baclofen solution for low-volume therapeutic delivery

Abstract

A high concentration baclofen solution is provided suitable for therapeutic use in a medical setting. A high concentration solution of baclofen in multivalent physiological ion solution such as artificial cerebrospinal fluid is provided with concentrations of baclofen of 10 mg/ml. Artificial cerebrospinal fluid is particularly advantageous as a baclofen solvent. A medical package is also provided for baclofen delivery to patients suffering from spasticity.

1 . A solution comprising baclofen in a multivalent physiological ion solution having a concentration of baclofen at or greater than 2 mg/ml. 
     
     
         2 . The solution of  claim 1  wherein said multivalent physiological ion solution is artificial cerebrospinal fluid. 
     
     
         3 . The solution of  claim 1  wherein the concentration of baclofen is greater than 2.0 mg/ml. 
     
     
         4 . The solution of  claim 1  where in the concentration of baclofen is greater than 2.0 mg/ml and equal to or less than 10 mg/ml. 
     
     
         5 . The use of the solution of  claim 1  for delivery to a patient. 
     
     
         6 . The use of the solution of  claim 5  wherein said delivery is selected from the group comprising: intrathecal, intraventrical, oral, intravenous, intra-arterial, intraperitoneal, epidural, intramuscular, or subcutaneous delivery. 
     
     
         7 . The use of the solution of  claim 1  to medically treat a disease or injury. 
     
     
         8 . The use of  claim 7  where in said disease or injury is selected from the group comprising: spasticity, brain injury, cerebral palsy, spinal cord injury, cervical injury, multiple sclerosis, thoracic injuries, spinal pathology, or combinations thereof. 
     
     
         9 . A medical package containing the solution of  claim 1  along with instructions for the use thereof to treat spasticity. 
     
     
         10 . The medical package of  claim 9  wherein said medical package contains a single dose of baclofen. 
     
     
         11 . A solution of baclofen comprising baclofen in a solution consisting essentially of 130-160 mM NaCl, 2.7-3.9 mM KCl, 1-10 mM CaCl 2 .2H 2 O, 0.5-10 mM MgCl 2 .6H 2 O and a remainder water, having a concentration of baclofen of at or between 2 mg/ml and 10 mg/ml inclusive. 
     
     
         12 . The solution of  claim 11  further comprising 0.5-1.0 mM Na 2 HPO 4  and 0.1-0.5 mM NaH 2 PO 4 . 
     
     
         13 . The solution of  claim 11  comprising 148 mM NaCl; 3 mM KCl; 1.4 mM CaCl 2 .2H 2 O; 0.8 mM MgCl 2 .6H 2 O; 0.8 mM Na 2 HPO 4 .7H 2 O; 0.2 mM NaH 2 PO 4 .H 2 O. 
     
     
         14 . The solution of  claim 11  wherein the pH is at or between 5 and 8. 
     
     
         15 . The solution of  claim 11  further comprising 15-35 mM HCO 3 . 
     
     
         16 . The solution of  claim 11  further comprising one or more pain regulating agents selected from the group comprising morphine, clondine, hydromorphine, hydrocodone, merperidine, celeroxib, tramadol, oxycodone, acetometaphen, ketaprofen, ibuprofen, naproxen sodium, aspirin, and combinations thereof. 
     
     
         17 . The solution of  claim 11  for intrathecal delivery to a patient by manual or automatic injection apparatus. 
     
     
         18 . The solution of  claim 11  for delivery to a patient by a route selected from the group comprising intraventrical, oral, intravenous, intra-arterial, intraperitoneal, epidural, intramuscular, subcutaneous, and combinations thereof. 
     
     
         19 . The use of the solution of  claim 11  to medically treat a disease or injury selected from the group comprising spasticity, brain injury, cerebral palsy, spinal cord injury, cervical injury, multiple sclerosis, thoracic injuries, spinal pathology, and combinations thereof.