保益乐（POLYOX）.PDF

POLYOX? Application Data Water Soluble Resins The Influence of In Vitro Dissolution Method on the Release of a Highly Water Soluble Drug from Polyethylene Oxide and Hypromellose Hydrophilic Extended Release Matrices PURPOSE Hydrophilic matrices (HM) represent a popular and widely used approach for oral extended release (ER) drug delivery. Hypromellose (HPMC) remains the polymer of choice as the rate-controlling carrier.(1) In addition to HPMC, polyethylene oxide (PEO) has been extensively studied as a matrix-forming polymer. This is mainly attributed to its availability in a range of molecular weight/viscosity grades, FDA acceptance and unique swelling/erosion characteristics which can be utilized for modulating drug release.(2, 3) The in vitro drug release from hydrophilic matrix tablets may be affected by various factors(1) and is often dependent on the hydrodynamic conditions used during dissolution testing. Different dissolution apparatus operated at varying agitation intensities create different hydrodynamics.(4) This causes varying degrees of mechanical stress on the hydrated matrix which may lead to alterations of polymer erosion rate. The objective of this study was to investigate the influence of different dissolution methods on the release of a high solubility drug - metformin hydrochloride (HCl)) from an ER matrix formulation containing either HPMC or PEO as the rate-controlling polymer. METHODS Formulation Manufacture of ER Matrices Two formulations containing 50% w/w metformin HCl (AMRI, India) as a freely water soluble model drug, 30% w/w PEO (POLYOXTM water soluble resin -1105, Dow Chemical Co., USA) or HPMC (METHOCELTM premium cellulose ether K100M CR, Dow Chemical Co., USA), 19% w/w microcrystalline cellulose (Microcel 102, Blanver, Brazil), 0.5% w/w fumed sil