The aim of this study is to develop a sustained-release microparticle containing ropinirole hydrochloride for orally disintegrating tablets. The main indication of ropinirole hydrochloride is Parkinson's disease. The patient group of Parkinson's disea...
The aim of this study is to develop a sustained-release microparticle containing ropinirole hydrochloride for orally disintegrating tablets. The main indication of ropinirole hydrochloride is Parkinson's disease. The patient group of Parkinson's disease has difficulty swallowing tablets due to geriatrics, dysphagia and dyskinesia. The sustained-release microparticles were prepared using a fluid bed coater for the application of ropinirole hydrochloride to orally disintegrating tablets as a patient friendly dosage forms.
A drug-ion exchange resin complex of ropinirole hydrochloride and Amberlite™ IRP 69 was prepared to control the rapid release of ropinirole hydrochloride and to mask the bitter taste in the mouth. Ropinirole hydrochloride was loaded with the sustained-release ion exchange resin, Amberlite™ IRP 69, in a batch method. The prepared drug-ion exchange resin complex showed more sustained-release than the active coated particles of ropinirole hydrochloride on Amberlite™ IPR 69. This confirmed that the drug-ion exchange resin complex was suitable as the core of sustained-release microparticle coated with hydrophobic polymer, Eudragit® RL PO, for further release control. To be equivalent to the reference drug, REQUIP® XL, in in vitro release study, drug-ion exchange resin complex was coated with Eudragit® RL PO to prepare sustained-release microparticles. The size of the prepared sustained-release microparticles was 200 µm or less and the sustained-release microparticles were suitable for orally disintegrating tablets because particles.
The sustained-release microparticles prepared were mixed with excipients and compressed into tablets for application to orally disintegrating tablets. The formulation and process parameters were optimized to produce sustained-release orally disintegrating tablets. The orally disintegrating tablets containing sustained-release microparticles of ropinirole hydrochloride were prepared by varying the ratio of diluent, tableting pressure, and the thickness of coating layer of the sustained-release microparticle and evaluated by hardness study, disintegration study, and in vitro release study. The final optimized formulation for sustained-release orally disintegrating tablet of ropinirole hydrochloride was consisting of the sustained-release microparticle coated with 25% Eudragit® RL PO and 240 mg mannitol as diluent. The sustained-release orally disintegrating tablet met the release criteria of USP for ropinirole sustained-release tablet and the bitter taste of ropinirole hydrochloride was successfully masked. This tablet had proper mechanical strength with hardness of 67.0 N and disintegration time of 55.58 seconds. Additionally, the tablet was equivalent with REQUIP® XL 4mg in comparative release study and the similarity factor(f2) with the value of 43.38 was more than 40 which the criteria of f2 value for sustained-release tablets.