Denaturants for sympathomimetic amine salts

Abstract

The instant invention makes impractical the use of sympathomimetic amine compositions in illicit drug production. More specifically, the preparation of methamphetamine from the disclosed pseudoephedrine hydrochloride formulations is inhibited. The present invention defines pharmaceutical compositions comprising a sympathomimetic amine salt and at least one combination inhibitor, the combination inhibitor which acts both to interfere with the isolation of the sympathomimetic amine from the composition and to interfere with the conversion of the sympathomimetic amine to another pharmacologically active compound. The contemplated compositions may also include reaction and separation inhibitors in any mixture to assure maximum protection against the use of the sympathomimetic amine-containing compositions for illegal drug manufacture. The presence of the combination, reaction and separation inhibitors does not significantly alter the release of the sympathomimetic amine from the composition.

1 - 54 . (canceled)  
     
     
         55 . A pharmaceutical composition comprising: an acid salt of a sympathomimetic amine; and at least one combination inhibitor, said combination inhibitor being an amino polymer or a salt of a transition metal selected from the group consisting of iron, cobalt, copper, manganese, nickel and zinc, wherein each said combination inhibitor is a single component and is present in amounts sufficient to interfere with the isolation of said sympathomimetic amine and to interfere with the conversion of said sympathomimetic amine to other pharmacologically active compounds without significantly altering the release of said sympathomimetic amine from said pharmaceutical composition as compared to the undenatured composition.  
     
     
         56 . The pharmaceutical composition according to  claim 55  further comprising at least one reaction inhibitor, wherein said reaction inhibitor is present in amounts sufficient to interfere with the conversion of said sympathomimetic amine to other pharmacologically active compounds without significantly altering the release of said sympathomimetic amine from said pharmaceutical composition as compared to the undenatured composition.  
     
     
         57 . The pharmaceutical composition according to  claim 55  further comprising at least one separation inhibitor, wherein said separation inhibitor is present in amounts sufficient to interfere with the isolation of said sympathomimetic amine without significantly altering the release of said sympathomimetic amine from said pharmaceutical composition as compared to the undenatured composition.  
     
     
         58 . The pharmaceutical composition according to  claim 56  further comprising at least one separation inhibitor, wherein said separation inhibitor is present in amounts sufficient to interfere with the isolation of said sympathomimetic amine without significantly altering the release of said sympathomimetic amine from said pharmaceutical composition as compared to the undenatured composition.  
     
     
         59 . The pharmaceutical composition according to  claim 55  wherein said sympathomimetic amine is selected from the group consisting of phenylephrine, salts thereof and combinations thereof.  
     
     
         60 . The pharmaceutical composition according to  claim 59  wherein said sympathomimetic amine is phenylephrine hydrochloride.  
     
     
         61 . The pharmaceutical composition according to  claim 55  wherein said amino polymer is in a neutralized salt form.  
     
     
         62 . The pharmaceutical composition according to  claim 61  wherein said amino polymer is from about 50% to about 100% in the neutralized salt form.  
     
     
         63 . The pharmaceutical composition according to  claim 61  wherein said amino polymer is from about 85% to about 98% in the neutralized salt form.  
     
     
         64 . The pharmaceutical composition according to  claim 55  wherein said amino polymer is a copolymer of methyl methacrylate, butyl methacryl ate and dimethylaminoethyl methacryl ate.  
     
     
         65 . The pharmaceutical composition according to  claim 64  wherein said amino polymer is the neutralized hydrochloride salt form of the copolymer of methyl methacrylate, butyl methacrylate and dimethylaminoethyl methacrylate.  
     
     
         66 . The pharmaceutical composition according to  claim 55  wherein said transition metal salt has an anion selected from the group consisting of chloride, oxide, sulfate and gluconate.  
     
     
         67 . The pharmaceutical composition according to  claim 55  wherein said transition metal salt is selected from the group consisting of ferric chloride, ferric oxide, ferrous sulfate, ferrous chloride, ferrous gluconate, ferrous oxide, zinc gluconate and copper gluconate.  
     
     
         68 . The pharmaceutical composition according to  claim 67  wherein said transition metal salt is selected from the group consisting of ferrous gluconate, zinc gluconate and copper gluconate.  
     
     
         69 . The pharmaceutical composition according to claims  56  wherein said reaction inhibitor is selected from the group consisting of water insoluble polyhydroxy compounds, non-polymeric water soluble polyhydroxy compounds and solvent soluble ester compounds.  
     
     
         70 . The pharmaceutical composition according to  claim 69  wherein said water insoluble polyhydroxy compound is selected from the group consisting of ethylcellulose and cellulose.  
     
     
         71 . The pharmaceutical composition according to  claim 69  wherein said non-polymeric water soluble polyhydroxy compound is selected from the group consisting of fructose, glycerin, sorbitol, lactitol, mannitol, xylitol, maltitol and galactose.  
     
     
         72 . The pharmaceutical composition according to  claim 69  wherein said solvent soluble ester is selected from the group consisting of glycerin esters, esters of glycerin polymers, sorbitol esters, propylene glycol esters, polyethylene glycol esters, sucrose esters and esters of ethoxylated fatty alcohols.  
     
     
         73 . The pharmaceutical composition according to claims  57  or  58  wherein said separation inhibitor is selected from the group consisting of water soluble cellulose compounds, polysaccharide gums, polyethylene oxide polymers, acrylic acid polymers, starches, magnesium aluminum silicates, polyvinylpyrrolidones and clays.