Compositions for nasal administration

Abstract

There is provided a composition for the nasal delivery of a drug suitable for the treatment of erectile dysfunction to a mammal wherein the composition is adapted to provide an initial rise in plasma level followed by a sustained plasma level of the drug.

We claim:  
     
         1 . A composition for nasal delivery comprising a drug suitable for the treatment of erectile dysfunction, wherein the composition is adapted to provide an initial rise in plasma level followed by a sustained plasma level of the drug.  
     
     
         2 . A composition for nasal delivery comprising a drug useful in the treatment of erectile dysfunction and one or more excipients, wherein the composition is adapted to provide an initial rise in plasma level followed by a sustained plasma level of the drug.  
     
     
         3 . A composition according to    claim 2   , wherein the drug is a weak base or a weak acid and the combination of drug with excipient results in complexation as a result of an ion exchange process.  
     
     
         4 . A composition according to    claim 2   , wherein the drug is a weak base or a weak acid, and is combined with a block copolymer.  
     
     
         5 . A composition according to    claim 4   , wherein the block copolymer is selected from the group consisting of poloxamines, poloxamers and polylactidepolyoxyethylene copolymers.  
     
     
         6 . A composition according to    claim 2   , wherein the excipient is an ion exchange polymeric material.  
     
     
         7 . A composition according to    claim 2   , wherein the excipient provides for controlled delivery of the drug to the nasal membrane and comprises a polysaccharide and/or a block copolymer comprising a polyoxyethylene block.  
     
     
         8 . A composition according to    claim 2   , wherein the excipient is an anionic polysaccharide selected from the group consisting of xanthans, gellans, alginates, hyaluronic acid, carboxymethylcellulose.  
     
     
         9 . A composition according to    claim 2   , wherein the excipient is a pectin.  
     
     
         10 . A composition according to    claim 2   , wherein the excipient is a carboxylated starch.  
     
     
         11 . A composition according to    claim 2   , wherein the excipient is chitosan.  
     
     
         12 . A composition according to    claim 1   , wherein the composition is a liquid.  
     
     
         13 . A composition according to    claim 2   , wherein the composition is a liquid system which is adapted to gel in the nasal cavity.  
     
     
         14 . A composition according to    claim 13   , wherein the composition is adapted to gel on contact with the cations present in the nasal cavity.  
     
     
         15 . A composition according to    claim 14   , wherein the composition comprises a source of cations.  
     
     
         16 . A composition according to    claim 14   , wherein the excipient comprises pectin and/or gellan.  
     
     
         17 . A composition according to    claim 1   , wherein the composition is in the form of microspheres.  
     
     
         18 . A composition according to    claim 17   , wherein the microspheres are produced from carboxylated starch.  
     
     
         19 . A composition according to    claim 17   , wherein the microspheres are produced from chitosan.  
     
     
         20 . A composition according to    claim 1   , wherein the composition comprises a drug selected from the group consisting of the alpha-adrenoreceptor antagonists, e.g. phentolamine, phenoxybenzamine, yohimbine, moxislyte delaquamine; compounds with central D 2 -receptor antagonist activity, e.g. apomorphine; compounds that act primarily by blocking the re-uptake of serotonin into nerve terminals, e.g. trazadone and chlorophenylpiperazine; competitive and selective inhibitors of c-GMP type V phosphodiesterases, e.g. sildenafil; L-arginine; papaverine, and the pharmaceutically acceptable salts thereof.  
     
     
         21 . A composition according to    claim 20   , wherein the composition comprises a drug with central D 2 -receptor antagonist activity.  
     
     
         22 . A composition according to    claim 21   , wherein the composition comprises apomorphine.  
     
     
         23 . A method for the controlled delivery of a drug to the systemic circulation of a mammal which comprises the nasal administration of a composition according to    claim 1   , to the mammal.  
     
     
         24 . A method of treatment of a disease in which the controlled delivery of a drug to the circulation is desirable which comprises the nasal administration of a composition according to    claim 1   , to a mammal.  
     
     
         25 . A method as claimed in    claim 24   , wherein the drug is apomorphine and the disease is Parkinson's disease.  
     
     
         26 . A method as claimed in    claim 24   , wherein the disease is erectile dysfunction.  
     
     
         27 . A method for treating a disease which comprises nasal administration of a composition according to    claim 1   .  
     
     
         28 . A method for treating erectile dysfunction which comprises nasal administration of a composition according to    claim 1   .  
     
     
         29 . The use of a composition according to    claim 1   , in the manufacture of a medicament for the controlled delivery of a drug useful in the treatment of erectile dysfunction to the systemic circulation of a mammal.  
     
     
         30 . The use of a composition according to    claim 1   , in the manufacture of a medicament for nasal administration of a drug useful in the treatment of erectile dysfunction.  
     
     
         31 . The use of a composition according to    claim 1   , in the manufacture of a medicament for treating erectile dysfunction.  
     
     
         32 . A process for the preparation of a composition according to    claim 2    which comprises admixing the drug with the excipient.  
     
     
         33 . A composition for nasal delivery comprising a drug useful in the treatment of erectile dysfunction and an excipient comprising an anionic or cationic polysaccharide or a block copolymer containing a polyoxyethylene block.  
     
     
         34 . A composition according to    claim 33   , wherein the drug is apomorphine.