Pharmacokinetic study on dry powder inhalation administration of α-asarone in rats.
- Author:
Yu-yi QIAN
;
Jin LU
;
Liu-hong ZHANG
;
Fei-yan SHI
;
Ting-ming FU
;
Li-wei GUO
- Publication Type:Journal Article
- MeSH:
Administration, Inhalation;
Animals;
Anisoles;
administration & dosage;
blood;
pharmacokinetics;
Biological Availability;
Drugs, Chinese Herbal;
administration & dosage;
analysis;
pharmacokinetics;
Half-Life;
Male;
Rats;
Rats, Sprague-Dawley
- From:
China Journal of Chinese Materia Medica
2015;40(4):739-743
- CountryChina
- Language:Chinese
-
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.