Graduate School of Pharmaceutical Sciences, Tokyo University of Science, Noda, Chiba, Japan.
J Appl Biomater Funct Mater. 2012 Jun 26;10(1):22-8. doi: 10.5301/JABFM.2012.9272.
Bio-convertible artificial bone with slow release of anti-osteoporosis drug is useful to treat osteoporosis. Apatite cement containing 6% simvastatin (APD) had lower crystallinity than natural bone. In-vitro drug release tests in simulated body fluid (pH 7.8) and acetate buffer (pH 4.5) were performed at 37.0 C as physical models of osteoblast and osteoclast conditions (SOB and SOC). The device had lower drug release rate under SOB, but significantly higher rates under SOC. The simvastatin release rate changed depending on dissolution media, it repeated twice, and the rate under SOC was 15 times higher than under SOB. The device showed dissolution medium responsive drug release. After implantation of the APD in osteoporosis rats, the bone mineral density was evaluated by the x-ray computed tomography. The result indicated that the bone mineral density of APD implanted rat was significantly higher than that of control diseased. The result indicated that the device was therapeutically useful to bone regeneration.
具有抗骨质疏松药物缓慢释放功能的生物转化型人工骨可用于治疗骨质疏松症。载有 6%辛伐他汀的磷酸钙骨水泥（APD）的结晶度比天然骨低。在 37°C 下的模拟体液（pH7.8）和醋酸缓冲液（pH4.5）中进行体外药物释放试验，作为成骨细胞和破骨细胞条件（SOB 和 SOC）的物理模型。该装置在 SOB 下的药物释放率较低，但在 SOC 下的释放率显著更高。辛伐他汀的释放率取决于溶解介质，它重复了两次，在 SOC 下的释放率比 SOB 下高 15 倍。该装置表现出溶解介质响应性药物释放。将 APD 植入骨质疏松症大鼠后，通过 X 射线计算机断层扫描评估骨矿物质密度。结果表明，APD 植入大鼠的骨矿物质密度明显高于对照组患病大鼠。结果表明，该装置对骨再生具有治疗作用。
