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引用本文:谢黎崖,詹传明,侯振清,陈月,吴永良.双修饰壳聚糖载丝裂霉素C纳米粒在大鼠体内的药动学研究[J].中国现代应用药学,2014,31(3):312-316.
XIE Liya,ZHAN Chuanming,HOU Zhenqing,CHEN Yue,WU Yongliang.Pharmacokinetics of Dual Conjugated Chitosan-mitomycin C Nanoparticles in Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(3):312-316.
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双修饰壳聚糖载丝裂霉素C纳米粒在大鼠体内的药动学研究
谢黎崖1, 詹传明2, 侯振清2, 陈月1, 吴永良1
1.厦门大学附属第一医院,福建 厦门 361003;2.厦门大学生物医学工程研究中心,福建 厦门 361005
摘要:
目的 研究双修饰壳聚糖载丝裂霉素C纳米粒在大鼠体内的药动学特征。方法 2组大鼠分别静脉注射4 mg·kg-1丝裂霉素C纳米粒和丝裂霉素C注射剂后,采用高效液相色谱-串联质谱法(HPLC-MS)测定给药后不同时间点血浆中丝裂霉素C的浓度,计算主要药动学参数。结果 丝裂霉素C的线性范围20~1 000 μg·L-1,最低定量限为20 μg·L-1,提取回收率均>95%,日内、日间精密度RSD均<15%。双修饰壳聚糖载丝裂霉素C纳米粒和丝裂霉素C注射剂t1/2分别为(2.64±0.11)h、(0.49±0.049)h;AUC0-∞分别为(2.01±0.11)mg·h-1·L-1、(0.93±0.075)mg·h-1·L-1;Vz分别为(1.52±0.18)L、(0.63±0.065)L;CL分别为(6.95±0.70)mL·min-1、(15.47±1.89)mL·min-1,2者均有显著性差异。结论 该方法灵敏、准确、专一,适用于丝裂霉素C的药动学研究。与丝裂霉素C注射剂相比,双修饰壳聚糖载丝裂霉素C纳米粒具有缓释和长循环的作用。
关键词:  丝裂霉素C  壳聚糖  纳米粒  高效液相色谱-质谱联用  药动学
DOI:
分类号:
基金项目:厦门市科学技术计划项目资助项目(3502Z20114007)
Pharmacokinetics of Dual Conjugated Chitosan-mitomycin C Nanoparticles in Rats
XIE Liya1, ZHAN Chuanming2, HOU Zhenqing2, CHEN Yue1, WU Yongliang1
1.First Affiliated Hospital of Xiamen University, Xiamen 361003, China;2.Research Center of Biomedical Engineering of Xiamen University, Xiamen 361005, China
Abstract:
OBJECTIVE To study the pharmacokinetics of dual conjugated chitosan-mitomycin C nanoparticles (CS-MMC-NPs) in rats. METHODS The two groups of rats were injected with CS-MMC-NPs and MMC injection at the dose of 4 mg·kg-1. The concentrations of MMC in plasma at different time were determined by HPLC-MS and the main pharmacokinetic parameters were calculated. RESULTS The calibration curves were linear over the range of 20-1 000 μg·L-1. The limit of quantitation was 20 μg·L-1. The within day and day to day relative standard deviation(RSD) was <15%. The main pharmacokinetic parameters of CS-MMC-NPs and MMC injection were as follows: t1/2 were (2.64±0.11)h and (0.49±0.049)h, AUC0-∞ were (2.01±0.11)mg·h-1·L-1 and (0.93±0.075)mg·h-1·L-1, Vz were (1.52±0.18)L and (0.63±0.065)L, CL were (6.95±0.70)mL·min-1 and (15.47±1.89)mL·min-1. The differences of parameters were significant between two preparations. CONCLUSION The method is sensitive, accurate, specific for the pharmacokinetic study of CS-MMC-NPs. Compared with MMC injection, CS-MMC-NPs has a controlled releasing rate, a high level of blood concentrations and a long blood circulation time, which benefits the control of acute toxicity of MMC for the rats.
Key words:  mitomycin C  chitosan  nanoparticles  HPLC-MS  pharmacokinetics
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