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 (epsilon), the fractal dimensions (Df) and the microscopic viscosity (eta matrix) of the matrices on the release rate of DIL were investigated on the basis of the linear least square equation as well as the Higuchi's 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 Higuchi's equation including the values of epsilon, Df and eta matrix. It is likely that the release rate of DIL from pHEMA matrices is mainly controlled by epsilon and Df, but eta matrix was less effective.
Yanagawa
F
F
Department of Pharmaceutics, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan. fumikiyanagawa@gmail.com <fumikiyanagawa@gmail.com>
Ishii
Y
Y
Onuki
Y
Y
Morishita
M
M
Takayama
K
K
D000465:Algorithms; D002851:Chromatography, High Pressure Liquid; D004110:Diltiazem / Q000008:administration & dosage / Q000737:chemistry*; D004578:Electron Spin Resonance Spectroscopy; D017709:Fractals; D006207:Half-Life; D007700:Kinetics; D016018:Least-Squares Analysis; D016014:Linear Models; D008689:Methacrylates / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D016062:Porosity; D013056:Spectrophotometry, Ultraviolet; D014783:Viscosity
D008689:Methacrylates; C005044:hydroxyethyl methacrylate; D004110:Diltiazem