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 a mixture of (i) hydrocodone or a pharmaceutically acceptable salt thereof; and   (ii) a gelling agent comprising polyethylene oxide and a cellulosic polymer, 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 ml to about 10 ml of an aqueous liquid;   the matrix having a ratio of gelling agent to hydrocodone or pharmaceutically acceptable salt thereof from about 40:1 to about 1:40; and   the matrix providing a therapeutic effect for at least about 24 hours when orally administered to a human patient.   
     
     
         42 . The controlled release oral dosage form of  claim 41 , wherein the cellulosic polymer is selected from the group consisting of microcrystalline cellulose, sodium carboxymethylcellulose, methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose. 
     
     
         43 . The controlled release oral dosage form of  claim 42 , wherein the cellulosic polymer comprises microcrystalline cellulose. 
     
     
         44 . The controlled release oral dosage form of  claim 42 , wherein the cellulosic polymer comprises hydroxypropylcellulose. 
     
     
         45 . The controlled release oral dosage form of  claim 42 , wherein the cellulosic polymer comprises hydroxypropylcellulose and microcrystalline cellulose. 
     
     
         46 . The controlled release oral dosage form of  claim 45 , wherein the gelling agent further comprises polyethylene glycol. 
     
     
         47 . The controlled release oral dosage form of  claim 46 , wherein the dosage form does not comprise a semi-permeable coating. 
     
     
         48 . The controlled release oral dosage form of  claim 47 , wherein the dosage form comprises a film coating. 
     
     
         49 . The controlled release oral dosage form of  claim 46 , wherein the hydrocodone or pharmaceutically acceptable salt thereof and the gelling agent are granulated and compressed into a tablet. 
     
     
         50 . The controlled release oral dosage form of  claim 46 , wherein the imparted viscosity makes the tampered dosage form difficult to pull into an insulin syringe. 
     
     
         51 . The controlled release oral dosage form of  claim 46 , 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. 
     
     
         52 . The controlled release oral dosage form of  claim 46 , wherein a tampered dosage form cannot be filled into an insulin syringe without picking up pockets of air. 
     
     
         53 . The controlled release oral dosage form of  claim 46 , wherein a tampered dosage form has a milk like color. 
     
     
         54 . The controlled release oral dosage form of  claim 46 , wherein the aqueous liquid is water. 
     
     
         55 . The controlled release oral dosage form of  claim 46 , wherein the viscosity is imparted when the dosage form is subjected to tampering by dissolution in about 1 ml to about 3 ml of aqueous liquid. 
     
     
         56 . The controlled release oral dosage form of  claim 46 , wherein the viscosity is imparted when the dosage form is subjected to tampering by crushing and dissolution in the aqueous liquid. 
     
     
         57 . The controlled release oral dosage form of  claim 46 , wherein the viscosity is imparted when the dosage form is subjected to tampering by dissolution in the aqueous liquid at ambient temperature. 
     
     
         58 . The controlled release oral dosage form of  claim 46 , 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. 
     
     
         59 . The controlled release oral dosage form of  claim 46 , wherein the gelling agent is in an effective amount to impart a viscosity of about 10 cP or more when the dosage form is subjected to tampering by dissolution in from about 0.5 ml to about 10 ml of an aqueous liquid. 
     
     
         60 . The controlled release oral dosage form of  claim 46 , 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 ml to about 10 ml of an aqueous liquid. 
     
     
         61 . The controlled release oral dosage form of  claim 46 , 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 ml to about 10 ml of an aqueous liquid. 
     
     
         62 . The controlled release oral dosage form of  claim 46 , 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 ml to about 10 ml of an aqueous liquid. 
     
     
         63 . The controlled release oral dosage form of  46 , wherein the hydrocodone or pharmaceutically acceptable salt thereof comprises hydrocodone bitartrate. 
     
     
         64 . The controlled release oral dosage form of  claim 63 , comprising from about 75 ng to about 750 mg hydrocodone bitartrate. 
     
     
         65 . The controlled release dosage form of  claim 46 , 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 46 , 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 46 , wherein the ratio of gelling agent to hydrocodone or pharmaceutically acceptable salt thereof is from about 1:1 to about 40:1. 
     
     
         68 . The controlled release dosage form of  claim 46 , wherein the ratio of gelling agent to hydrocodone or pharmaceutically acceptable salt thereof is from about 1:1 to about 30:1. 
     
     
         69 . A controlled release oral dosage form comprising:
 a matrix comprising compressed granules, the granules comprising (i) from about 75 ng to about 750 mg hydrocodone or a pharmaceutically acceptable salt thereof; and   (ii) a gelling agent comprising polyethylene oxide, hydroxypropylcellulose, and microcrystalline cellulose, the gelling agent in an effective amount to impart a viscosity of at least 10 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 ml to about 10 ml of an aqueous liquid;   the matrix having a ratio of gelling agent to hydrocodone or pharmaceutically acceptable salt thereof from about 30:1 to about 1:30;   the matrix providing a therapeutic effect for at least about 24 hours when orally administered to a human patient; and   the dosage form not comprising a semi-permeable coating.   
     
     
         70 . A controlled release oral dosage form comprising:
 a tablet comprising compressed granules, the granules comprising (i) from about 75 ng to about 750 mg hydrocodone or a pharmaceutically acceptable salt thereof; and   (ii) a gelling agent comprising polyethylene oxide, hydroxypropylcellulose, microcrystalline cellulose and polyethylene glycol, 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 ml to about 10 ml of an aqueous liquid;   the matrix having a ratio of gelling agent to hydrocodone or pharmaceutically acceptable salt thereof from about 1:1 to about 1:30;   the matrix providing a therapeutic effect for at least about 24 hours when orally administered to a human patient; and   the dosage form not comprising a semi-permeable coating.