Pharmacokinetics, Tissue Distribution and Excretion of Isoalantolactone and Alantolactone in Rats after Oral Administration of Radix Inulae Extract

Molecules

Renjie Xu²  Guisheng Zhou²  Ying Peng²  Mengyue Wang²  Xiaobo Li¹ 

[1] School of Pharmacy, Shanghai Jiao Tong University, No.800 Dongchuan Road, Minhang District, Shanghai 200240, China;

关键词: Radix Inulae;    isoalantolactone;    alantolactone;    pharmacokinetics;    tissue distribution;    excretion;   

DOI  :  10.3390/molecules20057719

来源: mdpi

【 摘 要 】

Radix Inulae is endemic to China and has been used in traditional medicine to treat upper body pain, emesis and diarrhoea, and to eliminate parasites. Here, an UPLC-MS/MS method was developed and applied to study the pharmacokinetics, distribution and excretion of isoalantolactone and alantolactone, which are two main active sesquiterpene lactones in Radix Inulae, in Sprague-Dawley rats following oral administration of total Radix Inulae extract. Isoalantolactone, alantolactone and osthole (internal standard) were prepared using acetonitrile precipitation, and the separation of isoalantolactone and alantolactone was achieved by isocratic elution using water (containing 0.1% formic acid) and acetonitrile as the mobile phase using a ZORBAX Eclipse Plus C₁₈ column. The total run time was 6.4 min. The present study showed poor absorption of isoalantolactone and alantolactone in vivo. The apparent C_max, T_max, T_1/2 and total exposure (AUC_0–12h) in rat plasma were 37.8 ng/mL, 120 min, 351.7 min and 6112.3 ng-min/mL for isoalantolactone and 25.9 ng/mL, 90 min, 321.0 min and 4918.9 ng-min/mL for alantolactone, respectively. It was shown that the highest concentration was achieved in the small intestine and feces clearance was shown to be the dominant elimination pathway of the lactones.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.