FORMULATION, DEVELOPMENT, AND IN VITRO CHARACTERIZATION OF PRAMIPEXOLE TABLETS FOR SUSTAINED RELEASE DRUG DELIVERY SYSTEM

Abstract

The objective of the present study was to design and evaluate sustained release matrix tablets of Pramipexole dihydrochloride, a non-ergoline dopamine agonist used in the management of Parkinson’s disease and restless legs syndrome. Sustained drug delivery is crucial in chronic neurological disorders to ensure consistent therapeutic levels, minimize side effects, and improve patient adherence. Conventional dosage forms of Pramipexole necessitate frequent dosing due to its relatively short half-life (~8 hours), which can lead to fluctuations in plasma concentration and increased risk of adverse effects. To address these limitations, matrix tablets were formulated using various grades of hydrophilic polymer Hydroxypropyl Methylcellulose (HPMC K4M, K15M, and K100M) and Eudragit polymers (L-100 and S-100) in different ratios, combined with excipients like microcrystalline cellulose (MCC), PVP K30, talc, and magnesium stearate. The direct compression method was employed for tablet preparation. Pre-compression blends were evaluated for micromeritic properties, and the compressed tablets underwent standard post-compression tests including hardness, friability, drug content uniformity, and thickness. In vitro dissolution studies were carried out in simulated gastric and intestinal fluids using USP Type II dissolution apparatus. Drug release data were analysed using various kinetic models (zero- order, first-order, Higuchi, and Korsmeyer-Peppas) to understand the mechanism of release. The results demonstrated that formulations containing higher viscosity grades of HPMC (particularly K100M) and combinations with Eudragit showed a more controlled and prolonged drug release up to 12 hours. FTIR studies confirmed the absence of drug-excipient interactions, and short-term stability studies indicated the physical and chemical stability of the optimized formulation under accelerated conditions. This study successfully establishes a promising sustained release oral formulation of Pramipexole that can potentially enhance therapeutic efficacy, reduce dosing frequency, and improve the quality of life in patients suffering from Parkinson’s disease.