摘要
目的:制备一种塞来昔布微乳凝胶,以此提高药物的体外透皮渗透和体内的相对生物利用度。方法:通过伪三元相图法得到微乳区,并利用单因素考察微乳中各个成分的处方比例。市售胶囊剂作为对照,考察了塞来昔布微乳凝胶在家兔体内药动学。结果:塞来昔布微乳凝胶各组分的质量百分含量Triacetin为6.7%,聚山梨酯-80为21.5%,Transcutol-p为21.5%,水为50%,塞来昔布为1.5%,卡波姆940为1%。结论:塞来昔布微乳凝胶较好地提高药物体外透皮渗透性能以及生物利用度,有望成为一种新型的经皮给药系统。
Objective： To develop microemulsion-based organogels（ MBGs） to enhance the in vitro transdermal penetration and bioavailability of celecoxib. Methods： Microemulsion was obtained based on the pseudo-ternary phase diagram. By using single-factor test,the formation of microemulsion was optimized. Pharmacokinetics of MBGs in experimental rabbits was studied in comparison with the marketed capsules. Results： The celecoxib microemulsion gel was composed of triacetin 6. 7%,21. 5% Tween-80,21. 5% Transcutol-p,50% water,1. 5% celecoxib,and 1% carbopol 940. Conclusion： The devoloped MBGs have improved bioavailability and may be a new delivery system for transdermal administration of celecoxib.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2016年第9期1075-1080,共6页
Chinese Journal of New Drugs
关键词
塞来昔布
微乳
凝胶
伪三元相图
经皮给药
药动学
celecoxib
microemulsion-based organogels
pseudo-ternary phase diagram
transdermal release
pharmacokinetics
