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乙酰半胱氨酸纳米粒的制备及在小鼠体内的分布
引用本文:王福根,庄让笑,席建军,方红英,高建青.乙酰半胱氨酸纳米粒的制备及在小鼠体内的分布[J].中国医药工业杂志,2012(7):572-576.
作者姓名:王福根  庄让笑  席建军  方红英  高建青
作者单位:1. 浙江大学药学院,浙江杭州310058;浙江中医药大学附属第六医院,浙江杭州310014
2. 浙江中医药大学附属第六医院,浙江杭州,310014
3. 浙江大学药学院,浙江杭州,310058
摘    要:以壳聚糖为载体,溶剂扩散法制备乙酰半胱氨酸纳米粒,制得的纳米粒呈大小均匀的球形,平均粒径(163.0±12.8)nm,包封率(81.2+1.2)%,载药量(28.9+0.4)%。用HPLC法测定了小鼠单剂量尾静脉注射乙酰半胱氨酸纳米粒或其注射液后各脏器(心、肝、脾、肺和肾)和血浆中的药物浓度,并以相对摄取量和靶向效率评价纳米粒的靶向性。结果表明,纳米粒明显改变了药物在小鼠体内的生物分布。与注射液组相比,纳米粒组在肝组织中乙酰半胱氨酸浓度明显提高,血浆、心和肾组织中的药物浓度显著降低。

关 键 词:乙酰半胱氨酸  纳米粒  壳聚糖  组织分布  制备

Preparation and Distribution in Mice of Acetylcysteine Nanoparticles
Authors:WANG Fugen  ZHUANG Rangxiao  XI Jianjun  FANG Hongying  GAO Jianqing
Institution:1) (1.College of Pharmaceutical Sciences,Zhejiang University,Hangzhou 310058;2.The Sixth Hospital Affiliated to Zhejiang University of Traditional Chinese Medicine,Hangzhou 310014)
Abstract:The acetylcysteine nanoparticles were prepared with chitosan as the carrier by solvent diffusion method.The average diameter,encapsulation efficiency and drug loading of products with a spherical appearance were (163.0±12.8)nm,(81.2±1.2)%and(28.9±0.4)%,respectively.The drug concentrations in plasma and several tissues (heart,liver,spleen,lung and kidney) of mice after iv administration of acetylcysteine nanoparticles or its injection with a single dose were determined by HPLC.The relative tissue exposure(R_e) and targeting efficiency(T_e) were calculated to evaluate the targeting effect of acetylcysteine nanoparticles.The results showed that the nanoparticles significantly changed the drug distribution in mice.Compared with the injection group,the acetylcysteine concentration in liver of prepared nanoparticles group was significantly increased while the concentrations in plasma,heart and kidney were decreased.
Keywords:acetylcysteine  nanoparticle  chitosan  tissue distribution  preparation
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