Formulation and Evaluation of Controlled Release Tablet of Ropinirole HCL

摘要

ABSTRACT The aim of the present work is to develop hydrophilic and hydrophobic polymer based control release matrix tablet of Ropinirole HCl (RPN) which can release the drug up to time period of 24 hr. Ropinirole is a non-ergoline dopamine agonist. Its biological half-life is about 5-6 hrs periods, It is given in dose of 8-10mg/day; it requires multiple dosing to maintain therapeutic drug blood levels. The most frequent side effect of RPN Immediate Release(IR) dosage form is fluctuations in plasma level concentration of drug which may lead to development of some symptoms of Parkinson Disease (PD). To avoid this, the control release formulation maintains steady plasma level concentration of drug throughout a period of 24 hrs, which avoids the symptom of PD. Differential scanning calorimetric analysis confirmed the absence of any drug polymer interaction. In present work different matrices are used to control release of Ropinirole. HPMC K100M, HPMC K15M, Gum guar, PEO etc. are used as Hydrophilic Release Rate Modifier. Hydrophobic release rate used are Ethyl cellulose, Glyceryl Monostearate, Hydrogenated Castor Oil. Tablets (F1-F12, F29-F35) were prepared by Direct Compression and other batches (F12-F25) by Melt Granulation Technique. The tablets were evaluated for thickness, diameter, weight variation test, hardness, friability, and drug content. In vitro drug release studies were carried out in citrate buffer (pH 4) using a USP II dissolution apparatus at 100 rpm, Batch F29 give 96% CDR till the period of 24 hr, it also avoids initial burst release. The best fit model for F29 formulation follows Zero order  (r2= 0.989) and n value was found to be 0.91 which signified that release pattern of optimized batch F29 follows the Fickian diffusion. SEM study of F29 was also performed. During Accelerated Stability studies formulation F29 was found to be stable. Thus the matrix tablets of Ropinirole HCl were prepared successfully. Keywords: Ropinirole HCl, Controlled Release, Parkinson Disease