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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 prepare a celecoxib microemulsion gel to enhance the in vitro transdermal penetration of drugs and the relative bioavailability in vivo. Methods: The microemulsion region was obtained by pseudo-ternary phase diagram method, and the prescription proportion of each component in microemulsion was investigated by single factor. Commercial capsules as a control, investigated the celecoxib microemulsion gel in rabbits pharmacokinetics. Results: The content of Triacetin was 6.7%, polysorbate-80 was 21.5%, transcutol-p was 21.5%, water was 50% and celecoxib was 1.5 %, Carbomer 940 is 1%. CONCLUSION: Celecoxib microemulsion gel can improve the transdermal permeability and bioavailability of drug in vitro, which is expected to become a new transdermal drug delivery system.