Empirical Study On Acupoint Transdermal Absorption Of Dasuanxiaohuang Pasta

Dasuanxiaohuang Pasta is from 《Zhong Yi Tian Jiu Liao Fa》, which is composed with30g rhubarb、30g Sodium Sulfate、120g garlic and quantum satis old vinegar. Concoctingthose materia into a pasta, and then applying on Shenque acupoint, is used in the treatment ofintestinal obstruction.Objective： To discuss the transdermal absorption rule of point-applyingDasuanxiaohuang Pasta, so as to provide help for clinical to enact more reasonablemedication program.Methods：Use rhubarb anthraquinone ingredients-aloe emodin、rhein、emodin、chrysophanol、physcion as index, by using in vitro、in vivo, conduct a transdermal absorptionexperiment investigation in Dasuanxiaohuang Pasta, and compare the effec of drugtransdermal characteristic on different parts of the skin (abdomen、 back、lateral region ofabdomen)、 different excipient (vinegar、 ginger juice、 vegetable oil) and differentcompatibility.Result：1.Transdermal absorption in vitro experiments showed that: the transdermalabsorption of rhubarb anthraquinone ingredients on different parts of mice’s skin、differentexcipient and different compatibility are all zero-order kinetics; the8h accumulation transitdose and transdermal rate of every ingredient on mice’s skin of abbomen are all significantlyhigher than the back and lateral region of abdomen skin; using vinegar as excipient, the8haccumulation transit dose and transdermal rate of every ingredient are largest, followed byginger juice and vegetable oil; in the different compatibility test, the8h accumulation transitdose and transdermal rate of anagraph which is all ingredients are most, rhubarb-SodiumSulfate anagraph are slightly lower, followed by rhubarb-garlic anagraph, and only rhubarbanagraph are lowest.2. Transdermal absorption in vivo experiments showed that: aloe emodin、rhein、emodin、chrysophanol all occur bimodal behavior in rabbits’ vivo, that is appearing twice peak time.The first peak time of aloe emodin、rhein、emodin is2h, the second peak time is5h; the firstpeak time of chrysophanol is2h, the second peak time is6h. The respective elimination halflives of aloe emodin、rhein、emodin、chrysophanol in rabbits’ vivo are37.991、22.849、 24.465、31.179h, the respective AUC are12.392、12.050、71.732、32.166μg· mL-1·h.Conclusions：1. The transdermal absorption effect of applying Dasuanxiaohuang Pastaon mice’s skin of abdomen is better than the back and lateral region of abdomen skin.2. The excipient of Dasuanxiaohuang Pasta with vinegar is best, and followed by gingerjuice, vegetable oils is worst.3. Garlic and Sodium Sulfate have the auxoaction on the transdermal absorption ofrhubarb anthraquinone ingredients, Sodium Sulfate is greater than garlic.4. The four rhubarb anthraquinone ingredients in rabbits’ blood plasm all occurbimodal behavior, that may be associated with the twice Dasuanxiaohuang Pasta applying.5. The peaking about plasma concentration of transdermal absorption in vivo whenpoint-applying Dasuanxiaohuang Pasta is6h, so the best clinical medication program ofDasuanxiaohuang Pasta is applying total of6h.