FORMULATION AND IN-VITRO OPTIMIZATION OF EXTENDED RELEASE TABLETS OF PRAMIPEXOLE DIHYDROCHLORIDE MONOHYDRATE FOR PARKINSON’S DISEASE

摘要

The main aim of the extended release tablets is to reduce the dose frequency and to improve the patient compliance. The objective of the present study was to formulate and optimize the extended release tablets of Pramipexole dihydrochloride monohydrate for 24hrs, which made the advantage of this formulation as once daily with more patient compliance. The combination of different hydrophilic polymers and hydrophobic polymer in varying concentrations were used to get the desired extended release profile over a period of 24 h. The drug and excipients mixed granules was subjected to evaluate the physical properties like angle of repose, bulk density, compressibility index were found to be satisfactory. The hydrophilic polymer Hydroxy propyl methyl cellulose (HPMC K200M) at 41.7% and( HPMC E 3LV) at 5% in combination with hydrophobic polymer (Eudragit L100) at 5% level produced desired extended release Pramipexole dihydrochloride monohydrate matrix tablets. The in vitro drug release of optimized formulation (F9) was 99% and was more release than innovator product of Mirapex ER (94.5%) which extended up to 24 h. The drug release pattern from the optimized matrix formulation (F9) was diffusion controlled obeying Higuchi equation, and by Non-Fickian mechanism obeying Koresemeyer – Peppa’s equation. The innovator product Mirapex ER (0.375mg) drug release profiles were shown to be followed first order release kinetics. The prepared once daily extended release Pramipexole dihydrochloride monohydrate tablets in combination of hydrophilic (HPMC K200M), (HPMC E 3LV) and hydrophobic (Eudragit L100) polymers, is a suitable one to treat the Parkinson’s disease.