Pramipexole

The present study was to formulate and characterize oral floating microspheres of Pramipexole to sustain the gastric residence time and to target gastritis. The floating microspheres were prepared by ionotropic gelation technique. Sodium alginate was used as polymer, sodium bicarbonate as gas generating agent, calcium chloride as cross-linking agent, HPMC K4, as rate retarding agent. Microspheres were characterized for the Micromeretic properties, incorporation efficiency, buoyancy test, SEM analysis, FTIR, and in vitro diffusion studies. The diffusion studies were carried out in 0.1N HCl and the results were applied to various kinetic models.  Among the total 14 formulations F12 was found to be optimized on the basis of different evaluation parameters. The % yield of F12 formulation was found to be 98.58%. On the basis of optical microscopy, the particle size was 65.12±0.04µm. The % buoyancy, % entrapment efficiency and swelling index of F12 formulation was 98.12%, 96.56% and 97.10, respectively. The Cumulative % drug release of F12 formulation was 98.3±5.10% in 12h.  SEM studies showed the particles were in spherical shape. On the basis of obtained results, Floating microspheres were of good candidate for targeting to GIT.

A selective, sensitive and rapid UPLC-MS/MS method has been developed and validated for simultaneous quantification of pramipexole, ropinirole and rasagiline in human plasma using trimetazidine as internal standard (IS). The analytes and IS were extracted from 200 µL of plasma by solid phase extraction technique using strata cartridges which offers high sensitivity, wide linearity without interferences form endogenous matrix components. Chromatographic separation was achieved in 3.00 min run time on a Synergi Polar RP column using a 5 mM ammonium acetate/methanol mobile phase in gradient mode. The quantification of target compounds was performed in a positive electrospray ionization mode and multiple reaction monitoring (MRM). The proposed method was validated over the concentration ranges of 5-50000 pg/mL for each analyte. The intra- and inter-day precision and accuracy results were acceptable as per FDA guidelines. Stability of compounds were established in a battery of stability studies, i.e. bench top, auto sampler, dry extract and long term storage stability as well as freeze-thaw cycles. The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic studies.