Früher|Nächster

Local pharmacokinetics of the transdermal drug delivery of Dinggui San in the umbilical region

  • role： First author第一作者
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

  • Introduction：张永太，男，博士，教授，博士生导师
ZHANG Yongtai1,  
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

HOU Xiaolin1,  
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

SHEN Huifang1,  
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

TIAN Ting1,  
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

ZHANG Kai1,  
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

LI Zhe1,  
  • role： Corresponding author通信作者
  • Affiliation：

    Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China

  • Email：npfeng@shutcm.edu.cn
  • Introduction：Prof. FENG Nianping, Ph.D., Doctoral Supervisor. Shanghai University of Traditional Chinese Medicine, No.1200, Cailun Road, Pudong New District, Shanghai 201203. E-mail: npfeng@shutcm.edu.cn
FENG Nianping1*

Resümee

ObjectiveWe sought to compare the local pharmacokinetics of the active ingredients in the skin after the transdermal administration of Dinggui San(powder made from cloves and cinnamon) on the CV8, the position beside the CV8, and oral administration using a microdialysis technique.MethodsMale SD rats in a SPF grade were divided into four groups(n=4 each): the group of normal rats administered Dinggui San on CV8(N-CV8), the group of ulcerative colitis rats administered on CV8(UC-CV8), the group of ulcerative colitis rats administered on the position beside 2 mm CV8 group(UC-PA), and the group of ulcerative colitis rats administered orally(UC-oral). After modeling, the rats in the group received the corresponding administration with 0.1 g each(external use or oral). A microdialysis linear probe was implanted into the subcutaneous tissues of the corresponding external administration regions or CV8 in UC-oral, and perfused with 20% ethanolic saline solution at a flow rate of 0.2 mL/h. After 15 min of administration, the receiving fluid was collected every 30 min, and altogether collected 20 times, lasted 600 min. The receiving fluid was collected and directly analyzed by HPLC for the determination of cinnamic acid, a metabolite of cinnamaldehyde, and eugenol, as the main active ingredients in Dinggui San. The data obtained were fitted to a non-compartment model using the DAS 2.1 pharmacokinetic analysis software to analyse and compare pharmacokinetic parameters.ResultsThe forward recovery rates in vitro of eugenol and cinnamic acid were 41.4%±2.6% or 51.6%±2.1%, and the reverse recovery rates in vitro were 45.9%±1.5% or 50.6%±0.6%. The average recovery rates in vivo of eugenol and cinnamic acid were 40.4%, 42.8%. At each time point, the mass concentration in the skin of eugenol of all external administration groups were higher than that of UC-oral(less than 0.15 mg/L), and that of UC-CV8 was the highest. The area under the concentration-time curve from time 0 to last time of quantifiable concentration(AUC0-t) and maximum concentration(Cmax) of eugenol increased significantly, compared with N-CV8, UC-PA and UC-oral(P<0.05). At the most time points, the mass concentration in the skin of cinnamic acid of UC-oral were lower(less than 0.15 mg/L). Of all the four groups, AUC0-t and Cmax of cinnamic acid in UC-oral were the lowest and that in UC-CV8 highest. The differences of UC-oral to UC-CV8 were significant(P<0.05).ConclusionThe transdermal umbilical administration of Dinggui San improves the absorption and distribution of the active ingredients in the local skin tissues. The microdialysis technique seems to be suitable for evaluation of TCM compound prescription via percutaneous delivery.

Schlüsselwort

clove;cinnamon;ulcerative colitis;microdialysis;pharmacokinetics;eugenol;cinnamic acid;rats

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