title: [Pharmacokinetic study on dry powder inhalation administration of α-asarone in rats].
abstract: To study the pharmacokinetic characteristics and absolute bioavailability of α-asarone through dry powder inhalation in rats, and compare with that through oral administration and intravenous injection. A HPLC method was established for the determination of α-asarone in rat plasma to detect the changes in plasma concentrations of α-asarone through dry powder inhalation (20 mg · kg(-1)), oral administration (80 mg · kg(-1)) and intravenous injection (20 mg · kg(-1)) in rats. DAS 2.0 software was used to calculate the pharmacokinetic parameters. The absolute bioavailability of α-asarone was calculated according to AUC(0-t)) of administration routes and administration doses. According to the results, α-asarone showed good linear relations (r = 0. 999 4) at concentrations between 0.282-14.1 mg · L(-1), with the limit of detection (LOD) at 0.212 mg · L(-1). Through dry powder inhalation, oral administration and intravenous injection of α-asarone, the metabolic processes of α-asarone in rats conformed to one, two and three compartment models respectively, with the elimination half-life of (95.48 ± 48.28), (64.34 ± 27.59), (66.99 ± 29.76) min. According to the bioavailability formula, the absolute bioavailability of α-asarone through dry powder inhalation and oral administration were 78.32% and 33. 60%, respectively. This study showed that significant increase in elimination half-life and absolute bioavailability of α-asarone through dry powder inhalation, which lays a theoretical foundation for preparing α-asarone dry powder inhalers.
authors.forename: Yu-yi
authors.initials: YY
authors.lastname: Qian
authors.forename: Jin
authors.initials: J
authors.lastname: Lu
authors.forename: Liu-hong
authors.initials: LH
authors.lastname: Zhang
authors.forename: Fei-yan
authors.initials: FY
authors.lastname: Shi
authors.forename: Ting-ming
authors.initials: TM
authors.lastname: Fu
authors.forename: Li-wei
authors.initials: LW
authors.lastname: Guo
mesh_terms: D000280:Administration, Inhalation; D000081248:Allylbenzene Derivatives; D000818:Animals; D000840:Anisoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics*; D006207:Half-Life; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000081248:Allylbenzene Derivatives; D000840:Anisoles; D004365:Drugs, Chinese Herbal; C012195:asarone