title: Comparative study of pharmacokinetics and tissue distribution of osthole in rats after oral administration of pure osthole and Libanotis buchtormensis supercritical extract.
abstract: BACKGROUND
  Libanotis buchtormensis is the source of an important traditional medicine from Shaanxi province of China used in the treatment of many illnesses. Libanotis buchtormensis supercritical extract (LBSE) has analgesic, sedative and anti-inflammatory qualities. Osthole is one of the major bioactive components of LBSE; it is known for its significant anti-tumor, analgesic, and anti-inflammatory properties, it also alleviates hyperglycemia.
  
  
  OBJECTIVE
  The purpose of the present study was to compare the pharmacokinetics and tissue distribution of osthole in Sprague-Dawley (SD) rats after oral administration of pure osthole and LBSE. The two preparations were administered at the same osthole dose (approximately 130 mg/kg). The results should provide some guidance for the clinical applications of Libanotis buchtormensis.
  
  
  METHODS
  Comparative pharmacokinetics and tissue distribution of osthole in SD rats after oral administration of pure osthole and LBSE were analyzed using reversed-phase high-performance liquid chromatography (RP-HPLC). All pharmacokinetic data were analyzed using 3P97 software. Samples of blood and internal organs (heart, liver, spleen, lungs and kidney) were collected and pretreated according to the experimental schedule. After pretreatment, plasma and tissue samples were extracted using ether-ethyl acetate mixture (3:1, v/v). The concentration of osthole in the plasma and tissues were determined using the RP-HPLC method.
  
  
  RESULTS
  The procedure described in this paper shows good precision and stability and is suitable for the osthole assays in biological samples. We found that the average plasma concentration-time profile of osthole after oral administration of osthole and LBSE showed a single peak. There were also clear differences between plasma concentrations of osthole after oral administration of pure osthole and LBSE. Non-osthole ingredients in LBSE showed some pharmacokinetic interactions with osthole and hence decreased its absorption levels (p<0.05). Our results show different tissue distribution of osthole in the single and composite administration regimens.
  
  
  CONCLUSIONS
  This study compares the pharmacokinetic characteristics and tissue distribution of osthole in rats after oral administration of pure osthole and LBSE; the results might be useful in clinical application of this traditional Chinese herbal medicine.
authors.affiliation: Faculty of Pharmacy, School of Medicine, Xi'an Jiaotong University, Xi'an 710061, China.
authors.forename: Juan
authors.initials: J
authors.lastname: Shi
authors.forename: Qiang
authors.initials: Q
authors.lastname: Fu
authors.forename: Wang
authors.initials: W
authors.lastname: Chen
authors.forename: Hai-Ping
authors.initials: HP
authors.lastname: Yang
authors.forename: Jing
authors.initials: J
authors.lastname: Liu
authors.forename: Xiao-Meng
authors.initials: XM
authors.lastname: Wang
authors.forename: Xu
authors.initials: X
authors.lastname: He
mesh_terms: D000284:Administration, Oral; D000700:Analgesics / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D019661:Apiaceae / Q000737:chemistry*; D003374:Coumarins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D008297:Male; D010936:Plant Extracts / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
chemical_list: D000700:Analgesics; D003374:Coumarins; D010936:Plant Extracts; C046627:osthol