Baclofen

A new, simple, specific, accurate and precise RP-HPLC method was developed for determination of Baclofen. In the present study, stress testing of Baclofen was carried out according to ICH guidelines Q1A (R2). Baclofen was subjected to stress conditions of hydrolysis, oxidation, photolysis and neutral decomposition. Extensive degradation was found to occur in acidic, condition. Mild degradation was observed in basic and at thermal conditions. Successful separation of drug from degradation products formed under stress conditions was achieved on a Hypersil BDS C18 column (250 mm × 4.6 mm, 5.0 μ particle size) using acetonitrile: acetate buffer (pH 3.7 ± 0.05) (50:50 v/v), at a flow rate of 1.0 mL/min and column was maintained at 40˚C. Quantification and linearity was achieved at 272 nm over the concentration range of 5 - 100 μg/mL for Baclofen. The method was validated for specificity, linearity, accuracy, precision, LOD, LOQ and robustness.

The sustained release of Baclofen is desired because of its short biological half-life. Microspheres of Baclofen were prepared using the non-aqueous emulsification solvent evaporation method. The impacts of different factors such as type of Eudragit polymer as matrix polymer, Eudragit: HPMC K4M ratio on the characteristics of the microspheres were investigated. The morphology of microspheres was studied using optical and scanning electron microscopy and it was shown that microspheres had a spherical shape and smooth surface. The percentage yield of microspheres of all formulation was in the range of 94.01% to 99.12%. The drug content determination showed that even if the polymer composition was changed the solvent evaporation process was highly efficient to give microspheres having maximum drug loading. In termination, the prolonged sustained release time and enhanced stability resulting from the Baclofen microspheres might make contribution to its use.