Orally administered analgesic compositions containing nalbuphine

Abstract

The present invention provides orally administered pharmaceutical compositions which contains an effective amount of free base or pharmaceutically acceptable salts of nalbuphine and/or nalbuphine ester, an oily substance, and a solubility-assisting agent. The oily substance is preferably sesame oil. The solubility-assisting agent is preferably benzyl benzoate. The pharmaceutical composition is useful as an analgesic. The compositions achieves a much higher bioavailability rate and yields much longer lasting effects on nalbuphine than other nalbuphine products currently in the market.

We claim:  
     
         1 . A pharmaceutical composition comprising: as an active ingredient, an effective amount of free base or pharmaceutically acceptable salts of nalbuphine or nalbuphine ester; 
 an oily substance; and    a solubility-assisting agent;    wherein said pharmaceutical composition is an orally administered composition.    
     
     
         2 . The pharmaceutical composition according to  claim 1 , wherein said nalbuphine ester is nalbuphine monoester or nalbuphine polyester.  
     
     
         3 . The pharmaceutical composition according to  claim 2 , wherein said nalbuphine monoester is at least one selected from the group consisting of nalbuphine propionate, nalbuphine pivalate, nalbuphine enanthate, nalbuphine decanoate, nalbuphine erucicate, nalbuphine arachidate, and nalbuphine benzoate.  
     
     
         4 . The pharmaceutical composition according to  claim 2 , wherein said nalbuphine polyester is at least one selected from the group consisting of adipoyl dinalbuphine ester, sebacoyl dinalbuphine ester, 1,3-cyclohexane diacid dinalbuphine ester, docosanodic dinalbuphine ester, 3,3-dimethylglutaric diacid dinalbuphine ester, trinalbuphine trimesoyl ester, 1,3,5-cyclohexane triacid trinalbuphine ester, and pyromellitoyl tetranalbuphine ester.  
     
     
         5 . The pharmaceutical composition according to  claim 2 , wherein said nalbuphine polyester is sebacoyl dinalbuphine ester (SDN).  
     
     
         6 . The pharmaceutical composition according to  claim 1 , wherein said oily substance is vegetable oil.  
     
     
         7 . The pharmaceutical composition according to  claim 6 , wherein said vegetable oil is sesame oil.  
     
     
         8 . The pharmaceutical composition according to  claim 1 , wherein said solubility-assisting agent is benzyl benzoate  
     
     
         9 . The pharmaceutical composition according to  claim 1 , wherein said nalbuphine ester is about 1% to 15% by weight of said composition.  
     
     
         10 . The pharmaceutical composition according to  claim 9 , wherein said nalbuphine ester is about 10% by weight of said composition.  
     
     
         11 . The pharmaceutical composition according to  claim 1 , wherein said oily substance is about 30% to 90% by weight of said composition.  
     
     
         12 . The pharmaceutical composition according to  claim 9 , wherein said wherein said oil substance is about 55% by weight of the composition.  
     
     
         13 . The pharmaceutical composition according to  claim 1 , wherein said solubility-assisting agent is about 5% to 50% by weight of the composition.  
     
     
         14 . The pharmaceutical composition according to  claim 11 , wherein said solubility-assisting agent is about 45% by weight of said composition.  
     
     
         15 . A method for treating patients with pain comprising orally administering the pharmaceutical composition according to  claim 1  to patients.  
     
     
         16 . The method according to  claim 15 , wherein said pain is caused by at least one selected from the group consisting of cardiac surgery, pulmonary surgery, osteopathia surgery, obstetrical surgery, burn injury, and terminal stage of cancer.  
     
     
         17 . An analgesic agent comprising the pharmaceutical composition of  claim 1.