Nasal delivery of apomorphine

Abstract

Intranasal delivery methods and compositions for the delivery of dopamine receptor agonists are provided which are effective for the amelioration of erectile dysfunction in a mammal without causing substantial intolerable adverse side effects to the mammal. Nasally administered compositions for treating male erectile dysfunction in a mammal are also provided which include a therapeutically effective amount of a dopamine receptor agonist which has been dispersed in a system to improve its solubility and/or stability.

1 - 61 . (Canceled)  
     
     
         62 . A method for treating sexual dysfunction in a mammalian subject comprising administering to said subject a therapeutically effective dosage unit of 2 mg or less of apomorphine or a chemically modified equivalent or pharmaceutical salt thereof formulated in a composition for intranasal administration, which is therapeutically effective to alleviate said sexual dysfunction without causing substantial intolerable adverse side effects.  
     
     
         63 . The method of  claim 62 , wherein said therapeutically effective dosage unit is 1 mg or less.  
     
     
         64 . The method of  claim 62 , which is therapeutically effective to prevent or reduce symptoms of erectile dysfunction in the subject.  
     
     
         65 . The method of  claim 64 , which is therapeutically effective to elicit an erection in said subject within about 30 minutes following intranasal administration.  
     
     
         66 . The method of  claim 62 , wherein said composition is an aqueous solution.  
     
     
         67 . The method of  claim 66 , wherein said aqueous solution is selected from the group consisting of aqueous gels, aqueous suspensions, aqueous liposomal dispersions, aqueous emulsions, aqueous microemulsions and combinations thereof.  
     
     
         68 . The method of  claim 62 , wherein said composition is a non-aqueous solution.  
     
     
         69 . The method of  claim 68 , wherein said non-aqueous solution is selected from the group consisting of non-aqueous gels, non-aqueous suspensions, non-aqueous liposomal dispersions, non-aqueous emulsions, non-aqueous microemulsions and combinations thereof.  
     
     
         70 . The method of  claim 62 , wherein said composition is a powder formulation.  
     
     
         71 . The method of  claim 70 , wherein said powder formulation is selected from the group consisting of simple powder mixtures, powder microspheres, coated powder microspheres, and combinations thereof.  
     
     
         72 . The method of  claim 62 , wherein said composition further comprises one or more pharmaceutical excipients.  
     
     
         73 . The method of  claim 62 , wherein said composition further comprises a pharmaceutically acceptable preservative.  
     
     
         74 . The method of  claim 62 , wherein said composition further comprises a humectant.  
     
     
         75 . The method of  claim 62 , wherein said composition further comprises a buffer selected from the group consisting of acetate, citrate, prolamine, carbonate and phosphate buffers.  
     
     
         76 . The method of  claim 62 , wherein said composition further comprises a stabilizing agent selected from the group consisting of glycerin, a sugar alcohol, and glycol derivatives.  
     
     
         77 . The method of  claim 76 , wherein said glycol derivative is a propylene glycol.  
     
     
         78 . The method of  claim 76 , wherein said glycol derivative is a polyethylene glycol.  
     
     
         79 . The method of  claim 62 , wherein said composition further comprises a plurality of reducing agents yielding enhanced stability of said apomorphine or chemically modified equivalent or pharmaceutical salt thereof.  
     
     
         80 . The method of  claim 79 , wherein at least one of said plurality of reducing agents is selected from sodium metabisulfite, ascorbic acid, and sodium ascorbate.  
     
     
         81 . The method of  claim 80 , wherein at least two of said plurality of reducing agents are selected from sodium metabisulfite, ascorbic acid, and sodium ascorbate.  
     
     
         82 . The method of  claim 62 , wherein said composition further comprises a buffer to maintain a pH of the composition at a value from about 3.0 to about 3.5.  
     
     
         83 . The method of  claim 82 , wherein said composition has a pH of about 3.5.  
     
     
         84 . The method of  claim 82 , wherein said composition has a pH of about 3.0.