白芥子涂方穴位与非穴位给药皮肤渗透特性的比较研究

Tetrahydropalmatine′s permeative properties of acupoint and non-acupoint transdermal administration of Baijiezi Tufang in vitro and in vivo

目的:研究白芥子涂方经穴位和非穴位皮肤给药的渗透特性,为其临床穴位贴敷预防和治疗哮喘提供实验支持。方法:以白芥子涂方中延胡索乙素为评价指标,采用HPLC定量,用Franz扩散池法研究涂方离体经穴位和非穴位皮肤的渗透特性;在体渗透实验,采用冰冻切片法比较穴位与非穴位皮肤中各层药物的分布,并用荧光显微镜进行可视化验证。结果:24 h内,离体试验中延胡索乙素经穴位皮肤的累积透过量为(13.53±3.92)μg.cm-2,是经非穴位皮肤的4倍(P<0.05);穴位皮肤稳态透皮速率(0.659 1μg.cm-2.h-1)是非穴位(0.147 2μg.cm-2.h-1)的4.5倍;离体透皮试验和在体渗透试验中,24 h皮肤中药物滞留量均为穴位>非穴位(P<0.05),切片显示皮肤各层的药物含量为角质层>活性表皮>真皮层>皮下层。结论:白芥子涂方浸膏在穴位皮肤的透过量和皮肤滞留量均显著高于非穴位皮肤,验证了涂方临床使用以穴位经皮给药的科学性。

Objective： To study tetrahydropalmatine′s permeative properties of acupoint and non-acupoint transdermal administration of baijiezi tufang in vitro and in vivo.Method： Taking tetrahydropalmatine as an evaluative component to assess the permeative of baijiezi tufang in acupoint skin and non-acupoint skin with the modified Franz diffusion cell method and in vivo penetration studies.The content of tetrahydropalmatine was determined by a HPLC method.Result：The 24 hours cumulative permeation amount through acupoint skin was（13.53±3.92）μg·cm-2,about 4 times higher than non-acupoint skin.The steady-state infiltration rates of tetrahydropalmatine in acupoint skin was（0.659 1 μg·cm-2·h-1）,4.5 times higher than non-acupoint skin.The content in acupoint skin was signally higher than that in non-acupoint skin（P0.05）.An accumulation of fluorescence can be clearly seen in the four layers： stratum corneum viable epidermis dermis subcutaneous.Conclusion： In vitro and in vivo studies show that the permeation of baijiezi tufang in acupoint skin was better than in non-acupoint skin,following a higher cumulative amount and skin content.