Factors affecting release rate of diltiazem hydrochloride from poly (2-hydroxyethyl methacrylate) matrices

Sustained release diltiazem hydrochloride (DIL) formulation is widely used over 110 countries worldwide, and is among the drugs recommended as a first-line therapy in the major guidelines for the management of hypertension. In search for a most suitable controlled release formulation of DIL, we investigated poly (2-hydroxyethyl methacrylate) matrix (pHEMA matrix) synthesized by photopolymerization. Factors affecting the release rate of DIL from pHEMA matrices were investigated, focusing on the internal structure of the matrices. The effects of the porosity (ɛ), the fractal dimensions (Df) and the microscopic viscosity (ηmatrix) of the matrices on the release rate of DIL were investigated on the basis of the linear least square equation as well as the Higuchiʹs equation. A relation between the actual value and predicted value based on the linear least square equation exhibited a fairly good linearity (r = 0.979). Furthermore, the release rate of DIL was represented based on the Higuchiʹs equation including the values of ɛ, Df and ηmatrix. It is likely that the release rate of DIL from pHEMA matrices is mainly controlled by ɛ and Df, but ηmatrix was less effective.