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.

1 - 40 . (canceled) 
     
     
         41 . A controlled release oral dosage form comprising:
 a matrix comprising (i) an opioid agonist; and   (ii) a gelling agent selected from the group consisting of polyethylene oxide, a cellulosic polymer and a combination thereof, the gelling agent in an effective amount to impart a viscosity unsuitable for parenteral administration when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid;   the dosage form having a ratio of gelling agent to opioid agonist from about 40:1 to about 1:40;   the matrix providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.   
     
     
         42 . The controlled release oral dosage form of  claim 41 , wherein the cellulosic polymer is hydroxypropylmethylcellulose. 
     
     
         43 . The controlled release oral dosage form of  claim 42 , wherein the gelling agent comprises polyethylene oxide and hydroxypropylmethylcellulose. 
     
     
         44 . The controlled release dosage form of  claim 43 , wherein the gelling agent further comprises polyethylene glycol. 
     
     
         45 . The controlled release dosage form of  claim 44 , further comprising alpha-tocopherol. 
     
     
         46 . The controlled release dosage form of  claim 44 , wherein the matrix is a compressed tablet. 
     
     
         47 . The controlled release dosage form of  claim 46 , wherein the tablet is coated with a film. 
     
     
         48 . The controlled release dosage form of  claim 47 , wherein the film is a seal coat. 
     
     
         49 . The controlled release dosage form of  claim 47 , wherein the film comprises polyethylene glycol. 
     
     
         50 . The controlled release dosage form of  claim 47 , wherein the film comprises polyvinyl alcohol. 
     
     
         51 . The controlled release dosage form of  claim 47 , wherein the film comprises talc. 
     
     
         52 . The controlled release oral dosage form of  claim 44 , wherein the gelling agent is in an effective amount to impart a viscosity of at least about 10 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid. 
     
     
         53 . The controlled release oral dosage form of  claim 44 , wherein the gelling agent is in an effective amount to impart a viscosity of at least about 60 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid. 
     
     
         54 . The controlled release oral dosage form of  claim 44 , wherein the gelling agent is in an effective amount to impart a viscosity of at least about 120 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid. 
     
     
         55 . The controlled release oral dosage form of  claim 44 , wherein the gelling agent is in an effective amount to impart a viscosity from about 120 cP to about 5,000 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid. 
     
     
         56 . The controlled release oral dosage form of  claim 44 , wherein the imparted viscosity makes the tampered dosage form difficult to pull into an insulin syringe. 
     
     
         57 . The controlled release oral dosage form of  claim 43 , wherein the imparted viscosity makes the tampered dosage form difficult to pull into an insulin syringe as compared to the same dosage form having an inert pharmaceutically acceptable excipient in place of the gelling agent. 
     
     
         58 . The controlled release oral dosage form of  claim 44 , wherein the imparted viscosity makes the tampered dosage form difficult to pull into an insulin syringe as compared to the same dosage form having an inert pharmaceutically acceptable excipient in place of the gelling agent. 
     
     
         59 . The controlled release oral dosage form of  claim 44 , wherein a tampered dosage form cannot be filled into an insulin syringe without picking up pockets of air. 
     
     
         60 . The controlled release oral dosage form of  claim 44 , wherein a tampered dosage form has a milk like color. 
     
     
         61 . The controlled release oral dosage form of  claim 44 , wherein the aqueous liquid is water. 
     
     
         62 . The controlled release oral dosage form of  claim 44 , wherein the viscosity is imparted when the dosage form is subjected to tampering by crushing and dissolution in the aqueous liquid. 
     
     
         63 . The controlled release oral dosage form of  claim 44 , wherein the viscosity is imparted when the dosage form is subjected to tampering by dissolution in the aqueous liquid at ambient temperature. 
     
     
         64 . The controlled release oral dosage form of  claim 44 , wherein the viscosity is imparted when the dosage form is subjected to tampering by dissolution in the aqueous liquid with heating greater than 45° C. 
     
     
         65 . The controlled release dosage form of  claim 44 , wherein the polyethylene oxide has a weight average molecular weight from about 100,000 daltons to about 1,000,000 daltons. 
     
     
         66 . The controlled release dosage form of  claim 44 , wherein the polyethylene oxide has a weight average molecular weight from about 1,000,000 daltons to about 10,000,000 daltons. 
     
     
         67 . The controlled release dosage form of  claim 44 , wherein the ratio of polyethylene oxide to opioid agonist is from about 1:1 to about 40:1. 
     
     
         68 . The controlled release dosage form of  claim 44 , wherein the ratio of polyethylene oxide to opioid agonist is from about 1:1 to about 30:1. 
     
     
         69 . A controlled release oral dosage form comprising:
 a mixture of (i) from about 75 ng to about 750 mg of an opioid agonist hydrochloride salt;   (ii) polyethylene oxide,   (iii) hydroxypropylmethylcellulose; and   (iv) polyethylene glycol;   the dosage form of imparting a viscosity unsuitable for parenteral administration when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid;   the mixture compressed into a tablet and coated with a film;   the dosage form having a ratio of polyethylene oxide to opioid agonist hydrochloride salt from about 40:1 to about 1:40;   the mixture providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.   
     
     
         70 . A controlled release oral dosage form comprising:
 (i) from about 75 ng to about 750 mg of an opioid agonist hydrochloride salt;   (ii) polyethylene oxide,   (iii) hydroxypropylmethylcellulose;   (iv) polyethylene glycol;   (v) alpha-tocopherol;   (vi) polyvinyl alcohol; and   (vii) talc;   the dosage form imparting a viscosity unsuitable for parenteral administration when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid;   the dosage form having a ratio of polyethylene oxide to opioid agonist hydrochloride salt from about 40:1 to about 1:40;   the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.