摘要
目的建立大鼠脑组织中天麻苷元的HPLC测定方法,并研究川芎对天麻苷元在大鼠脑内药动学的影响。方法 144只SD大鼠随机分为天麻单用组(灌胃给予天麻提取物0.945 mg.kg-1)和天麻-川芎配伍组(灌胃给予天麻提取物0.945 mg.kg-1和川芎提取物3.78 mg.kg-1),于给药后不同时间点取脑组织。采用HPLC法测定大鼠脑组织中天麻苷元的浓度,以DAS2.0药动学软件计算药动学参数。结果天麻苷元在0.125～8 mg.L-1(r=0.999 6)范围内线性关系良好,绝对回收率为86.54%～89.96%,日内及日间精密度均低于5%。天麻-川芎配伍组中天麻苷元脑内药物浓度曲线下面积为天麻单用组的1.66倍;平均滞留时间延长,清除率为天麻单用组的64.58%,与天麻单用组相比有显著差异(均P<0.05)。结论川芎可提高天麻苷元在大鼠脑内的生物利用度,减缓天麻苷元在大鼠脑内的消除速度。
AIM To establish an HPLC method for determination of gastrodigenin and investigate the influence of chuanxiong rhizoma on brain pharmacokinetics of gastrodigenin in rats. METHODS One hundred and forty-four rats were divided into gastrodiae rhizoma group （0.945 mg·kg-1 gastrodiae rhizoma extract by intragastric administration） and chuanxiong rhizoma combining gastrodiae rhizoma group （0.945 mg·kg-1 gastro- diae rhizoma extract and 3.78 mg·kg-1 chuanxiong rhizoma extract by intragastric administration）. Brain tissue was collected at different times after drug administration. The concentrations of gastrodigenin were determined by HPLC method. DAS2.0 software package was used to analyze the calculations of pharmacokinetic parameters. RESULTS The calibration curves of gastrodigenin were linear over the concentration range of 0.125 - 8 mg.L-~ （r = 0.999 6） in brain tissue. The absolute recoveries were 86.54% - 89.96%, and the RSDs of the intra-and inter-day precision were less than 5%. The area of gastrodigenin in the brain tissue under the drug concentration curve of the chuanxiong rhizoma combining gastrodiae rhizoma group was 1.66 times larger than the gastrodiae rhizoma group, and mean residence time was longer and the clearance was lower than the gastrodiae rhizoma group, which all had significantly differents （P 〈 0.01） . CONCLUSION Chuanxiong rhizoma improve the bioavailability of gastrodigenin in brain tissue of rats and reduce its elimination speed.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2012年第5期263-266,共4页
Chinese Journal of New Drugs and Clinical Remedies
基金
"中药新型给药系统技术平台"十一五重大新药创制项目(2009ZX09310-005)
江西省卫生厅中医药科研计划(2010A091)
关键词
川芎
天麻
天麻苷元
药动学
血脑屏障
生物利用度
chuanxiong rhizoma
gastrodiae rhizoma
gastrodigenin
pharmacokinetics
blood-brainbarrier
biological availability
