title: In Vivo Pharmacokinetics of Puerarin via Different Drug Administration Routes Based on Middle Cerebral Artery Occlusion Model.
abstract: OBJECTIVE
  Pueraria labata has traditionally been applied in the treatment of stroke in Chinese clinics. Puerarin is the key ingredient in it for brain protection effect. To find a superior administration route for puerarin in the treatment of ischemic cerebrovascular disease, the pharmacokinetics of puerarin based on the middle cerebral artery occlusion (MCAO) rat via different administration routes were studied and compared.
  
  
  METHODS
  Ten rats (MCAO model) divided into two groups were treated with puerarin via intravenous and intranasal routes. Samples of brain and plasma were collected by microdialysis and tested by high-performance liquid chromatography with tandem mass spectrometric detection (HPLC-MS/MS).
  
  
  RESULTS
  In olfactory bulb, the intranasal group got a higher Cmax, which was eight times higher than that of intravenous group. The AUC of puerarin were 255.96 ± 87.74 and 24.56 ± 15.50 min·μg/ml for intranasal and intravenous group, respectively. The intranasal group also got a longer T1/2compared with intravenous group. The drug target index (DTI) of intranasal group was up to 47.98%, which was highly improved, compared with intravenous group.
  
  
  CONCLUSIONS
  The in vivo experiments based on the MCAO model showed that, compared with intravenous route, the bioavailability and brain-targeting of drug were highly improved via intranasal route. In pathological conditions, compared with normal rats, the AUC of puerarin in brain and DTI increased significantly.
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Pengyue
authors.initials: P
authors.lastname: Li
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Bai
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Boyu
authors.initials: B
authors.lastname: Dong
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China. landocean28@163.com.
authors.forename: Yang
authors.initials: Y
authors.lastname: Lu
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Shengwei
authors.initials: S
authors.lastname: Zhang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Guo
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Tan
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Mengdi
authors.initials: M
authors.lastname: Zhao
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China. dsydulaoshi@126.com.
authors.forename: Shouying
authors.initials: S
authors.lastname: Du
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China.
authors.forename: Puning
authors.initials: P
authors.lastname: Cao
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D001682:Biological Availability; D001921:Brain / Q000378:metabolism*; D004195:Disease Models, Animal; D020244:Infarction, Middle Cerebral Artery / Q000188:drug therapy / Q000378:metabolism*; D007262:Infusions, Intravenous; D007529:Isoflavones / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D017551:Microdialysis; D017207:Rats, Sprague-Dawley; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D007529:Isoflavones; D014665:Vasodilator Agents; C033607:puerarin