Threo-dops controlled release formulation

Abstract

The present invention relates to pharmaceutical formulations for the controlled delivery of threo-3-(3,4-dihydroxyphenyl)serine (threo-DOPS) and derivatives of it. Such formulations can contain an extended or slow release component that maintains therapeutic concentration of threo-DOPS in the blood plasma over a prolonged time period. They can be further combined with an immediate release formulation to produce a product that, when administered to a patient in need thereof, results in substantially steady levels of active drug, eliminating the sharp peaks and troughs in blood plasma drug levels experienced with the existing threo-DOPS formulations.

1 . A controlled release pharmaceutical formulation, comprising: an effective amount of L-threo-DOPS, a derivative thereof, or a pharmaceutically-acceptable salt thereof, in an extended release form.  
   
   
       2 . A controlled release pharmaceutical formulation of  claim 1 , wherein the extended release form is a dissolution controlled release delivery system.  
   
   
       3 . A controlled release pharmaceutical formulation of  claim 2 , wherein the dissolution controlled release delivery system is oral and comprises a slowly soluble material which is selected from the group consisting of: ethylcellulose, cellulose acetate phthalate, acrylic resins, methacrylate hydrogels, methylmethacrylate, polymethacrylate, polylactic acid, polyvinyl chloride, polyvinyl chloride, polymethacrylate, hydroxypropylmethylcellulose, polyethylene glycols, carboxymethylcellulose, and sodium carboxymethylcellulose.  
   
   
       4 . A controlled release pharmaceutical formulation of  claim 1 , wherein the controlled release formulation is non-oral and maintains the release of L-threo-DOPS, a derivative thereof, or salt thereof, over a period of at least 24 hours.  
   
   
       5 . The controlled release pharmaceutical formulation of  claim 1 , wherein the controlled release formulation is oral and suitable for once-daily administration.  
   
   
       6 . The controlled release pharmaceutical formulation of  claim 1 , wherein the controlled release formulation is oral and suitable for twice- or three-times daily administration.  
   
   
       7 . A controlled release pharmaceutical formulation of  claim 1 , further comprising an effective amount of L-threo-DOPS, a derivative thereof, or a pharmaceutically-acceptable salt thereof, in an immediate release form.  
   
   
       8 . A controlled release pharmaceutical formulation of  claim 7 , wherein the formulation comprises 45-85% by weight of total active drug of L-threo-DOPS in extended release form and 15-55% by weight of total active drug of L-threo-DOPS in immediate release form.  
   
   
       9 . A controlled release pharmaceutical composition of  claim 1  which is for oral use.  
   
   
       10 . A controlled release pharmaceutical composition of  claim 1 , further comprising a pharmaceutically-acceptable carrier.