摘要
目的：制备酮基布洛芬（ＫＴＰ）经皮吸收涂膜剂，研究其经皮吸收性能及抗炎作用。方法：采用双室渗透扩散装置，进行体外渗透试验；用大鼠为炎症模型，考察ＫＴＰ涂膜剂的抗炎作用。结果：ＫＴＰ涂膜剂体外透皮释药方程为：Ｑ＝０．４３８５ｔ－０．１０３０（ｒ＝０．９９９８），８ｈ累积渗透量为３．５０７ｍｇ·ｃｍ－２；本品对大鼠角叉莱胶性足趾肿胀，棉球性肉芽组织增生及大鼠佐剂性关节炎的原发病变和继发病变均有显著抑制作用。结论：涂膜剂使ＫＴＰ以零级动力学透过皮肤，可以提供比口服制剂稳定的血药浓度；ＫＴＰ具有显著抗炎作用。
OBJECTIVE: To prepare a ketoprofen film and study its transdermal delivery and anti inflammatory effect. METHODS: Ketoprofen permeation tests in vitro through rat skin in two compartment diffusion cells were performed and its anti inflammatory effect was studied on rats. RESULTS: The penetration equation of ketoprofen film was Q=0.438 5 t-0.103 0 (r=0.999 8). The cumulative release level in 8 h was 3.507 mg·cm -2 through rat skin in vitro. Ketoprofen film reduced the swelling of hind paw in rats caused by injection of carrageenin. It also inhibited the proliferation of granuloma induced by cotton pellet and reduced primary and recurrent inflammatory swelling of adjuvant arthritis in rat. CONCLUSION: The permeation of ketoprofen in film through the rat skin followed zero order kinetics. Ketoprofen film showed a remarkable anti inflammatory effect.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1997年第9期535-538,共4页
Chinese Pharmaceutical Journal
关键词
酮基布洛芬
涂膜剂
体外渗透
ketoprofen, film, in vitro penetration, anti inflammatory effect
