Polymeric delivery system for a nonviscous prostaglandin-based solution without preservatives

Abstract

This invention concerns an ophthalmic solution including: at least one prostaglandin; a solubilizing agent; a gelling agent of the carbomer type; a carbomer polymerization-inhibiting agent; a co-gelling/co-solubilizing agent.

1 - An ophthalmic solution including:
 at least one prostaglandin;   a solubilizing agent;   a gelling agent of the carbomer type;   a carbomer polymerization-inhibiting agent;   a co-gelling/co-solubilizing agent.   
     
     
         2 - Solution as claimed in  claim 1 , characterised in that it has a Brookfield viscosity at 25° C. that is between 8 and 20 mPa·s, advantageously between 10 and 14 mPa·s. 
     
     
         3 - Solution as claimed in  claim 1 , characterised in that the concentration of the carbomer gelling agent is between 0.05 and 0.15% (w/v). 
     
     
         4 - Solution as claimed in  claim 1 , characterised in that it contains no antimicrobial preservatives, advantageously of the quaternary ammonium type, and even more advantageously benzalkonium chloride (BAK). 
     
     
         5 - Solution as claimed in  claim 1 , characterised in that the prostaglandin is chosen from the group including 17-phenyl-13,14 dihydro trinor prostaglandin F 2α  isopropyl ester (latanoprost), 20-ethyl prostaglandin F 2α , (+)-fluprostenol isopropyl ester (travoprost), 17-phenyl trinor prostaglandin F 2α  amide, 17-phenyl-13,14 dihydro trinor prostaglandin F 2α  ethyl amide (bimatoprost), tafluprost prostaglandin F 2α  ethanolamide, bimatoprost (free acid)-d 4 , bimatoprost-d 4 , latanoprost ethyl amide, 13,14 dihydro-15-keto-20-ethyl prostaglandin F 2α  (unoprostone), 13,14 dihydro-15-keto-20-ethyl prostaglandin F 2α  isopropyl ester (unoprostone isopropyl ester), advantageously latanoprost. 
     
     
         6 - Solution as claimed in  claim 1 , characterised in that the concentration of prostaglandins in the solution is between 0.002 and 0.15% (w/v). 
     
     
         7 - Solution as claimed in  claim 1 , characterised in that the agent inhibiting the polymerization of the carbomer is a source of sodium ions, advantageously sodium EDTA, sodium acetate or sodium chloride. 
     
     
         8 - Solution as claimed in  claim 1 , characterised in that the solubilizing agent is macrogolglycerol hydroxystearate. 
     
     
         9 - Solution as claimed in  claim 1 , characterised in that the co-gelling/co-solubilizing agent is a polymer chosen from the group including polyethylene glycol (PEG), polyvinyl alcohol (PVA) or polyvinylpyrrolidone (PVP). 
     
     
         10 - Solution as claimed in  claim 1 , characterised in that the solution is stable for at least 18 months at ambient temperature (25 or 30° C.). 
     
     
         11 - Solution as claimed in  claim 1 , characterised in that the solution is compatible with single-use or multi-dose bottles made of LDPE containing no additives. 
     
     
         12 - Solution as claimed in  claim 1 , characterised in that it also contains an antiglaucoma agent chosen from the group including beta blockers, carbonic anhydrase inhibitors and alpha-adrenergic agonists. 
     
     
         13 - Solution as claimed in  claim 1 , characterised in that it also contains an additive chosen from the group including isotonic agents, antioxidants and buffer systems. 
     
     
         14 - Solution as claimed in  claim 1  for its use in treating glaucoma and/or reducing intraocular pressure. 
     
     
         15 - Solution as claimed in  claim 14  consisting in topically administering one drop of said solution a day to each eye in humans or animals. 
     
     
         16 - Single-use or multi-dose bottle made of LDPE containing no additives containing the ophthalmic solution covered by  claim 1 .