ZL-004的PLGA纳米粒的大鼠肠吸收特征  

Intestinal Absorption of PLGA Nanoparticles Loaded with ZL-004

作　　者：赵锋[1] 栾瀚森[1] 马银玲[2] 张晓红[3] 王浩[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203 [2]河北省人民医院药学部,河北石家庄050051 [3]上海现代制药股份有限公司嘉定基地,上海201800

出　　处：《中国医药工业杂志》2014年第1期49-55,共7页Chinese Journal of Pharmaceuticals

基　　金："十二五重大新药创制"注射用可降解药用辅料PLGA的产业化研究项目(2011ZX09401-403-1)

摘　　要：采用超声乳化均质法制备包裹ZL-004（1）的PLGA纳米粒（1-NP），其体外释放明显高于原药。以单向灌流法考察1-NP的大鼠在体肠吸收性质。结果表明，1-NP在大鼠各肠段均有吸收，且吸收系数（Ka）与渗透系数（Peff）均显著大于其原药（P〈0．01）。1-NP在小肠段（十二指肠、空肠和回肠）的Ka与Peff均显著大于结肠（P〈0．01），且各肠段吸收量随1浓度（5～20μg／ml）的增加而增加。The PLGA nanoparticles loaded with ZL-004 （1） were prepared successfully by ultrasonic homoemulsification method. The in vitro release rate from the product was higher than that of the bulk drug. Then the intestinal absorption of 1 PLGA nanoparticles in rats was investigated by means of in situ single pass perfusion model. The absorption was observed in the whole intestinal tract. The absorption constant （Ka） and the effective absorption coefficient （Pete） of 1 nanoparticles were higher than those of the bulk drug （P〈0.01）. The Ka and Peff of I nanoparticles at small intestine （duodenum, jejunum and ileum） were higher than those at colon （P〈0.01）. In addition, the accumulative absorption amounts of 1 nanoparticles at different segments of intestinal tract were increased with the increasing of drug concentration in the range of 5 - 20 μg/ml.

关 键 词：ZL-004 在体单向灌流 肠吸收 

分 类 号：R944.9[医药卫生—药剂学]