US2016185788A1PendingUtilityA1

Process for preparing oxycodone compositions

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Assignee: PURDUE PHARMA LPPriority: Mar 30, 2004Filed: Mar 4, 2016Published: Jun 30, 2016
Est. expiryMar 30, 2024(expired)· nominal 20-yr term from priority
Inventors:Robert ChapmanLonn S. RiderQi-Zhong HongDonald J. KyleRobert Kupper
A61P 29/00A61P 25/04C07D 489/04A61K 31/485C07D 489/02A61K 9/0053C07D 489/08A61K 9/14A61K 9/4833A61K 9/20A61K 9/48A61K 47/30A61K 9/2095
67
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Claims

Abstract

In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.

Claims

exact text as granted — not AI-modified
1 - 79 . (canceled) 
     
     
         80 . A process for preparing an oxycodone salt composition comprising less than 100 ppm 14-hydroxycodeinone, which process comprises steps of:
 (a) titrating an oxycodone base composition comprising 8α,14-dihydroxy-7,8-dihydrocodeinone with an acid under conditions sufficient to provide an oxycodone salt composition comprising less than 100 ppm 14-hydroxycodeinone; and   (b) isolating the oxycodone salt composition comprising less than 100 ppm 14-hydroxycodeinone.   
     
     
         81 . The process of  claim 80 , wherein the conditions affect acid catalyzed dehydration consisting of conversion of the 8α,14-dihydroxy-7,8-dihydrocodeinone to 14-hydroxycodeinone. 
     
     
         82 . The process of  claim 81 , wherein the conditions reduce the rate of dehydration of the 8α,14-dihydroxy-7,8-dihydrocodeinone to the 14-hydroxycodeinone. 
     
     
         83 . The process of  claim 80 , wherein at least some of the 8α,14-dihydroxy-7,8-dihydrocodeinone is dehydrated to 14-hydroxycodeinone during the process. 
     
     
         84 . The process of  claim 82 , comprising preferentially removing at least some of the 14-hydroxycodeinone. 
     
     
         85 . The process of  claim 80 , wherein the acid comprises hydrochloric acid. 
     
     
         86 . The process of  claim 80 , wherein step (a) is performed under reducing conditions. 
     
     
         87 . The process of  claim 80 , wherein the process is for preparing an oxycodone hydrochloride salt composition. 
     
     
         88 . The process of  claim 80 , wherein the process is for preparing an oxycodone hydrochloride active pharmaceutical ingredient composition. 
     
     
         89 . The process of  claim 80 , wherein the oxycodone salt composition is isolated by a process comprising crystallization. 
     
     
         90 . The process of  claim 80 , wherein the oxycodone salt composition in step (a) comprises 0.25 ppm or more 14-hydroxycodeinone. 
     
     
         91 . The process of  claim 80 , wherein the oxycodone salt composition in step (a) comprises 1 ppm or more 14-hydroxycodeinone. 
     
     
         92 . The process of  claim 80 , wherein the oxycodone salt composition in step (a) comprises 5 ppm or more 14-hydroxycodeinone. 
     
     
         93 . A process for preparing an oxycodone salt composition, which process comprises steps of:
 (a) titrating an oxycodone base composition comprising 8α,14-dihydroxy-7,8-dihydrocodeinone with an acid under conditions sufficient to provide an oxycodone salt composition that is substantially free of 14-hydroxycodeinone; and   (b) isolating the oxycodone salt composition that is substantially free of 14-hydroxycodeinone.   
     
     
         94 . The process of  claim 93 , wherein the conditions affect acid catalyzed dehydration consisting of conversion of the 8α,14-dihydroxy-7,8-dihydrocodeinone to 14-hydroxycodeinone. 
     
     
         95 . The process of  claim 94 , wherein the conditions reduce the rate of dehydration of the 8α,14-dihydroxy-7,8-dihydrocodeinone to the 14-hydroxycodeinone. 
     
     
         96 . The process of  claim 93 , wherein at least some of the 8α,14-dihydroxy-7,8-dihydrocodeinone is dehydrated to 14-hydroxycodeinone during the process. 
     
     
         97 . The process of  claim 96 , comprising preferentially removing at least some of the 14-hydroxycodeinone. 
     
     
         98 . The process of  claim 93 , wherein the acid comprises hydrochloric acid. 
     
     
         99 . The process of  claim 93 , wherein step (a) is performed under reducing conditions. 
     
     
         100 . The process of  claim 93 , wherein the process is for preparing an oxycodone hydrochloride salt composition. 
     
     
         101 . The process of  claim 93 , wherein the process is for preparing an oxycodone hydrochloride active pharmaceutical ingredient composition. 
     
     
         102 . The process of  claim 93 , wherein the oxycodone salt composition is isolated by a process comprising crystallization. 
     
     
         103 . The process of  claim 93 , wherein the isolated oxycodone salt composition comprises less than 25 ppm 14-hydroxycodeinone. 
     
     
         104 . The process of  claim 103 , wherein the isolated oxycodone salt composition comprises less than 15 ppm 14-hydroxycodeinone. 
     
     
         105 . The process of  claim 104 , wherein the isolated oxycodone salt composition comprises less than 10 ppm 14-hydroxycodeinone. 
     
     
         106 . The process of  claim 93 , wherein the isolated oxycodone salt composition comprises 0.25 ppm or more 14-hydroxycodeinone. 
     
     
         107 . The process of  claim 106 , wherein the oxycodone salt composition comprises 0.5 ppm or more 14-hydroxycodeinone. 
     
     
         108 . The process of  claim 107 , wherein the oxycodone salt composition comprises 1 ppm or more 14-hydroxycodeinone. 
     
     
         109 . The process of  claim 108 , wherein the oxycodone salt composition comprises 5 ppm or more 14-hydroxycodeinone.

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