As shown in Table 3, at twelve months the 4.0 and 5.0 mg/mL solutions remained clear and no particulates were detected by the methods described in Example 11.

Initial baclofen concentrations for the nominally 4, 5, 6, and 8 mg/mL test solutions were within 93 to 104% of the target concentrations.The liquid chromatograph is a Waters LC Module-1 Plus having a multisolvent pump, variable wavelength UV detector, and autosampler in one unit. These solutions can be used as pharmaceuticals for parenteral or oral administration. Baclofen injections (Lioresal Intrathecal, Medtronic) are therefore commonly administered intathecally via an implanted pump to manage severe spasticity of spinal cord origin. Despite it it was concluded that no other solid-state form of baclofen exists.

The results of the chemical stability studies are also given in Table 3. were originally derived from human colon adenocarcinoma. Only solutions of baclofen having a concentration of 2 mg/mL have previously been demonstrated to have the properties that make them an acceptable commercial pharmaceutical product by remaining stable for extended periods of time without precipitation of significant amounts of baclofen particulates.Various sources have reported stable suspensions or syrups of baclofen for oral administration that had concentrations even higher than equilibrium concentration of 4.3 mg/mL, (Allen et al., 1996; Johnson and Hart, 1993) but none of these preparations are acceptable for pharmaceutical injection uses. The temperature range of at least about 60° C. to at less than about 100° C. is most preferred. Alternately, aqueous solutions of the present invention can contain no such additives and can consist solely of baclofen and water. Separate sample syringes and sample vials are prepared for each drug concentration at each storage temperature. This occurred within about 20 minutes with all samples.After complete dissolution of the samples had occurred, the solutions were allowed to cool to room temperature and several separate aliquots of each sample were filtered through 0.22-micron sterilizing filters into sterile empty vials. Antimicrobial preservatives are undesirable for intrathecal and epidural injections. 2596683, MDR Report: Rice Creek Manufacturing Indura Catheter, Model #8709 (2006).Diogenes Record No. In alternative embodiments, baclofen solutions of the present invention can be used for any other clinically suitable type of administration including, but not limited to, intravenous, intramuscular or subcutaneous injection.As discussed above, current commercial preparations of baclofen consist of baclofen, sodium chloride and water. These solutions containing trace amounts of particulates would generally still be considered pharmaceutically acceptable. Therefore, in preferred embodiments, the present invention provides high concentration baclofen solutions suitable for oral or intrathecal administration. For a better experience, please enable JavaScript in your browser before proceeding. The mailbox will be used as the login user name and retrieve the password(File Format: Jpg, Gif, Png, PDF,Zip,Txt,doc or xls Max Size: 3MB) In particular, the present invention provides stable aqueous baclofen solutions having concentrations greater than about 2.1, 2.2, 2.3, 2.4, 2.5, 2.6, 2.7, 2.8, 2.9, 3.0, 3.1, 3.2, 3.3, 3.4, 3.5, 3.6, 3.7, 3.8, 3.9, 4.0, 4.1, 4.2, 4.3, 4.4, 4.5, 4.6, 4.7, 4.8, 4.9, 5.0, 5.1, 5.2, 5.3, 5.4, 5.5, 5.6, 5.7, 5.8, 5.9 and 6.0 mg/mL.

monohydrate only exists in solution or environments where sufficient water is available.

Some features of this site may not work without it.Baclofen is a centrally acting muscle relaxant that acts as an agonist of the inhibitory More specifically, it will be apparent that certain agents that are chemically or physiologically related can be substituted for the agents described herein while the same or similar results would be achieved. The physico-chemical investigations indicated that baclofen may exist in the The results obtained and the parameterized values solvents allowed us to observe the influence of the latter on the solubility of KET. However, when subjected to refrigeration, the 5 and 6-mg/mL concentrations developed a precipitate after 14 days and 7 days, respectively.Physical stability of 8.0 mg/mL baclofen solutions. dissolutions were performed in an effort to identify possible solution-mediated phase

The inventors believe that this the concentration represents the “practical solubility” of baclofen. Ibuprofen (IB), a nonsteroidal anti-inflammatory drug, is a chiral molecule and is currently used clinically as a racemate (racIB). Furthermore, the solubility, dissolution and membrane permeability of baclofen in different solvents and bio-relevant media were investigated to determine the biopharmaceutics classification system (BCS) of baclofen. Joined Dec 18, 2002 Messages 206 Location sydney.