Claims for Patent: 12,246,094

Summary for Patent: 12,246,094

Title:	Tamper resistant dosage forms
Abstract:	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.
Inventor(s):	William H. McKenna, Richard O. Mannion, Edward P. O'Donnell, Haiyong H. Huang
Assignee:	Purdue Pharma LP , Purdue Pharmaceuticals LP
Application Number:	US18/603,884
Patent Claims:	1. A solid oral extended release dosage form, comprising: a shaped extended release matrix comprising from about 10 mg to about 160 mg oxycodone or a pharmaceutically acceptable salt thereof, and polyethylene oxide (PEO) having an approximate molecular weight of 4 million Da to 15 million Da based on rheological measurements, wherein the PEO comprises at least about 30% (by weight) of the total weight of the dosage form, wherein the extended release matrix is shaped to form a tablet and convection heated in a coating pan for a time period of at least about 5 minutes at a temperature of at least about 60° C. and thereafter cooled, and wherein the density of the shaped extended release matrix is equal to or less than about 1.20 g/cm3 as determined by Archimedes Principle using a liquid of known density (ρ0), and wherein the dosage form provides a mean maximum plasma concentration (Cmax) of oxycodone from about 6 ng/mL to about 240 ng/mL. 2. The solid oral extended release dosage form of claim 1, wherein a plurality of convection heated particles of PEO adhere to or fuse with each other within the matrix. 3. The solid oral extended release dosage form of claim 1, wherein the shaped extended release matrix further comprises magnesium stearate. 4. The solid oral extended release dosage form of claim 1, wherein the dosage form provides a dissolution rate, which when measured in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C., is between 12.5 and 55% (by wt) oxycodone or pharmaceutically acceptable salt thereof released after 1 hour, between 25 and 65% (by wt) oxycodone or pharmaceutically acceptable salt thereof released after 2 hours, between 45 and 85% (by wt) oxycodone or pharmaceutically acceptable salt thereof released after 4 hours and between 55 and 95% (by wt) oxycodone or pharmaceutically acceptable salt thereof released after 6 hours. 5. The solid oral extended release dosage form of claim 1, wherein the dosage form provides an in-vitro dissolution rate, when measured in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) comprising 40% ethanol at 37° C., characterized by the percent amount of oxycodone or pharmaceutically acceptable salt thereof released at 0.5 hours, that deviates no more than about 20% points 0.5 hours from the corresponding in-vitro dissolution rate measured in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C. without ethanol. 6. The solid oral extended release dosage form of claim 1, wherein the temperature is from about 62° C. to about 90° C. 7. The solid oral extended release dosage form of claim 1, wherein the temperature is from about 68° C. to about 85° C. 8. The solid oral extended release dosage form of claim 1, wherein the time period is from about 15 minutes to about 10 hours. 9. The solid oral extended release dosage form of claim 1, wherein the time period is from about 30 minutes to about 4 hours. 10. The solid oral extended release dosage form of claim 1, when subjected to a maximum force of about 196 N or about 439 N in a tablet hardness test, does not break. 11. The solid oral extended release dosage form of claim 1, wherein the tablet when subjected to an indentation test resists a work of at least about 0.06 J without cracking. 12. The solid oral extended release dosage form of claim 1, comprising oxycodone hydrochloride. 13. The solid oral extended release dosage form of claim 1, that provides a mean tmax of oxycodone at about 2 to about 6 hours. 14. The solid oral extended release dosage form of claim 1, further comprising a PEO having an approximate molecular weight of 100,000 Da to 900,000 Da based on rheological measurements. 15. The solid oral extended release dosage form of claim 1, wherein the total amount of PEO comprises at least about 65% (by wt) of the total weight of the dosage form. 16. The solid oral extended release dosage form of claim 1, wherein the total amount of PEO comprises at least about 80% (by wt) of the total weight of the dosage form. 17. A solid oral extended release dosage form comprising: an extended release matrix comprising from about 10 mg to about 160 mg oxycodone hydrochloride, magnesium stearate and polyethylene oxide (PEO) having an approximate molecular weight of 2 million Da to 15 million Da based on rheological measurements, wherein the PEO comprises at least about 30% (by weight) of the total weight of the dosage form; wherein the dosage form provides a mean maximum plasma concentration (Cmax) of oxycodone from about 6 ng/ml to about 240 ng/ml and wherein the density of the extended release matrix is equal to or less than about 1.20 g/cm3 as determined by Archimedes Principle using a liquid of known density (ρ0); wherein the extended release matrix is shaped to form a tablet and convection heated in a coating pan for a time period of at least about 5 minutes at a temperature of at least about 60° C. and thereafter cooled. 18. A solid oral extended release dosage form comprising: an extended release matrix comprising oxycodone hydrochloride, magnesium stearate and polyethylene oxide (PEO) having an approximate molecular weight of 2 million Da to 15 million Da based on rheological measurements; wherein the dosage form provides an in-vitro dissolution rate, when measured in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) comprising 40% ethanol at 37° C., characterized by the percent amount of oxycodone hydrochloride released at 0.5 hours, that deviates no more than about 20% points 0.5 hours from the corresponding in-vitro dissolution rate measured in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C. without ethanol and wherein the density of the extended release matrix is equal to or less than about 1.20 g/cm3 as determined by Archimedes Principle using a liquid of known density (ρ0); wherein the extended release matrix is shaped to form a tablet and convection heated in a coating pan for a time period of at least about 5 minutes at a temperature of at least about 60° C. and thereafter cooled. 19. A solid oral extended release dosage form, comprising: a shaped extended release matrix comprising oxycodone hydrochloride, magnesium stearate and polyethylene oxide (PEO) having an approximate molecular weight of 2 million Da to 15 million Da based on rheological measurements, wherein the PEO comprises at least about 30% (by weight) of the total weight of the dosage form, wherein the extended release matrix is shaped to form a tablet and convection heated in a coating pan for a time period of at least about 5 minutes at a temperature of at least about 60° C. and thereafter cooled, wherein the dosage form provides a dissolution rate, which when measured in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C., is between 12.5 and 55% (by wt) oxycodone hydrochloride released after 1 hour, between 25 and 65% (by wt) oxycodone hydrochloride released after 2 hours, between 45 and 85% (by wt) oxycodone hydrochloride released after 4 hours and between 55 and 95% (by wt) oxycodone hydrochloride released after 6 hours, and wherein the density of the extended release matrix is equal to or less than about 1.20 g/cm3 as determined by Archimedes Principle using a liquid of known density (ρ0).