摘要
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。
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.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2016年第23期4362-4367,共6页
China Journal of Chinese Materia Medica
基金
江苏省高校自然科学研究项目(14KJB360001)
江苏省中药资源产业化过程协同创新中心项目(ZDXMHT-1-15)
江苏省"青蓝工程"和江苏省高校优势学科建设工程项目
关键词
中药挥发油
透皮吸收促进剂
凝胶
布洛芬
体内外相关性
essential oils
penetration enhancers
hydrogel
ibuprofen
in vitro/in vivo correlation