Pharmaceutical formulation of apomorphine for buccal administration

Abstract

The present invention provides a kit comprising, in separate compartments of a container, the following components (a) and (b): (a) a combination of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier; and (b) a solution which comprises a diluent and a pH modifying agent; the components being presented such that they can be combined at the point of use into a formulation which is adjusted to a pH ranging from mildly acidic to alkaline and which is suitable for buccal administration. The formulation is useful in treating Parkinson's disease and in promoting sexual function.

1 . A kit comprising a container, which comprises separate first and second compartments, wherein the first compartment comprises the following components (a):
 (a) a combination of:
 (i) apomorphine or a pharmaceutically acceptable acid addition salt thereof, and 
 (ii) a pharmaceutically acceptable excipient or carrier; and wherein the second compartment comprises the following component (b): 
   (b) a solution which comprises a diluent and a pH modifying agent; wherein the first and second compartments are arranged such that components (a) and (b) can be combined at the point of use of the kit to produce a formulation having a pH ranging from mildly acidic to alkaline, and which is suitable for buccal administration.   
   
   
       2 . A kit according to  claim 1  wherein the diluent is water. 
   
   
       3 . A kit according to  claim 1  wherein the pH modifying agent is a buffer and the formulation is buffered to a pH ranging from mildly acidic to alkaline. 
   
   
       4 . A kit according to  claim 1  wherein component (a) is present in particulate form. 
   
   
       5 . A kit according to  claim 1  wherein component (a) is present in suspension or liquid form. 
   
   
       6 . A kit according to  claim 1  wherein component (b) further comprises one or more additional pharmaceutically acceptable agents selected from the group consisting of solubilizers, adhesive agents, antioxidants, flavouring agents, sweeteners, and combinations thereof. 
   
   
       7 . A process for producing a pharmaceutical composition, which process comprises combining apomorphine or a pharmaceutically acceptable acid addition salt thereof with a solution which comprises a diluent and a pH modifying agent, such that the resulting formulation is has a pH ranging from mildly acidic to alkaline, and is suitable for buccal administration. 
   
   
       8 . A process according to  claim 7  wherein the diluent is water. 
   
   
       9 . A process according to  claim 7  wherein the pH modifying agent is a buffer, such that the formulation is buffered to a pH ranging from mildly acidic to alkaline. 
   
   
       10 . (canceled) 
   
   
       11 . (canceled) 
   
   
       12 . (canceled) 
   
   
       13 . (canceled) 
   
   
       14 . (canceled) 
   
   
       15 . A method of administering an apomorphine composition to a patient in need thereof, comprising:
 (a) optionally adjusting the pH of a composition comprising a pharmaceutically effective amount of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier to a pH ranging from mildly acidic to alkaline; and   (b) delivering the composition buccally to a patient in need thereof.   
   
   
       16 . The method of  claim 15 , wherein the diluent comprises water. 
   
   
       17 . The method of  claim 15 , wherein the adjusting of the pH of the composition comprises adding to the composition a pH modifying agent. 
   
   
       18 . The method of  claim 17 , wherein the pH modifying agent comprises a buffer capable of buffering the composition to a pH ranging from mildly acidic to alkaline. 
   
   
       19 . The method of  claim 15 , wherein composition is administered to treat Parkinson's disease. 
   
   
       20 . The method of  claim 15 , wherein the composition is administered to promote sexual function, treat sexual dysfunction, enhance libido, reduce impotence, or a combination thereof.