Use of a combination of morphine and at least one opiate antagonist to treat opiate dependency and prevent non-oral opiate abuse among opiate addicts

Abstract

The present invention relates to the use of an inseparable combination of morphine and at least one opiate antagonist with a bioavailability of less than 5% on oral administration for producing a medicament to be administered orally for treatment of opiate dependency in humans and to the use of an inseparable combination of an opiate and at least one opiate antagonists with a bioavailability of less than 5% on oral administration for producing a medicament to be administered orally for prevention of non-oral opiate abuse in opiate addicts.

1 . A process of substitution therapy among opiate or heroin addicts comprising preparing a non-separable combination of morphine, or its physiologically acceptable salts, and at least one opiate antagonist, or its physiologically acceptable salts, wherein the opiate antagonist or its physiologically acceptable salts have a bioavailability of less than 5% when the non-separable combination is administered orally, and administering the non-separable combination only orally to the addicts. 
   
   
       2 . The process according to  claim 1 , further comprising alleviating or preventing opiate-specific side-effects of the addicts administering the combination to the addicts. 
   
   
       3 . The process according to  claim 1 , characterized in that the opiate antagonist comprises naloxone. 
   
   
       4 . The process according to  claim 1  wherein, the combination is selected from the group consisting of the morphine is retarded and the at least one opiate antagonist is retarded, the morphine is retarded and the at least one opiate antagonist is non-retarded, the morphine is non-retarded and the at least one opiate antagonist is retarded, and the morphine is non-retarded and the at least one opiate antagonist is non-retarded. 
   
   
       5 . The process according to enema  claim 1 , characterized in that the morphine is adsorbed on a polymer and embedded in a matrix or the morphine is suspended in an ethyl cellulose polymer. 
   
   
       6 . The process according to  claim 1 , characterized in that the substitute therapy is administered among heroin addicts. 
   
   
       7 . The process according to  claim 1 , characterized in that the combination is administered once or twice daily. 
   
   
       8 . The process according to  claim 1 , characterized in that the morphine is used in the form of morphine hydrochloride or morphine sulphate pentahydrate. 
   
   
       9 . The process according to  claim 3 , characterized in that the naloxone is used in the form of naloxone hydrochloride or naloxone hydrochloride dihydrate. 
   
   
       10 . The process according to  claim 1 , characterized in that the combination contains 100 mg to 2000 mg of retarded morphine. 
   
   
       11 . The process according to  claim 3 , characterized in that the combination contains 0.1 to 10 mg of naloxone per 100 mg of retarded morphine. 
   
   
       12 . (canceled) 
   
   
       13 . The process of  claim 1  wherein the combination comprises retarded morphine and non-retarded naloxone present as a mixture of granules, wherein the granules preferably have grain sizes of 0.1 mm to 2 mm. 
   
   
       14 . The process of  claim 3 , characterized in that the morphine comprises morphine sulphate pentahydrate and the naloxone comprises naloxone hydrochloride or naloxone hydrochloride dihydrate. 
   
   
       15 . The process of  claim 1  wherein the opiate antagonist consists essentially of naloxone. 
   
   
       16 . A process for prevention of non-oral opiate abuse among opiate addicts comprising preparing a non-separable combination of morphine, or its physiologically acceptable salts, and at least one opiate antagonist, or its physiologically acceptable salts, wherein the opiate antagonist or its physiologically acceptable salts have a bioavailability of less than 5% when the non-separable combination is administered orally, and administering the non-separable combination only orally to the addicts. 
   
   
       17 . A process for manufacturing a medicinal product for substitution therapy comprising preparing a non-separable combination of morphine, or its physiologically acceptable salts, and at least one opiate antagonist, or its physiologically acceptable salts, wherein the opiate antagonist or its physiologically acceptable salts have a bioavailability of less than 5% when the non-separable combination is administered orally.