Pharmaceutical Formulation Containing Gelling Agent
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 mixture of (i) from about 10 mg to about 160 mg oxycodone or a pharmaceutically acceptable salt thereof; and
(ii) a gelling agent 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;
the dosage form providing a mean minimum plasma concentration of oxycodone from about 3 to about 120 ng/ml from about 10 to about 14 hours after administration every 12 hours after repeated dosing through steady state conditions and 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 , providing a mean maximum plasma concentration of oxycodone from about 6 to about 240 ng/ml from a mean of about 2 to about 4.5 hours after administration.
43 . The controlled release oral dosage form of claim 41 , comprising (i) from about 10 to about 40 mg oxycodone hydrochloride, the dosage form providing a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration or (ii) from about 40 mg to about 160 mg oxycodone hydrochloride, the dosage form providing a mean maximum plasma concentration of oxycodone from about 60 to about 240 ng/ml from a mean of about 2 to about 4.5 hours after administration.
44 . The controlled release dosage form of claim 41 , wherein the gelling agent is selected from the group consisting of sugars, sugar derived alcohols, mannitol, sorbitol, starch, starch derivatives, cellulose derivatives, microcrystalline cellulose, sodium carboxymethyl cellulose, methylcellulose, ethyl cellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, attapulgites, bentonites, dextrins, alginates, carrageenan, gum tragacanth, gum acacia, guar gum, xanthan gum, pectin, gelatin, kaolin, lecithin, magnesium aluminum silicate, carbomers, carbopols, polyvinylpyrrolidone, polyethylene glycol, polyethylene oxide, polyvinyl alcohol, silicon dioxide, surfactants, mixed surfactant/wetting agent systems, emulsifiers, polymeric materials and mixtures thereof.
45 . The controlled release oral dosage form of claim 41 , wherein the gelling agent 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.
46 . The controlled release oral dosage form of claim 41 , 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.
47 . The controlled release oral dosage form of claim 41 , wherein the gelling agent is in an effective amount to impart a viscosity of at least about 375 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid.
48 . The controlled release oral dosage form of claim 41 , wherein the gelling agent is in an effective amount to impart a viscosity of at least about 2,000 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid.
49 . The controlled release oral dosage form of claim 41 , 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.
50 . 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.
51 . 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.
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 375 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 2,000 cP when the dosage form is subjected to tampering by dissolution in from about 0.5 to about 10 ml of an aqueous liquid.
54 . 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.
55 . The controlled release oral dosage form of claim 41 , comprising from about 10 mg to about 160 mg oxycodone hydrochloride.
56 . The controlled release oral dosage form of claim 44 , comprising from about 10 mg to about 160 mg oxycodone hydrochloride.
57 . The controlled release oral dosage form of claim 46 , comprising from about 10 mg to about 160 mg oxycodone hydrochloride.
58 . The controlled release oral dosage form of claim 49 , comprising from about 10 mg to about 160 mg oxycodone hydrochloride.
59 . The controlled release oral dosage form of claim 41 , wherein the viscosity is measured using a Brookfield Synchro-Lectric Viscometer.
60 . The controlled release oral dosage form of claim 44 , wherein the viscosity is measured using a Brookfield Synchro-Lectric Viscometer.
61 . The controlled release oral dosage form of claim 46 , wherein the viscosity is measured using a Brookfield Synchro-Lectric Viscometer.
62 . The controlled release oral dosage form of claim 49 , wherein the viscosity is measured using a Brookfield Synchro-Lectric Viscometer.
63 . The controlled release oral dosage form of claim 51 , wherein the ratio of gelling agent to oxycodone or pharmaceutically acceptable salt thereof is from about 1:40 to about 40:1.
64 . The controlled release oral dosage form of claim 51 , wherein the aqueous liquid is water.
65 . The controlled release oral dosage form of claim 51 , wherein the viscosity is imparted when the dosage form is subjected to tampering by dissolution in about 1 to about 3 ml of aqueous liquid.
66 . The controlled release oral dosage form of claim 65 , comprising from about 10 mg to about 80 mg oxycodone hydrochloride.
67 . The controlled release oral dosage form of claim 51 , wherein the viscosity is obtained when the dosage form is subjected to tampering by crushing and dissolution in the aqueous liquid.
68 . The controlled release oral dosage form of claim 51 , wherein the viscosity is obtained when the dosage form is subjected to tampering by dissolution in the aqueous liquid with heating greater than 45° C.
69 . The controlled release oral dosage form of claim 51 , further comprising acetaminophen.
70 . The controlled release oral dosage form of claim 51 , further comprising ibuprofen.