Olanoff L, Koinis T, Anderson J M
J Pharm Sci. 1979 Sep;68(9):1147-50. doi: 10.1002/jps.2600680924.
A membrane-controlled drug delivery device was developed to release tetracycline at zero-order rates. The tetracycline delivery vehicle is a trilaminate disk consisting of core and coating membranes fabricated from a series of 2-hydroxyethyl methacrylate and methyl methacrylate copolymers. Appropriate adjustment of the monomer composition ratio imparts a hydrophobic nature to the copolymer outer coating membrane (relative to the core material), which serves as the rate-limiting membrane in drug diffusion. The trilaminate disks demonstrated a zero-order tetracycline release over 4 months in vitro. The zero-order release rate was a function of the general device geometry, coating membrane thickness, disk surface, area, level of core reservoir drug loading, and membrane coating copolymer composition. Permeability parameters of tetracycline diffusion through a series of 2-hydroxyethyl methacrylate-methyl methacrylate copolymer membranes were determined by a flux-lag time method. Equilibrium hydration values of these membranes also were determined. The ability of trilaminate 2-hydroxyethyl methacrylate-methyl methacrylate devices to release tetracycline at constant rates over a prolonged period offers unique therapeutic and investigational possibilities.
研发了一种膜控释给药装置，以零级速率释放四环素。四环素给药载体是一种三层盘片，由一系列甲基丙烯酸2-羟乙酯和甲基丙烯酸甲酯共聚物制成的核心膜和包衣膜组成。适当调整单体组成比例可使共聚物外涂层膜（相对于核心材料）具有疏水性，该外涂层膜在药物扩散中作为限速膜。三层盘片在体外4个月内呈现出四环素的零级释放。零级释放速率是一般装置几何形状、包衣膜厚度、盘片表面积、核心储库药物负载水平以及膜包衣共聚物组成的函数。通过通量滞后时间法测定了四环素通过一系列甲基丙烯酸2-羟乙酯-甲基丙烯酸甲酯共聚物膜的扩散渗透参数。还测定了这些膜的平衡水合值。三层甲基丙烯酸2-羟乙酯-甲基丙烯酸甲酯装置在较长时间内以恒定速率释放四环素的能力提供了独特的治疗和研究可能性。
