白头翁素凝胶剂的体外经皮渗透及小鼠抗炎试验

Transdermal penetration of anemonin gels and its anti-inflammation test in mice

目的:设计白头翁素凝胶剂,考察不同浓度羟丙甲基纤维素(HMPC)及月桂氮芯卓酮对白头翁素体外经皮渗透的影响,观察优选处方的抗炎作用。方法:制备不同组分的白头翁素含醇凝胶剂,采用TK-6A型透皮扩散仪,用人皮进行体外渗透试验;用HPLC法测定各时间点接受室中药物浓度,求算经皮渗透的相关参数。用二甲苯使小鼠耳壳致肿,测定白头翁素凝胶剂对肿胀的抑制作用。结果:HPMC含醇凝胶剂作为基质时白头翁素经皮渗透速率1%HPMC>3%HPMC>5%HPMC;月桂氮芯卓酮对其有显著的透皮促进作用;含3%月桂氮芯卓酮的白头翁素1%HMPC凝胶剂可明显抑制二甲苯引起的耳壳肿胀。结论:白头翁素凝胶剂有望开发成为一种新型的中药抗炎经皮吸收制剂。

OBJECTIVE To investigate the effects of different concentration of HPMC and azone on the permeating charac teristies of anemonin in various gels vehicle in vitro and observe the anti-inflammatory effects of anemonin gel to develop a new anti-inflamrnatory transdermal preparation. METHODS The penetrating experiments were performed using human skin on modified Franz diffusion cells in vitro. The concentrations of anemonin in receptor compartment at specified time points were determined by HPLC. The steady flux and the accumulative quantity of anemonin permeating through skin were calculated. Determined the effects of anemonin gel on the inflammatory edema of ear induced by xylol in mice. RFNULTS The flux of anemonin through human skin from HPMC gel was 1% HPMC〉3%HPMC〉5% HPMC; and the anemonin gel can markedly inhibited the inflammatory edema in the ear of mice induced by xylene. CONCLUSION The anemonin gel can be developed as a new anti-inflammatory transdermal preparation.