Tamper resistant dosage forms

Patent metadata

Field	Value
Publication number	US-9492390-B2
Application number	US-201514729601-A
Country	US
Kind code	B2
Filing date	Jun 3, 2015
Priority date	Aug 25, 2006
Publication date	Nov 15, 2016
Grant date	Nov 15, 2016

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.

First claim

The invention claimed is:

1. A method of treating pain comprising administering to a patient in need thereof a cured shaped pharmaceutical tablet comprising:
(1) an opioid or a pharmaceutically acceptable salt thereof,
(2) at least one low molecular weight polyethylene oxide having, based on rheological measurements, an approximate molecular weight of less than 1,000,000, and
(3) at least one high molecular weight polyethylene oxide having, based on rheological measurements, an approximate molecular weight of 7,000,000; and
(4) at least one component selected from an additive and a coating;

wherein said tablet is prepared by a process comprising the steps of:
(a) combining said opioid or pharmaceutically acceptable salt thereof with each of said low molecular weight polyethylene oxide and said high molecular weight polyethylene oxide, and optionally said additive to form at least one blend;
(b) applying each said blend to form a shaped tablet;
(c) optionally applying said coating to the shaped tablet; and
(d) curing said shaped tablet by subjecting the shaped tablet to an air temperature from about 60 to about 90° C. for a duration about 15 minutes to about 10 hours,

wherein said cured shaped tablet comprises an extended release once-a-day tablet having at least 79% by weight, based upon the total weight of said uncoated tablet, of the total combined weight of said high and low molecular weight polyethylene oxides.

2. A method according to claim 1 , wherein said opioid or pharmaceutically acceptable salt comprises at least 2.4% by weight, based upon the total weight of said uncoated tablet.

3. A method according to claim 1 , wherein said duration in said curing step is 15 minutes to 90 minutes.

4. A method according to claim 1 , wherein said air temperature in said curing step is from 70 to 78° C.

5. A method according to claim 1 , wherein
said coating, when present, is applied at least one of before or after said curing step and said coating comprises a film coating, microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate, talc, silica, fumed silica, colloidal silica dioxide, calcium stearate, carnauba wax, stearic acid, stearyl alcohol, mineral oil, paraffin, glycerin, propylene glycol, polyethylene glycol, lactose, povidone, and combinations thereof, and
said additive, when present, comprises microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate, talc, silica, fumed silica, colloidal silica dioxide, calcium stearate, carnauba wax, stearic acid, stearyl alcohol, mineral oil, paraffin, glycerin, propylene glycol, polyethylene glycol, lactose, povidone, and combinations thereof.

6. A method of treating pain comprising administering to a patient in need thereof a cured shaped tablet comprising:
(1) hydrocodone or a pharmaceutically acceptable salt thereof,
(2) at least one low molecular weight polyethylene oxide having, based on rheological measurements, an approximate molecular weight of less than 1,000,000,
(3) at least one high molecular weight polyethylene oxide having, based on rheological measurements, an approximate molecular weight of 7,000,000; and
(4) at least one component selected from an additive and a coating;

wherein said tablet is prepared by a process comprising the steps of:
(a) combining said hydrocodone or pharmaceutically acceptable salt thereof with each of said low molecular weight polyethylene oxide and said high molecular weight polyethylene oxide, and optionally said additive, to form at least one blend;
(b) applying each said blend to form a shaped tablet;
(c) optionally applying said coating to the shaped tablet; and
(d) curing said shaped tablet by subjecting the shaped tablet to an air temperature from about 60 to about 90° C. for a duration about 15 minutes to about 10 hours,
wherein said cured shaped tablet comprises an extended release once-a-day tablet having at least 79% by weight, based upon the total weight of said uncoated tablet, of the total combined weight of said high and low molecular weight polyethylene oxides, and wherein said low molecular weight polyethylene oxide comprises at least 20% by weight, based upon the total weight of said uncoated tablet.

7. A method according to claim 6 , wherein, said air temperature in said curing step is from 70 to 78° C.

8. A method according to claim 6 , wherein
said coating, when present, is applied at least one of before or after said curing step and said coating comprises a film coating, microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate, talc, silica, fumed silica, colloidal silica dioxide, calcium stearate, carnauba wax, stearic acid, stearyl alcohol, mineral oil, paraffin, glycerin, propylene glycol, polyethylene glycol, lactose, povidone, and combinations thereof, and
said additive, when present, comprises microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate, talc, silica, fumed silica, colloidal silica dioxide, calcium stearate, carnauba wax, stearic acid, stearyl alcohol, mineral oil, paraffin, glycerin, propylene glycol, polyethylene glycol, lactose, povidone, and combinations thereof.

9. A method according to claim 6 , wherein said low molecular weight polyethylene oxide is at least 22% by weight and said high molecular weight polyethylene oxide is at least 50% by weight, based upon the total weight of said uncoated tablet.

10. A method according to claim 6 , wherein said tablet comprises at least one coating, and at least 2.4% by weight of hydrocodone or pharmaceutically acceptable salt thereof, based upon the total weight of said uncoated tablet.

11. A method according to claim 6 , wherein said tablet comprises at least one coating, and at least 5% by weight of hydrocodone or pharmaceutically acceptable salt thereof, based upon the total weight of said uncoated tablet.

12. A method according to claim 6 , wherein said tablet comprises at least one coating, and at least 10% by weight of hydrocodone or pharmaceutically acceptable salt thereof, based upon the total weight of said uncoated tablet.

13. A method according to claim 10 , wherein said cured shaped tablet comprises at least 80% by weight, based upon the total weight of said uncoated tablet, of said high and low molecular weight polyethylene oxides.

14. A method according to claim 10 , wherein, said air temperature in said curing step is from 70 to 78° C.

15. A method according to claim 10 , wherein said duration in said curing step is 15 minutes to 90 minutes.

16. A method according to claim 10 , wherein
said coating, when present, is applied at least one of before or after said curing step and said coating comprises a film coating, microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate, talc, silica, fumed silica, colloidal silica dioxide, calcium stearate, carnauba wax, stearic acid, stearyl alcohol, mineral oil, paraffin, glycerin, propylene glycol, polyethylene glycol, lactose, povidone, and combinations thereof, and
said additive, when present, comprises microcrystalline cellulose, hydroxypropyl cellulose, magnesium stearate, talc, silica, fumed silica, colloidal silica dioxide, calcium stearate, carnauba wax, stearic acid, stearyl alcohol, mineral oil, paraffin, glycerin, propylene glycol, polyethylene glycol, lactose, povidone, and combinations thereof.

17. A method according to claim 10 , wherein said air temperature in said curing step is from 70 to 78° C. and said duration in said curing step is 15 minutes to 90 minutes.

18. A method according to claim 11 , wherei

Assignees

• Purdue Pharma Lp
• Purdue Pharmaceuticals LP

Inventors

• Mckenna William H
• Mannion Richard O
• O'Donnell Edward P
• Huang Haiyong H

Classifications

• A61P29/02

  without antiinflammatory effect · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title