TAMPER RESISTANT DOSAGE FORMS
The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.
1 - 193 . (canceled)
194 . A pharmaceutical tablet comprising an extended release matrix formulation, the extended release matrix formulation comprising:
(1) at least one active agent selected from opioid analgesics;
(2) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000;
(3) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of less than 1,000,000;
wherein said formulation comprises at least about 80% (by wt) of polyethylene oxide and at least about 50% (by wt) of polyethylene oxide having, based on rheological measurements, a molecular weight of at least 1,000,000 and
wherein said formulation has a cracking force of at least 110 N, at least 120 N, at least 130 N, or at least 140 N, when subjected to an indentation test.
195 . A pharmaceutical tablet comprising an extended release matrix formulation, the extended release matrix formulation comprising:
(1) at least one active agent selected from opioid analgesics;
(2) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000;
(3) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of less than 1,000,000; and
wherein said formulation comprises at least about 80% (by wt) of polyethylene oxide and at least about 50% (by wt) of polyethylene oxide having, based on rheological measurements, a molecular weight of at least 1,000,000;
wherein said formulation has a penetration depth to crack distance of at least 1.0 mm, at least 1.2 mm, at least 1.4 mm, or at least 1.6 mm, when subjected to an indentation test.
196 . A pharmaceutical tablet comprising an extended release matrix formulation, the extended release matrix formulation comprising:
(1) at least one active agent selected from opioid analgesics;
(2) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000;
(3) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of less than 1,000,000;
wherein said formulation comprises at least about 80% (by wt) of polyethylene oxide and at least about 50% (by wt) of polyethylene oxide having, based on rheological measurements, a molecular weight of at least 1,000,000 and
wherein said formulation is capable of resisting a work of at least 0.06 J without cracking.
197 . A pharmaceutical tablet comprising an extended release matrix formulation, the extended release matrix formulation comprising:
(1) at least one active agent selected from opioid analgesics;
(2) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000;
(3) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of less than 1,000,000; and
wherein said formulation comprises at least about 80% (by wt) of polyethylene oxide and at least about 50% (by wt) of polyethylene oxide having, based on rheological measurements, a molecular weight of at least 1,000,000 and
wherein said formulation has (a) a cracking force of at least 110 N, at least 120 N, at least 130 N, or at least 140 N, when subjected to an indentation test; (b) a penetration depth to crack distance of at least 1.0 mm, at least 1.2 mm, more at least 1.4 mm, or at least 1.6 mm, when subjected to an indentation test; and (c) is capable of resisting a work of at least 0.06 J without cracking.
198 . (canceled)
199 . The pharmaceutical tablet according to claim 194 having a density of less than 1.20 g/cm 3 or less than 1.19 g/cm 3 .
200 . The pharmaceutical tablet according to claim 195 having a density of less than 1.20 g/cm 3 or less than 1.19 g/cm 3 .
201 . The pharmaceutical tablet according to claim 196 having a density of less than 1.20 g/cm 3 or less than 1.19 g/cm 3 .
202 . The pharmaceutical tablet according to claim 197 having a density of less than 1.20 g/cm 3 or less than 1.19 g/cm 3 .
203 . The pharmaceutical tablet according to claim 194 , wherein the at least one active agent is selected from the group consisting of oxycodone, a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, and mixtures of any of the foregoing.
204 . The pharmaceutical tablet according to claim 195 , wherein the at least one active agent is selected from the group consisting of oxycodone, a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, and mixtures of any of the foregoing.
205 . The pharmaceutical tablet according to claim 196 , wherein the at least one active agent is selected from the group consisting of oxycodone, a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, and mixtures of any of the foregoing.
206 . The pharmaceutical tablet according to claim 197 , wherein the at least one active agent is selected from the group consisting of oxycodone, a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, and mixtures of any of the foregoing.
207 . The pharmaceutical tablet according to claim 194 , wherein the at least one active agent is selected from the group consisting of codeine, morphine, oxycodone, hydrocodone, hydromorphone, oxymorphone, pharmaceutically acceptable salts thereof, hydrates thereof, solvates thereof, and mixtures of any of the foregoing.
208 . The pharmaceutical tablet according to claim 195 , wherein the at least one active agent is selected from the group consisting of codeine, morphine, oxycodone, hydrocodone, hydromorphone, oxymorphone, pharmaceutically acceptable salts thereof, hydrates thereof, solvates thereof, and mixtures of any of the foregoing.
209 . The pharmaceutical tablet according to claim 196 , wherein the at least one active agent is selected from the group consisting of codeine, morphine, oxycodone, hydrocodone, hydromorphone, or oxymorphone or pharmaceutically acceptable salts, hydrates and solvates thereof, and mixtures of any of the foregoing.
210 . The pharmaceutical tablet according to claim 197 , wherein the at least one active agent is selected from the group consisting of codeine, morphine, oxycodone, hydrocodone, hydromorphone, or oxymorphone or pharmaceutically acceptable salts, hydrates and solvates thereof, and mixtures of any of the foregoing.
211 . The pharmaceutical tablet according to claim 203 , wherein the dosage form comprises 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 45 mg, 60 mg, 80 mg, 90 mg, 120 mg or 160 mg of oxycodone hydrochloride.
212 . The pharmaceutical tablet according to claim 204 , wherein the dosage form comprises 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 45 mg, 60 mg, 80 mg, 90 mg, 120 mg or 160 mg of oxycodone hydrochloride.
213 . The pharmaceutical tablet according to claim 205 , wherein the dosage form comprises 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 45 mg, 60 mg, 80 mg, 90 mg, 120 mg or 160 mg of oxycodone hydrochloride.
214 . The pharmaceutical tablet according to claim 206 , wherein the dosage form comprises 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 45 mg, 60 mg, 80 mg, 90 mg, 120 mg or 160 mg of oxycodone hydrochloride.
215 . The pharmaceutical tablet according to claim 194 , which is in the form of a tablet formed h direct compression and cured by at least subjecting said tablet to a temperature of at least about 60° C. or at least about 62° C. for a time period of at least about 1 minute, at least about 5 minutes, or at least about 15 minutes.
216 . The pharmaceutical tablet according to claim 195 , which is in the form of a tablet formed by direct compression and cured by at least subjecting said tablet to a temperature of at least about 60° C. or at least about 62° C. for a time period of at least about 1 minute, at least about 5 minutes, or at least about 15 minutes.
217 . The pharmaceutical tablet according to claim 196 , which is in the form of a tablet formed by direct compression of and cured by at least subjecting said tablet to a temperature of at least about 60° C. or at least about 62° C. for a time period of at least about 1 minute, at least about 5 minutes, or at least about 15 minutes.
218 . The pharmaceutical tablet according to claim 197 , which is in the form of a tablet formed by direct compression of the and cured by at least subjecting said tablet to a temperature of at least about 60° C. or at least about 62° C. for a time period of at least about 1 minute, at least about 5 minutes, or at least about 15 minutes.
219 . The pharmaceutical tablet according to claim 211 , wherein the tablet, when tested in a comparative clinical study, is bioequivalent to the commercial product OxyContin™.
220 . The pharmaceutical tablet according to claim 212 , wherein the tablet, when tested in a comparative clinical study, is bioequivalent to the commercial product OxyContin™.
221 . The pharmaceutical tablet according to claim 213 , wherein the tablet, when tested in a comparative clinical study, is bioequivalent to the commercial product OxyContin™.
222 . The pharmaceutical tablet according to claim 214 , wherein the tablet, when tested in a comparative clinical study, is bioequivalent to the commercial product OxyContin™.
223 . The pharmaceutical tablet according to claim 194 , wherein the composition comprises at least about 80% (by wt) polyethylene oxide having, based on theological measurements, an approximate molecular weight of at least 1,000,000.
224 . The pharmaceutical tablet according to claim 195 , wherein the composition comprises at least about 80% (by wt) polyethylene oxide having, based on theological measurements, an approximate molecular weight of at least 1,000,000.