Tamper-resistant pharmaceutical compositions of opioids and other drugs

Abstract

Tamper-resistant pharmaceutical compositions have been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. The tamper-resistant compositions retard the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.

1 .- 34 . (canceled) 
     
     
         35 . A tamper resistant pharmaceutical composition comprising a plurality of solid particles each particle comprising:
 (a) one or more drugs prone to abuse or a pharmaceutically acceptable salt thereof;   (b) one or more excipients comprising fats, fatty substances, waxes, wax-like substances or mixtures thereof;   wherein the particles have a D[0.50] between about 200 microns and about 400 microns and a D[0.90] between about 400 microns to about 700 microns.   
     
     
         36 . The composition of  claim 35  wherein the solid particles are substantially spherical. 
     
     
         37 . The composition of  claim 35  wherein the one or more excipients comprises a fatty acid. 
     
     
         38 . The composition of  claim 37  wherein the one or more fatty acids is selected from the group consisting of linoleic acid, octanoic acid, capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, and oleic acid. 
     
     
         39 . The composition of  claim 38 , wherein the one or more fatty acids is selected from the group consisting of stearic acid, palmitic acid, and myristic acid. 
     
     
         40 . The composition of  claim 39 , wherein the fatty acid is myristic acid. 
     
     
         41 . The composition of  claim 37  wherein the one or more fatty acids and the one or more drugs prone to abuse are in the form of a fatty acid salt. 
     
     
         42 . The composition of  claim 41  wherein the drug prone to abuse is oxycodone. 
     
     
         43 . The composition of  claim 41 , wherein the one or more fatty acids is selected from the group consisting of stearic acid, palmitic acid, and myristic acid. 
     
     
         44 . the composition of  claim 43  wherein the fatty acid is myristic acid. 
     
     
         45 . the composition of  claim 42  wherein the fatty acid is myristic acid. 
     
     
         46 . The composition of  claim 35 , wherein the one or more excipients comprises one or more wax or wax-like substances. 
     
     
         47 . The composition of  claim 46 , wherein the one or more wax or wax-like substances are selected from the group consisting of beeswax, glycowax, castor wax, carnauba wax, paraffins, microcrystalline wax, and candelilla wax. 
     
     
         48 . The composition of  claim 47 , wherein the wax or wax-like substances are beeswax and carnauba wax. 
     
     
         49 . The composition of  claim 35 , wherein the drug prone to abuse is an opioid analgesic. 
     
     
         50 . The composition of  claim 49  wherein the opioid analgesic is oxycodone, morphine, codeine, oxymorphone, hydromorphone, or a salt thereof. 
     
     
         51 . The composition of  claim 50  wherein the opioid analgesic is oxycodone or a salt thereof. 
     
     
         52 . The composition of  claim 35  wherein the one or more excipients comprise one or more fatty acids and one or more waxes substances. 
     
     
         53 . The composition of  claim 52  wherein one or more fatty acids is selected from the group consisting of linoleic acid, octanoic acid, capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, and oleic acid and the one or more waxes substances are selected from the group consisting of beeswax, glycowax, castor wax, carnauba wax, paraffins, microcrystalline wax, and candelilla wax. 
     
     
         54 . The composition of  claim 53  wherein the fatty acid is myristic acid and the waxes are beeswax and carnauba wax. 
     
     
         55 . The composition of  claim 52 , wherein the drug prone to abuse is an opioid analgesic. 
     
     
         56 . The composition of  claim 55  wherein the opioid analgesic is oxycodone, morphine, codeine, oxymorphone, hydromorphone, or a salt thereof. 
     
     
         57 . The composition of  claim 56  wherein the opioid analgesic is oxycodone or a salt thereof. 
     
     
         58 . The composition of  claim 54  wherein the opioid analgesic is oxycodone or a salt thereof. 
     
     
         59 . A method of treating pain comprising administering to a human subject in need thereof, a therapeutically effective amount of the composition of  claim 43 . 
     
     
         60 . A method of making the tamper resistant pharmaceutical composition of  claim 35 , comprising:
 (a) dispersing or dissolving a drug prone to abuse in a mixture comprising one or more excipients selected from fats, fatty substances, waxes, wax-like substances or mixtures thereof; and   (b) forming a plurality of particles wherein the drug is present as a solid dispersion or solid solution within the particles and wherein the particles have a D[0.5] between about 200 microns and about 400 microns and a D[0.90]between about 400 microns to about 700 microns.   
     
     
         61 . The method of  claim 60 , wherein said process comprises a spinning disc atomization process. 
     
     
         62 . The method of  claim 60  wherein oxycodone base is dispersed or dissolved in the mixture comprising one or more excipients selected from fats, fatty substances, waxes, wax-like substances or mixtures thereof.