创伤涂膜剂的体外透皮吸收

目的:通过大鼠离体皮肤的体外透皮试验,考察创伤涂膜剂中的3种药物成分在皮肤内的渗透过程,明确药物的释放机制,为临床确定用药剂量和用药时间提供实验依据。方法:采用Franz扩散池法,以SD大鼠背部皮肤作为渗透屏障,采用高效液相色谱法测定3种药物的含量,以单位面积累积渗透量对时间拟合,分别考察:3种药物在大鼠背部完整皮肤和破损皮肤的透皮吸收特性。结果:替硝唑、盐酸达克罗宁、醋酸氯己定完整皮肤24 h累积渗透率分别为35.3%,18.0%,0%,破损皮肤24 h累积渗透率分别为78.6%,63.8%,5.2%。药物成分的释放特征不同,替硝唑和盐酸达克罗宁对破损皮肤的释放曲线符合Higuchi模型,对完整皮肤的释放曲线符合零级模型,醋酸氯己定的累积渗透量较低。结论:替硝唑和盐酸达克罗宁在完整皮肤和破损皮肤均可不同程度透过,醋酸氯己定的累积渗透量较低,仅发挥局部抗菌作用。

Study on in vitro transdermal absorption of film forming solution for trauma

OBJECTIVE To study the permeation process and releasing mechanism of three components of a film forming solution for trauma by in vitro transdermal experiments on isolated rat skin,and to provide experimental evidence for suitable application of this preparation in clinical,including dosage and interval.METHODS The transdermal experiment was conducted with improved Franz diffusion cell using the rat’s dorsal skin as permeation barrier which included complete and damaged skin.Drug concentration in receptive cell was determined by HPLC.The releasing curves of the studied drug were constructed by fitting cumulative transdermal amount per unit area with sampling time.RESULTS The cumulative permeation rate of tinidazole,dyclonine hydrochloride and chlorhexidine acetate during 24 hours were 35.3%,18.0%,0% on complete skin and 78.6%,63.8%,5.2% on damaged skin,respectively.The releasing curves of tinidazole and dyclonine hydrochloride were fitted to Higuchi model well on damaged rat skin,but zero level model on complete rat skin.The cumulative permeation amount of chlorhexidine acetate was very low,so it could not be fitted to any model.CONCLUSION Tinidazole and dyclonine hydrochloride can penetrate rat skin at different extent and showing different release characteristic on complete and damaged skin.While chlorhexidine acetate scarcely penetrate the skin,so it just played local antibacterial action.