阿苯达唑纳米微粉在大鼠体内的药动学研究  

Pharmacokinetics Study of Albendazole Nano-powder in Rats

作　　者：马运芳[1] 王建华[1] 陈迹[1] 任洁如 

机构地区：[1]新疆医科大学第一附属医院药学部,乌鲁木齐830011

出　　处：《中国药房》2016年第34期4797-4799,共3页China Pharmacy

基　　金：新疆包虫病重点实验室项目(No.XJDX0202-2013-5)

摘　　要：目的：研究阿苯达唑（ABZ）纳米化后在大鼠体内的药动学变化,为ABZ纳米制剂的进一步研发奠定基础。方法：将16只大鼠随机分为ABZ原料药组（ABZ原料药混悬液）与ABZ纳米微粉组（ABZ纳米微粉混悬液）,每组8只,ig给药,剂量为63 mg/kg。各组大鼠于给药0.5、1、2、4、8、12、24、36、48、72 h后眼眶采血0.20.3 ml,以甲苯咪唑为内标,采用反相高效液相色谱法（RPHPLC）测定各时间点药物血药浓度,并采用3p97药动学软件拟合药动学参数。结果：ABZ原料及纳米微粉在大鼠体内的药动学符合二室模型,ABZ原料药组、ABZ纳米微粉组大鼠的cmax分别为（3.20±1.41）、（6.11±0.74）μg/ml,tmax分别为（3.42±0.91）、（3.15±0.27）h,t1/2分别为（7.53±1.20）、（6.26±0.85）h,AUC0-72h分别为（49.90±15.50）、（78.36±8.78）μg·h/ml,AUC0-∞分别为（52.30±10.10）、（80.27±8.26）μg·h/ml。与ABZ原料药组比较,ABZ纳米微粉组大鼠的cmax、AUC0-72h、AUC0-∞均显著升高（P〈0.05）。结论：ABZ纳米化后在一定程度上提高了药物的吸收速率,增加了药物的吸收,提高了ABZ的口服生物利用度。OBJECTIVE：To study the pharmacokinetic change of albendazole（ABZ） in rats after nanocrystallization,and to lay a foundation for further study of ABZ nano-preparation.METHODS：16 rats were randomly divided into ABZ raw material（ABZ suspension） group and ABZ nano-powder（ABZ nano-powder suspension） group,with 8 rats in each group.They were given relevant medicine 63 mg/kg intragastrically.0.2-0.3 ml blood samples were collected from orbital cavity 0.5,1,2,4,8,12,24,36,48,72 h after medication,respectively.Using mebendazole as internal standard,blood concentration of ABZ were determined by RP-HPLC,and pharmacokinetics parameters were calculated by using 3p97 software.RESULTS：The pharmacokinetics of ABZ raw material and ABZ nano-powder in rats were in line with two-compartment model.The main pharmacokinetic parameters of ABZ raw material group vs.ABZ nano-powder group were as follows as cmax（3.20±1.41） μg/ml vs.（6.11±0.74） μg/ml;tmax（3.42±0.91） hvs.（3.15±0.27） h;AUC0-72h（49.90±15.50） μg·h/ml vs.（78.36±8.78） μg·h/ml;AUC0-∞（52.30±10.10） μg·h/ml vs.（80.27±8.26） μg·h/ml.Compared with ABZ raw material group,cmax,AUC0-72h and AUC0-∞ of ABZ nano-powder group were increased significantly（P〈0.05）.CONCLUSIONS：The nanocrystallization of ABZ can enhance the absorbability rate and improve the absorption of drugs to some extent,and it also improves oral bioavailability of ABZ.

关 键 词：阿苯达唑 纳米微粉 药动学 大鼠 

分 类 号：R917[医药卫生—药物分析学]