US2018064704A1PendingUtilityA1

Immediate release pharmaceutical compositions comprising oxycodone and naloxone

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Assignee: PURDUE PHARMA LPPriority: Mar 10, 2009Filed: Nov 7, 2017Published: Mar 8, 2018
Est. expiryMar 10, 2029(~2.6 yrs left)· nominal 20-yr term from priority
Inventors:Helen Kathleen DanagherGeoffrey Gerard HayesGerhard Josef HeunHassan MohammadMalcolm WaldenJonathon Whitehouse
A61P 43/00A61P 25/00A61P 25/04A61P 29/02A61K 9/2018A61K 9/2059A61K 9/0053A61K 31/485A61K 2300/00A61K 9/28A61K 9/20
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Claims

Abstract

The present invention pertains to oral immediate release pharmaceutical compositions suitable for treating patients suffering from pain comprising oxycodone and naloxone or their pharmaceutically acceptable salts.

Claims

exact text as granted — not AI-modified
1 . An oral immediate release pharmaceutical composition comprising at least oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof in about a 2:1 ratio (oxycodone or a pharmaceutically acceptable salt thereof: naloxone or a pharmaceutically acceptable salt thereof) by weight. 
     
     
         2 . An oral immediate release pharmaceutical composition of  claim 1 , wherein the pharmaceutically acceptable salt of oxycodone and wherein the pharmaceutically acceptable salt of naloxone are selected from the hydrochloride salts of oxycodone and naloxone. 
     
     
         3 . An oral immediate release pharmaceutical composition of  claim 2 , wherein the composition comprises oxycodone hydrochloride and naloxone hydrochloride as the sole pharmaceutically active agents. 
     
     
         4 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2  or  3 , wherein the formulation comprises an amount of oxycodone or a pharmaceutically acceptable salt thereof equivalent to about 1 mg to about 160 mg of oxycodone hydrochloride and an amount of naloxone or a pharmaceutically acceptable salt thereof equivalent to about 0.5 mg to about 80 mg of naloxone hydrochloride. 
     
     
         5 . An oral immediate release pharmaceutical composition of  claim 4 , wherein the formulation comprises an amount of oxycodone or a pharmaceutically acceptable salt thereof equivalent to about 2.5 mg to about 40 mg of oxycodone hydrochloride and an amount of naloxone or a pharmaceutically acceptable salt thereof equivalent to about 1.25 mg to about 20 mg of naloxone hydrochloride. 
     
     
         6 . An oral immediate release pharmaceutical composition of  claim 5 , wherein the formulation comprises an amount of oxycodone or a pharmaceutically acceptable salt thereof equivalent to about 2.5 mg to about 20 mg of oxycodone hydrochloride and an amount of naloxone or a pharmaceutically acceptable salt thereof equivalent to about 1.25 mg to about 10 mg of naloxone hydrochloride. 
     
     
         7 . An oral immediate release pharmaceutical composition of  claim 6 , wherein the formulation comprises about 2.5 mg to about 20 mg of oxycodone hydrochloride and about 1.25 mg to about 10 mg of naloxone hydrochloride. 
     
     
         8 . An oral immediate release pharmaceutical composition of  claim 7 , wherein the composition comprises oxycodone hydrochloride and naloxone hydrochloride as the sole pharmaceutically active agents. 
     
     
         9 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7  or  8 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧75% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧75% of naloxone or a pharmaceutically acceptable salt thereof by weight at 45 min. 
     
     
         10 . An oral immediate release pharmaceutical composition of  claim 9 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧80% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧80% of naloxone or a pharmaceutically acceptable salt thereof by weight at 45 min. 
     
     
         11 . An oral immediate release pharmaceutical composition of  claim 9  or  10 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧80% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧80% of naloxone or a pharmaceutically acceptable salt thereof by weight at 15 min. 
     
     
         12 . An oral immediate release pharmaceutical composition of  claim 11 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧90% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧90% of naloxone or a pharmaceutically acceptable salt thereof by weight at 15 min. 
     
     
         13 . An oral immediate release pharmaceutical composition of  claim 12 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧95% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧95% of naloxone or a pharmaceutically acceptable salt thereof by weight at 15 min. 
     
     
         14 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12  or  13 , wherein the composition is in the form of a tablet, of a capsule, of multiparticulates, of pellets, or of a liquid. 
     
     
         15 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13  or  14 , wherein the formulation comprises at least a diluents and optionally a disintegrant as pharmaceutically acceptable excipients. 
     
     
         16 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  13  or  14 , wherein the formulation comprises at least a disintegrant and optionally a diluents as pharmaceutically acceptable excipients. 
     
     
         17 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15  or  16 , wherein the formulation comprises about 2.5 mg to about 20 mg of oxycodone hydrochloride and about 1.25 mg to about 10 mg of naloxone hydrochloride in about a 2:1 ratio (oxycodone hydrochloride:naloxone hydrochloride) by weight, wherein the composition comprises oxycodone hydrochloride and naloxone hydrochloride as the sole pharmaceutically active agents, wherein the composition is in solid form, optionally in the form of a tablet, wherein the formulation comprises at least a disintegrant and optionally a diluent as pharmaceutically acceptable excipients and wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧80% of oxycodone hydrochloride by weight and ≧80% of naloxone hydrochloride by weight at 45 min. 
     
     
         18 . An oral immediate release pharmaceutical composition of  claim 17 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧95% of oxycodone hydrochloride by weight and ≧95% of naloxone hydrochloride by weight at 15 min. 
     
     
         19 . An oral immediate release pharmaceutical composition comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof, wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧90% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧90% of naloxone or a pharmaceutically acceptable salt thereof by weight at 15 min. 
     
     
         20 . An oral immediate release pharmaceutical composition according to  claim 19 , wherein the formulation releases in vitro, when measured using the Ph. Eur. Paddle Method at 100 rpm in 0.1 N hydrochloric acid at 37° C. and using UV detection at 230 nm, ≧95% of oxycodone or a pharmaceutically acceptable salt thereof by weight and ≧95% of naloxone or a pharmaceutically acceptable salt thereof by weight at 15 min. 
     
     
         21 . An oral immediate release pharmaceutical composition according to  claim 19  or  20 , wherein the pharmaceutical composition comprises an amounts of oxycodone or a pharmaceutically acceptable salt thereof equivalent to about 1 mg to 160 mg of oxycodone hydrochloride and an amount of naloxone or a pharmaceutically acceptable salt thereof equivalent to about 0.5 mg to about 80 mg of naloxone hydrochloride. 
     
     
         22 . An oral immediate release pharmaceutical composition according to  claim 19 ,  20  or  21 , wherein the pharmaceutical composition comprises oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof in about a 2:1 ratio (oxycodone or a pharmaceutically acceptable salt thereof, naloxone or a pharmaceutically acceptable salt thereof) by weight. 
     
     
         23 . An oral immediate release pharmaceutical composition according to  claim 19 ,  20 ,  21  or  22 , wherein the pharmaceutical composition is in solid form. 
     
     
         24 . An oral immediate release pharmaceutical composition according to  claim 19 ,  20 ,  21 ,  22  or  23 , wherein the pharmaceutical composition additionally comprises at least a disintegrant. 
     
     
         25 . An oral immediate release pharmaceutical composition according to  claim 19 ,  20 ,  21 ,  22 ,  23  or  24 , wherein the pharmaceutical composition comprises oxycodone hydrochloride and naloxone hydrochloride as the sole pharmaceutically active agents. 
     
     
         26 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15 ,  16 ,  17 ,  18 ,  19 ,  20 ,  21 ,  22 ,  23 ,  24 ,  25  or  26  for use in titrating patients suffering from pain. 
     
     
         27 . An oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15 ,  16 ,  17 ,  18 ,  19 ,  20 ,  21 ,  22 ,  23 ,  24 ,  25  or  26  for treating breakthrough pain in patients suffering from pain. 
     
     
         28 . Use of an oral immediate release pharmaceutical composition of any of claims,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15 ,  16 ,  17 ,  18 ,  19 ,  20 ,  21 ,  22 ,  23 ,  24 ,  25  or  26  in the manufacture of a medicament for titrating patients suffering from pain. 
     
     
         29 . Use of an oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15 ,  16 ,  17 ,  18 ,  19 ,  20 ,  21 ,  22 ,  23 ,  24 ,  25  or  26  in the manufacture of a medicament treating breakthrough pain in patients suffering from pain. 
     
     
         30 . Method of titrating a patient suffering from pain by administering an oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15 ,  16 ,  17 ,  18 ,  19 ,  20 ,  21 ,  22 ,  23 ,  24 ,  25  or  26 . 
     
     
         31 . Method of treating breakthrough pain in a patient suffering from pain by administering an oral immediate release pharmaceutical composition of any of  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6 ,  7 ,  8 ,  9 ,  10 ,  11 ,  12 ,  13 ,  14 ,  15 ,  16 ,  17 ,  18 ,  19 ,  20 ,  21 ,  22 ,  23 ,  24 ,  25  or  26 .

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