低分子肝素透皮吸收制剂的研究

^Transdermal preparation of low molecular weight heparin

以低抗凝肝素为原料制备了平均分子量为５６００的低分子肝素，测定了理化指标和抗凝效价。分别制备了不合促进剂和含不同促透剂的低分子肝素和肝素Ｏ／ｗ型软膏。体外经皮渗透动力学实验结果表明，软膏中药物的透皮过程符合Ｆｉｃｋ’Ｓ扩散方程，并筛选软膏的最佳处方为：低分子肝素（或肝素）、Ｎ－甲基吡咯烷酮、基质。将该处方软膏敷于家兔背部脱毛皮肤一定时间，可显著延长血液凝固时间和抑制实验性血栓形成。

A Iow molecular weight heparin(LMWH)with average molecular weight of 5600was prepared from low anticoagulant activity heparin(LAAH).Its physicochemical parametersand anticoagulant activity were determined.Several kinds of o/w creams of LMWH and heparinwithout or with different penetration enhancers were prepared. Studies on the kinetics of thedrugs through skin in vitro showed that their penetration followed Fick's diffusion equation。Thebest formulation of the creams was chosen as LMWH(heparin),N-methyl pyrrolidone and base。This cream’s application on rabbit’s dorsal depilated skin for some time could prolong the bloodcoagulation time and inhibit the experimentaI thrombosis remarkably。