Pharmaceutical formulation containing gelling agent

Abstract

Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

What is claimed is  
     
         1 . A controlled release oral dosage form comprising: 
 a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients;    said dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid;    said dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.    
     
     
         2 . The controlled release oral dosage form of  claim 1 , wherein said excipient comprises a controlled release material.  
     
     
         3 . The controlled release oral dosage form of  claim 1 , wherein said gelling agent comprises a controlled release material.  
     
     
         4 . The controlled release oral dosage form of  claim 1 , wherein said drug is an opioid analgesic selected from the group consisting of levorphanol, meperidine, dihydrocodeine, dihydromorphine, oxymorphone, pharmaceutically acceptable salts thereof, and mixtures thereof.  
     
     
         5 . The controlled release oral dosage form of  claim 1 , wherein said drug is an opioid analgesic.  
     
     
         6 . The controlled release oral dosage form of  claim 5 , wherein said opioid analgesic is morphine or a pharmaceutically acceptable salt thereof.  
     
     
         7 . The controlled release oral dosage form of  claim 5 , wherein said opioid analgesic is hydromorphone or a pharmaceutically acceptable salt thereof.  
     
     
         8 . The controlled release oral dosage form of  claim 5 , wherein said opioid analgesic is hydrocodone or a pharmaceutically acceptable salt thereof.  
     
     
         9 . The controlled release oral dosage form of  claim 5 , wherein said opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.  
     
     
         10 . The controlled release oral dosage form of  claim 5 , wherein said opioid analgesic is codeine or a pharmaceutically acceptable salt thereof.  
     
     
         11 . The oral dosage form of  claim 1 , wherein said drug is selected from the group consisting of a tranquilizer, a CNS depressant, a CNS stimulant (e.g., methylphenidate or a pharmaceutically acceptable salt thereof), a sedative hypnotic, and combinations thereof.  
     
     
         12 . The controlled release oral dosage form of  claim 1 , wherein said ratio of said gelling agent to said drug is from about 1:40 to about 40:1.  
     
     
         13 . The controlled release oral dosage form of  claim 1 , wherein said ratio of said gelling agent to said drug is from about 1:1 to about 30:1.  
     
     
         14 . The controlled release oral dosage form of  claim 1 , wherein said ratio of said gelling agent to said drug is from about 2:1 to about 10:1.  
     
     
         15 . The controlled release oral dosage form of  claim 1 , wherein said gelling agent is selected from the group consisting of sugars, sugar derived alcohols, cellulose derivatives, gums, surfactants, emulsifying agents, and mixtures thereof.  
     
     
         16 . The controlled release oral dosage form of  claim 1 , wherein said gelling agent is selected from the group consisting of pectin, xanthan gum and combinations thereof.  
     
     
         17 . The controlled release oral dosage form of  claim 1 , wherein said aqueous liquid is water.  
     
     
         18 . The controlled release oral dosage form of  claim 1 , wherein said unsuitable viscosity is attained when about 1 to about 3 ml of aqueous liquid is mixed with the crushed dosage form.  
     
     
         19 . The controlled release oral dosage form of  claim 1 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 10 cP.  
     
     
         20 . The controlled release oral dosage form of  claim 1 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 60 cP.  
     
     
         21 . The controlled release oral dosage form of  claim 4 , further comprising an additional drug selected from the group consisting of an NSAID, a COX-2 inhibitor, acetaminophen, aspirin, an NMDA receptor antanalgesic, a drug that blocks a major intracellular consequence of NMDA-receptor activation, an antitussive, an expectorant, a decongestant, an antihistamine and mixtures thereof.  
     
     
         22 . A method of preventing abuse of an oral controlled release dosage form of a drug comprising: 
 preparing the dosage form with a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients;    said dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid;    said dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.    
     
     
         23 . The method of  claim 22 , wherein said excipient comprises a controlled release material.  
     
     
         24 . The method of  claim 22 , wherein said gelling agent comprises a controlled release material.  
     
     
         25 . The method of  claim 22 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 10 cP.  
     
     
         26 . The method of  claim 22 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 25 cP.  
     
     
         27 . The method of  claim 22 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 60 cP.  
     
     
         28 . The method of  claim 22 , wherein said drug is an opioid analgesic selected from the group consisting of of morphine, hydromorphone, hydrocodone, oxycodone, codeine, levorphanol, meperidine, dihydrocodeine, dihydromorphine, oxymorphone, pharmaceutically acceptable salts thereof and mixtures thereof.  
     
     
         29 . The method of  claim 22 , wherein said gelling agent is selected from the group consisting of sugars or sugar derived alcohols, cellulose derivatives, gums, surfactants, emulsifying agents, and mixtures thereof. comprises a controlled release material.  
     
     
         30 . A controlled release oral dosage form comprising: 
 a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients;    said dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid and thereafter heated;    said dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.    
     
     
         31 . A method of preventing abuse of an oral controlled release dosage form of a drug comprising: 
 preparing the dosage form with a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients;    said dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid and is thereafter heated;    said dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.    
     
     
         32 . A method of preventing diversion of an oral controlled release dosage form of a drug comprising: 
 preparing the dosage form with a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients:    said dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid;    said dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.    
     
     
         33 . The method of  claim 32 , wherein said excipient comprises a controlled release material.  
     
     
         34 . The method of  claim 32 , wherein said gelling agent comprises a controlled release material.  
     
     
         35 . The method of  claim 32 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 10 cP.  
     
     
         36 . The method of  claim 32 , wherein the addition of from about 0.5 to about 10 ml of said aqueous liquid causes said solubilized mixture to have a viscosity of at least about 25 cP.  
     
     
         37 . The method of  claim 32 , wherein said drug is a opioid analgesic selected from the group consisting of morphine, hydromorphone, hydrocodone, oxycodone, codeine, levorphanol, meperidine, dihydrocodeine, dihydromorphine, oxymorphone, pharmaceutically acceptable salts thereof and mixtures thereof.  
     
     
         38 . The method of  claim 32 , wherein said gelling agent is selected from the group consisting of sugars or sugar derived alcohols, cellulose derivatives, gums, surfactants, emulsifying agents, and mixtures thereof.  
     
     
         39 . A method of treating pain comprising: 
 administering to a patient a therapeutically effective amount of an opioid analgesic together with pharmaceutically acceptable excipients such that the dosage form provides effective pain relief for at least about 12 hours when orally administered to a human patient;    said dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for injection to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.    
     
     
         40 . A controlled release oral dosage form of comprising: 
 a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients;    and a gelling agent in an effective amount to impart a viscosity unsuitable for nasal absorption of the drug upon administration to the nasal passages after tampering;    said dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.