Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy, Musashino University, Shinmachi 1-1-20, Nishi-Tokyo 202-8585, Japan.
J Pharm Sci. 2010 Jan;99(1):286-92. doi: 10.1002/jps.21835.
To improve the biocompatibility, inter-connective pore structure, and drug delivery ability of self-setting apatite/collagen composite cement (ACC), a three-dimensionally perforated porous apatite/collagen composite cement (TPPACC) containing 3% indomethacin (IMC) was obtained in an arranged multi-cross with 20, 40, and 60 stainless steel needlelike male dies, and stored and hardened at 37 degrees C and 100% relative humidity for 24 h. The mean radius of micro-pores of the TPPACC was evaluated to be 0.125 microm by mercury porosimetry. X-ray powder diffraction and FT-IR spectroscopy suggested that TPPACC consisted of carbonated apatite and had a structure similar to that of natural rat bone. The IMC release rates from a TPPACC block containing the drug were measured in simulated body fluid. The rate of release increased with the number of macro-pores that from planar surface matrix systems followed the Higuchi equation. The relationship between the Higuchi constant and surface area of TPPACC showed a straight line with K = 0.2123 and R(2) = 0.9892. These results indicated that the rate of drug release from TPPACC could be controlled by the number of macro-pores for bone cells.
为了提高自固化磷灰石/胶原复合骨水泥（ACC）的生物相容性、互联孔结构和药物输送能力，采用 20、40 和 60 根不锈钢针状 male 模具排列成三维多孔磷灰石/胶原复合骨水泥（TPPACC），并含有 3%吲哚美辛（IMC）。将其在 37°C 和 100%相对湿度下储存和硬化 24 小时。通过压汞法评估 TPPACC 的微孔平均半径为 0.125 微米。X 射线粉末衍射和 FT-IR 光谱表明，TPPACC 由碳酸磷灰石组成，其结构与天然大鼠骨相似。在模拟体液中测量了含有药物的 TPPACC 块的 IMC 释放率。释放率随大孔数量的增加而增加，而从平面基质系统的释放率则遵循 Higuchi 方程。Higuchi 常数与 TPPACC 表面积之间的关系呈直线关系，K=0.2123，R²=0.9892。这些结果表明，TPPACC 中药物的释放速率可以通过大孔的数量来控制，从而为骨细胞提供了一种可控的药物释放系统。
