Baclofen formulations and methods for making same

摘要

Methods for preparing sterilized baclofen solutions include adjusting the pH to below a desired pH, and steam sterilizing the solution with adjusted pH, which results in the solution having the desired pH. Such solutions may also have low concentrations of 4-CPP. Injectable baclofen solutions having greater than 2 mg/mL baclofen include between 5 mM and 25 mM of a phosphate or sulfate species. The solution has an ionic strength equivalent of about 1.5 M NaCl. The present application also provides baclofen formulations for use in treating spasticity, brain injury, cerebral palsy, spinal cord injury, cervical injury, multiple sclerosis, thoracic injury, or withdrawal symptoms.

主权项

1. An injectable baclofen solution, the solution comprising:
baclofen in a concentration greater than 2 mg/mL; sulfate or phosphate in a concentration of between 10 mM and 25 mM, wherein the solution has an ionic strength equivalent of between 1, the solution c.4 M NaCl and 1.6 M NaCl comprising less than 1.3% of 4-(4-chlorophenyl)-2-pyrrolidinone (4-CPP) after at least 30 days of storage at room temperature, wherein the solution has a pH between about 5.5 and 6.5.