| 引用本文: | 谷福根，李文妍，孟根达来，王毅，吴春芝，张爱武.诺氟沙星-磺丁基醚-β-环糊精包合物在大鼠体内的药动学研究[J].中国现代应用药学,2012,29(4):346-349. |
| GU Fugen, LI Wenyan, MENG Gendalai, WANG Yi, WU Chunzhi, ZHANG Aiwu.Pharmacokinetic Study of Norfloxacin-Sulfobutylether-β-Cyclodextrin Complex in Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(4):346-349. |
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| 摘要: |
| 目的 研究诺氟沙星(NFX)-磺丁基醚-β-环糊精(SBE-β-CD)包合物在大鼠体内的药动学行为。方法 大鼠分别灌胃给予NFX及其SBE-β-CD包合物，采用HPLC测定给药后不同时间的血药浓度并计算有关药动学参数。结果 NFX及其SBE-β-CD包合物的Cmax分别为(3.57±2.46)μg·mL-1和(6.92±4.03)μg·mL-1；AUC0-∞分别为(9.94±5.72)μg·h·mL-1和(14.63±5.39)μg·h·mL-1，两组间差异有统计学意义(P<0.05)；包合物相对于原药的生物利用度为147.2%。结论 NFX制成SBE-β-CD包合物后，其在大鼠体内的吸收速度有所加快，血药峰浓度以及生物利用度显著增加。 |
| 关键词: 诺氟沙星 磺丁基醚-β-环糊精 包合物 大鼠 药动学 生物利用度 |
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| 基金项目:内蒙古自然科学基金资助课题(2009MS1202) |
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| Pharmacokinetic Study of Norfloxacin-Sulfobutylether-β-Cyclodextrin Complex in Rats |
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GU Fugen, LI Wenyan, MENG Gendalai, WANG Yi, WU Chunzhi, ZHANG Aiwu1,2
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1.Department of Pharmacy, Affiliated Hospital of Inner Mongolia Medical College, Hohhot 010050, China;2.School of Pharmacy, Inner Mongolia Medical College, Hohhot 010100, China
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| Abstract: |
| OBJECTIVE To study the pharmacokinetic behavior of NFX-SBE-β-CD complex in rats. METHODS NFX and its SBE-β-CD complex were administered orally to two groups of rats, respectively. The plasma NFX concentrations at different time following administration were determined by HPLC to estimate the main pharmacokinetic parameters. RESULTS The Cmax values for NFX and its SBE-β-CD complex were (3.57±2.46)μg·mL-1 and (6.92±4.03)μg·mL-1, AUC0-∞ were (9.94±5.72)μg·h·mL-1 and (14.63±5.39)μg·h·mL-1, respectively. The Cmax and AUC0-∞ values for the complex were significantly greater than those of NFX(P<0.05). The relative bioavailability of the NFX complex was 147.2%. CONCLUSION The absorption rate, especially the plasma drug peak concentration and bioavailability of the drug in rats were significantly increased by the complex formation of NFX with SBE-β-CD. |
| Key words: norfloxacin SBE-β-CD complex rats pharmacokinetics bioavailability |
