兔血浆利福平的反相高效液相色谱分析及药代动力-第三军医大学学报.docVIP

异烟肼、利福平白蛋白纳米粒在兔脊柱中利福平的缓释研究 张惠勇1，马 荣3，陈 振3，刘晓印1，梁思敏3，黑 龙3，杨小英2，戈朝晖3 （1.宁夏医科大学研究生院，银川 750004；2.宁夏宁夏异烟肼、利福平白蛋白纳米粒（INH-RFP-BSA-NPs）经静脉给药后利福平（rifampicin， RFPRFP浓度的反相高效液相色谱分析方法（reversed - phase high - performance liquid chromatography，RP-HPLC）。选取39只新西兰大白兔，按公斤体重计算给药剂量，经耳缘静脉给药后，选择13个时相点（1，2，4，6，8，10，12，24，36，48，72，96，120h）处死，每个时相点处死三只，取腰椎椎体及邻近椎旁肌组织，RP-HPLC法检测其中RFP的药物浓度。结果：静脉注射纳米粒后2小时，RFP在兔椎体及椎旁肌组织中的药物浓度达到峰值，其后逐渐下降。96小时后椎旁肌中仍能测到高于定量下限的RFP，椎体中可延长至120小时。同一时相点椎体中RFP的药物浓度略高于椎旁肌组织。结论：载异烟肼、利福平白蛋白纳米粒经静脉给药后，RFP在兔体内可浓聚到椎体和椎旁肌组织，明显提高了椎体和椎旁肌组织中药物的分布并延缓其消除，证实该纳米粒有显著的靶向性分布及良好的缓释特性。 【关键词】：纳米粒；利福平；脊柱；椎旁肌；高效液相色谱法；生物分布。 Study on sustained-release effect of rifampicin from albumin nanoparticles loaded with isoniazid and rifampicin in rabbit’s spine ZHANG Huiyong1，MA Rong3，CHEN Zhen3，LIU Xiaoyin1，YANG Xiaoying2，GE Zhaohui3 (1.Graduate School of Ningxia Med.University，Yinchuan 750004;2.Depof Pharmacy，General Hospital of Ningxia Med.University，Yinchuan 750004;3.Dep of Orthopedics Sugery，the General Hospital of Ningxia MedUniversity，Yinchuan 750004)[Abstract] Objective: To study the biodistribution of rifampicin released from albumin nanoparticles loaded with isoniazid and rifampicin (INH-RFP-BSA-NPs) in rabbit’s spine and paravertebral muscles after intravenous administration. Methods: RP-HPLC(reversed－phase high－performance liquid chromatography) method established to determinate the rifampicin(RFP) in rabbit’s spine and paravertebral muscles. 39 healthy New Zealand white rabbits were injected medicine into the ear vein. The amount of rifampicin applied to each rabbit was calculated according to body weight in kilograms. After the intravenous injection of INH-RFP-BSA-NPs, three rabbits randomly selected were killed at each of the following time (1,2,4,6,8,10,12,24,36,48,72,96,120h). The vertebrals and paravertebral muscles were harvested simultaneously, and then the concentrations of rifampicin in vertebral bodies and paraspinal muscles from each were determinated by RP-HPLC. Results: Two ho