摘要
目的:考察不同粒径的托氟啶(TFu)脂质体对小鼠口服吸收的影响。方法:按照托氟啶脂质体的处方工艺,采用薄膜分散-乳匀法分别制备530、320和180 nm三种粒径的托氟啶脂质体,并考察脂质体的Zeta电位、多分散性、包封率和体外释药等特性;将托氟啶混悬液和托氟啶脂质体分别给予小鼠灌胃,给药剂量均为100 mg/kg,在设定的时间点于眼底静脉丛取血,采用HPLC法测定托氟啶的血药浓度。用DAS(2.0)程序计算药物动力学参数,比较不同粒径组脂质体的相对生物利用度。结果:小鼠口服530、320和180 nm的托氟啶脂质体后的相对生物利用度分别为160.5%,221.6%和260.3%。结论:脂质体粒径对促进托氟啶的口服吸收有显著影响,口服吸收生物利用度随脂质体粒径的减小而增大。
Objective： To investigate the oral absorption effect of liposomes with different sizes on TFu in mice. Methods： Based on former studies, TFu liposomes of different particle sizes （530 nm, 320 nm and 180 nm） were prepared using the film dispersion-homogenization technique. The Zeta potentials and the polydispersity were evaluated by laser scatter analysis. The entrapment efficiencies were determined and the release characteristics in vitro were investigated. The mice were orally administered suspensions of TFu and liposomes of different particle sizes and venous blood was collected from the eyeholes of mice at a regular time. The plasma concentration of TFu was measured using the HPLC method and the pharmacokinetic parameters were calculated by the DAS（2.0） program. Results： The relative bioavailabilities of TFu liposomes with different particle sizes （530 nm, 320 nm and 180 nm） were 160.5%, 221.6%, and 260.3 %, respectively. Conclusion： The particle size of liposomes has a significant influence on oral absorption of TFu in mice： the relative bioavailability of liposomes increases with a decrease of particle size.
出处
《山东大学学报（医学版）》
CAS
北大核心
2007年第6期639-642,645,共5页
Journal of Shandong University:Health Sciences
