基于微透析技术的双丹脂质体凝胶大鼠皮肤药动学研究

目的应用经皮微透析技术研究双丹脂质体凝胶(SD-Lip Gels)和双丹凝胶(SD-Gels)的皮肤药动学过程,考察其在体经皮渗透性能。方法采用增量法和减量法考察微透析探针体外回收率与传递率,采用反透析法测定探针体内回收率,采用微透析技术采集不同时间的皮下药物样品,结合HPLC法测定样品中丹参酮ⅡA(DST)和丹皮酚(DPF)的浓度,并用DAS 2.0软件进行数据处理,计算相关药动学参数。结果SD-Gels与SDLip Gels的达峰时间(tmax)相近,SD-Gels的药峰浓度(Cmax)高于SD-Lip Gels,但SD-Lip Gels的滞留时间(MRT)、以及曲线下面积(AUC)均比SD-Gels有所提升,药物总透皮量显著高于SD-Gels。结论SD-Lip Gels可延长药物在皮下组织中的滞留时间及有效浓度,具有更优的缓释作用,可望成为双丹方经皮给药的新剂型。

Pharmacokinetics of Shuangdan Liposome Gels in Rat Skin Based on Microdialysis Technology

Objective To study the dermal pharmacokinetics of Shuangdan liposome gels(SD-Lip Gels)by transdermal microdialysis technique,and investigate its transdermal permeability in vivo.Methods The in vitro recovery rate of microdialysis probe was investigated by Gain method and Loss method.The in vivo recovery rate of microdialysis probe was determined by retrodialysis method.Microdialysis technology was used to collect subcutaneous drug samples at different time,and the concentrations of tanshinone II A(DST)and paeonol(DPF)were determined by HPLC.DAS 2.0 software was used to process the data and calculate the relevant pharmacokinetic parameters.Results The peak time(tmax)of the two preparations were similar.The Cmax of Shuangdan gels(SD-Gels)was higher than that of SD-Lip Gels,while the mean residence time(MRT)and AUC of the latter were all higher than those of SD-Gels,and the total penetration of the drug was significantly higher than that of SD-Gels.Conclusion Compared with SD-Gels,the SD-Lip Gels can effectively promote the penetration of drugs into skin and has better sustained release effect,which is expected to become a new transdermal dosage form.