Béchard S, McMullen J N
Faculté de Pharmacie, Université de Montréal, Quebec, Canada.
J Pharm Sci. 1988 Mar;77(3):222-8. doi: 10.1002/jps.2600770308.
Diffusional solute release from an inert porous polymeric matrix was evaluated using sodium salicylate released from fused, inwardly tapered, polyethylene disk matrices (1.27 cm in diameter) with a central releasing hole. Two types of matrix were made by compressing (175 MPa) a sodium salicylate-melt polyethylene mixture with two different sets of circular conical punches having angles of 20 degrees and 30 degrees, with an axis perpendicular to the cone. The matrix sodium salicylate loading was greater than its solubility limit in the release medium. The fused matrices were coated with wax and perforated in their center to create a surface available for solute release. Flat disks with a central cylindrical hole were also made to compare the release profiles. An approximate solution was developed for these inwardly tapered disks and tested against experimental results. The theoretical model and experimental results showed good agreement and indicated that this type of matrix geometry may be useful as a pharmaceutical dosage form to approximate zero-order release.
使用从带有中心释放孔的熔融、向内渐缩的聚乙烯圆盘基质(直径1.27厘米)中释放的水杨酸钠,评估了惰性多孔聚合物基质中溶质的扩散释放。通过用两组不同角度(20度和30度)的圆形圆锥冲头压缩(175兆帕)水杨酸钠-熔融聚乙烯混合物来制备两种类型的基质,圆锥轴垂直于圆锥。基质中的水杨酸钠负载量大于其在释放介质中的溶解度极限。将熔融的基质涂上蜡并在其中心打孔,以形成可用于溶质释放的表面。还制作了带有中心圆柱孔的平盘以比较释放曲线。针对这些向内渐缩的圆盘开发了一个近似解,并与实验结果进行了对比。理论模型与实验结果显示出良好的一致性,表明这种类型的基质几何形状可用作近似零级释放的药物剂型。