摘要
为提高核苷类药物对乙型肝炎的疗效并降低其毒性，用乳化聚合法制备了万乃洛韦聚氰基丙烯酸正丁酯毫微粒，对其形态、大小及其分布、体外释药特性、载药量、初步稳定性、动物体内的分布和体外肝细胞的摄取情况进行了研究。结果表明，该毫微粒粒径ｄａｖ＝１０４７７±１１７８ｎｍ；载药量１１２０％；包封率８４８５％；体外释药符合双相动力学规律；对肝细胞具有通透性；静注后１５ｍｉｎ有７４４９％集中在肝脏。提示。
The valaciclovir polybutylcyanoacrylate nanoparticles (VACAPBCANP) were prepared by emulsion polymerization method. The morphology, size and size distribution, release characteristics in vitro, drug loading, stability and distribution of VACVPBCANP in mice were studied. The results showed that the dav=10477±1178 nm, drug loading was 1120%. The release characteristics in vitro was in accord with twophase kinetics. 7449% of the VACV were concentrated in liver at 15 min after iv VACAPBCANP. The amount of VACV entering hepatocytes was also increased greatly. This research seems to have important value for increasing the antihepatitis B virus effect and decreasing toxicity of VACV.
出处
《药学学报》
CAS
CSCD
北大核心
1998年第9期702-706,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
万乃洛韦
毫微粒
肝靶向给药系统
乙型肝炎
Valaciclovir
Polybutylcyanoacrylate nanoparticles
Liver targeting drug delivery system
