations thereof. 
     
     
         7 . The process of  claim 1 , wherein the effervescent system is present in an amount from about 20% to about 90% by weight of the solid dosage form. 
     
     
         8 . The process 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. 
     
     
         9 . The process of  claim 1 , wherein the mixture at step (a) further comprises at least one lubricant chosen from a metal stearate, colloidal silicon dioxide, hydrogenated vegetable oil, sterotex, polyoxyethylene monostearate, polyethylene glycol, sodium stearyl fumarate, sodium benzoate, sodium lauryl sulfate, magnesium lauryl sulfate, light mineral oil, or combination thereof. 
     
     
         10 . The process of  claim 9 , wherein the at least one lubricant is present in an amount from about 0.1% to about 2% by weight of the solid dosage form. 
     
     
         11 . The process of  claim 1 , wherein the temperature at step (c) is from about 50° C. to about 80° C. 
     
     
         12 . The process of  claim 1 , further comprising coating the solid dosage form with a film coating. 
     
     
         13 . The process of  claim 1 , wherein the solid dosage form is a tablet, compact, pellet, caplet, or pill. 
     
     
         14 . The process of  claim 1 , wherein the at least one low molecular weight hydrophilic polymer is polyethylene oxide, hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose, polyethylene glycol, a poloxamer, or combination thereof; the at least one high molecular weight hydrophilic polymer is polyethylene oxide, xanthan gum, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, or combination thereof; the effervescent system comprises i) an acid component chosen from an organic acid, an inorganic acid, or combination thereof and ii) 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. 
     
     
         15 . The process of  claim 14 , 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 15% 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. 
     
     
         16 . The process of  claim 15 , wherein mixture at step (a) further comprises a lubricant chosen from magnesium stearate, calcium stearate, or zinc stearate, and the lubricant is present in an amount from about 0.3% to about 1% by weight of the solid dosage form. 
     
     
         17 . The process of  claim 16 , wherein the solid dosage form is a tablet. 
     
     
         18 . The process of  claim 17 , wherein the 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 process of  claim 17 , wherein the 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 process of  claim 17 , 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.