乙酰半胱氨酸纳米微球药动学及药效学评价  

Evaluation of pharmacokinetics and pharmacodynamics of acetylcysteine nanospheres in mice

作　　者：王福根[1] 庄让笑[1] 沈益琴[1] 方红英[1] 席建军[1] 

机构地区：[1]浙江中医药大学附属西溪医院

出　　处：《中国临床药理学与治疗学》2013年第2期136-141,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：浙江省医药卫生科技计划项目(2009A170);杭州市医药卫生科技计划项目(2009A023)

摘　　要：目的:对制备乙酰半胱氨酸纳米微球进行药动学和药效学评价。方法:尾静脉注射乙酰半胱氨酸纳米微球和乙酰半胱氨酸,不同时间检测血浆和各脏器的乙酰半胱氨酸。通过皮下注射CCl4建立大鼠肝损伤模型,不同剂量乙酰半胱氨酸纳米微球进行治疗,检测血清学指标和肝组织各项指标评价纳米微球治疗慢性肝损伤的疗效。结果:乙酰半胱氨酸纳米微球改变了药物在体内的分布,肝组织中药物浓度明显提高,半衰期显著增加。药效实验显示,纳米微球能降低血清学指标,提高肝组织抗氧化功能,减轻肝细胞脂肪变性、细胞浸润和坏死。结论:乙酰半胱氨酸纳米微球具有明显肝靶向性,有利于肝损伤的药物治疗,是一种比较理想的乙酰半胱氨酸新剂型。AIM. To evaluate the pharmacoki- netics and pharmacodynamics of acetylcysteine nanospheres. METHODS.. Two groups of NAC nanoparticles and free drug groups were injected into mouse tail vein. NAC was detected in plas- ma and different organs at different time. Chro- nic liver injury model was established by subcu- taneous injection of carbon tetrachloride in rats. Different doses of NAC nanoparticles were ad- ministrated. Treatment of NAC nanospheres ef- ficacy was evaluated on serum markers and indi- cators of liver tissue. RESULTS. Acetylcysteine nanospheres changed the distribution of drugs in the body. The results showed that drug concen- tration significantly increased in the liver tissue,half-life increased obviously. Pharmacodynamics result showed that the nanospheres can reduce serum markers and improve hepatic antioxidant function. Liver biopsy showed that the nano- sphere treatment groups ameliorated hepatic steatosis, inflammatory and necrosis. CONCLU- SION. The acetylcysteine nanosphere had obvi- ous liver targeting, improving therapy for liver injure. Nanospheres are an ideal new formula- tions for acetylcysteine.

关 键 词：乙酰半胱氨酸 纳米微球 药动学 药效学 

分 类 号：R969.1[医药卫生—药理学]