中国临床药学杂志

目的 研究伏立康唑骨水泥链珠的体外释放规律。方法 在100级层流超净工作台内，将注射用伏立康唑（样品A、B、C，剂量分别为600、800、1 000 mg）加入骨水泥粉剂（40.8 g）中，制成伏立康唑骨水泥链珠。采用等距浸出法设定取样时间点，用液质联用的方法测定伏立康唑在模拟体液中的释放情况。结果 600、800、1 000 mg伏立康唑加入骨水泥制备的伏立康唑骨水泥链珠，其28 d累计释放率分别为（44.00±4.33）%、（34.16±2.34）%和（28.40±2.08）%，释放规律符合Weibull方程lnln[1/（1-F）]=0.349 8ln t-2.667 7(r=0.992 3)。以磺丁基醚-β-环糊精钠为辅料的伏立康唑加入骨水泥后总体释放率高于以羟丙基-β-环糊精为辅料的伏立康唑，差异存在统计学意义（P<0.05）。结论 伏立康唑骨水泥链珠具有一定的缓释性，600 mg伏立康唑加入40 g骨水泥，是较为合适的配比。以磺丁基醚-β-环糊精钠为辅料的伏立康唑加入骨水泥后释放率更高。

AIM To investigate the in vitro release pattern of voriconazole bone cement beads, to provide reference for clinical application. METHODS Voriconazole from different doses and manufacturers was added to bone cement to make bone cement chain beads. The sampling time points were set by the isometric leaching method, the concentration of the leaching solution was measured by ultra-performance liquid chromatography-tandem mass spectrometry to observe the release pattern of voriconazole bone cement beads. RESULTS The cumulative release rates of 600, 800, and 1 000 mg voriconazole added to bone cement after 28 days were(44.00 ± 4.33)%,(34.16 ± 2.34)%, and(28.40 ± 2.08)%. The release patterns followed the Weibull equation lnln[1/(1-F)] = 0.349 8 ln t-2.667 7(r = 0.992 3). The overall release rate of voriconazole in bone cement with sodium sulfonamide-β-cyclodextrin was higher than that of voriconazole with hydroxypropyl-β-cyclodextrin, and the difference was statistically significant(P < 0.05). CONCLUSION Voriconazole bone cement chain beads have certain sustained-release properties. Adding 600 mg of voriconazole to 40 g of bone cement is a more suitable ratio. Voriconazole supplemented with sodium sulfonamide-β-cyclodextrin has a higher release rate when added to bone cement.