中药挥发油透皮促渗布洛芬的药动学及体内外相关性研究

考察不同中药挥发油透皮促渗布洛芬的药动学及体内外相关性。以经典促渗剂氮酮为对照,分别制备含不同中药挥发油(川芎挥发油、当归挥发油和肉桂挥发油)的布洛芬凝胶剂,大鼠腹部给药,考察不同挥发油对布洛芬的透皮促渗效果。与不加促渗剂的对照组相比,川芎挥发油、当归挥发油、肉桂挥发油和氮酮促渗布洛芬的相对生物利用度分别为161.87%,171.05%,151.37%,148.66%。采用反卷积法分别对3种中药挥发油促渗下布洛芬凝胶体内外透皮的数据进行相关性分析,结果表明含川芎挥发油、当归挥发油和肉桂挥发油的3种布洛芬凝胶剂体内外透皮吸收结果相关性良好(r分别为0.999 7,0.995 2,0.999 4)。川芎挥发油、当归挥发油和肉桂挥发油能够显著提高布洛芬经皮给药的生物利用度,以凝胶剂为剂型的中药挥发油透皮促渗研究具有良好的体内外相关性。

Evaluation of pharmacokinetics and in vitro/in vivo correlation of ibuprofen with essential oils as penetration enhancer following transdermal administration

The study was carried out to investigate the pharmacokinetics and in vitro/in vivo correlation of ibuprofen with essential oils as penetration enhancers (PE) following transdermal administration. With Azone as the positive control, ibuprofen hydrogels containing Chuanxiong oil, Angelica oil or Cinnamon oil as PE were prepared and administered to the rat abdominal skin. Then the pharmacokinetics of ibuprofen following transdermal administration were investigated and compared. In comparison with negative control (no PE was added), the relative bioavailability values with the addition of Chuanxiong oil, Angelica oil, Cinnamon oil and Azone as PE were determined to be 161.87%, 171.05%, 151.37% and 148.66%, respectively. In vitro/in vivo correlation analysis was performed by deconvolution method and the results demonstrated a good correlation between in vitro and in vivo percutaneous absorption studies. The correlation coefficients were measured to be 0.999 7, 0.995 2 and 0.999 4 for Chuanxiong oil, Angelica oil and Cinnamon oil respectively. In summary, Chuanxiong oil, Angelica oil and Cinnamon oil as PE could significantly enhance the bioavailability of ibuprofen following transdermal administration. A satisfactory in vitro/in vivo correlation could be obtained by using hydrogel as the dosage form.