不同剂型扑热息痛离体透皮吸收效果研究

Effects of Different Dosage Form of Paracetamol on Its Percutaneous Absorption in Vitro

目的:研究卡波姆凝胶、微乳、微囊、微囊凝胶、脂质体、脂质体凝胶等不同给药剂型对扑热息痛离体经皮渗透的效果。方法:使用Franz体外释药装置,采用紫外分光光度法检测接受液中扑热息痛的浓度并计算药物的经皮累积释放量。结果:各种剂型的扑热息痛均有经皮吸收作用,剂型不同吸收效果不同。透皮速率常数值由大到小的顺序为微囊>脂质体>微乳>脂质体凝胶>微囊凝胶>卡波姆凝胶,数据分别为387.93、353.71、220.75、120.93、114.76、84.02μg.cm-2.h-1,其中脂质体和微囊剂型的透皮吸收效果明显优于微乳和各种凝胶剂(P<0.05)。结论:脂质体和微囊适合作为扑热息痛经皮制剂的给药剂型。

OBJECTIVE： To investigate the effects of different dosage form （carbomer gel, mieroemulsion, microcapsule, microcapsule gel, liposome, liposome gel etc.） of paracetamol on its percutaneous absorption in vitro. METHODS： Franz diffusion cell was used to investigate the cumulative release amount of paracetamol which was determined by ultraviolet speetrophotometer, and the transdermal cumulative amount of the drug was computed. RESULTS： Different dosage forms of paraeetamol were all found to have different percutaneous absorption. The permeation rate constant of microcapsule was the highest, followed in descending order were microcapsule〉 liposome〉 microemulsion 〉 liposome gel〉 microcapsule gel 〉 carbomer gel （387.93, 353.71, 220.75, 120.93, 114.76, and 84.02 ug·cm^-2· h^-1, respectively）, with liposome and microcapsule showing significantly better percutaneous absorption efficacy than micromulsion and other gels （P〈0.05） . CONCLUSION： It is shown that liposome and microcapsule were the optimal dosage forms of paracetamol.