In Situ and in Vivo Study of Nasal Absorption of Paeonol in Rats

International Journal of Molecular Sciences

Xiaolan Chen¹  Yang Lu¹  Shouying Du¹  Bing Xu¹  Shan Wang¹  Yongsong Zhai¹  Xiao Song¹ 

[1] School of Chinese Materia Medica, Beijing University of Chinese Medicine, No.6, Zhonghuan South Road, Wangjing, Chaoyang district, Beijing 100102, China; E-Mails:

关键词: paeonol;    nasal absorption;    in situ;    single pass perfusion technique;    pharmacokinetics;   

DOI  :  10.3390/ijms11124882

来源: mdpi

【 摘 要 】

The objective of this work was to study the in situ and in vivo nasal absorption of paeonol. A novel single pass in situ nasal perfusion technique was applied to examine the rate and extent of nasal absorption of paeonol by rats. Various experimental conditions, such as perfusion rate, pH, osmotic pressure and drug concentration, were investigated. The in situ experiments showed that the nasal absorption of paeonol was not dependent on drug concentration, and fitted a first order process. The absorption rate constant, Ka, increased with an increase in perfusion speed. Paeonol was better absorbed in acidic solutions than in neutral or alkaline solutions. The value of Ka was higher in a hypertonic environment than under isotonic or hypotonic conditions. In vivo studies of paeonol absorption were carried out in rats and the pharmacokinetics parameters of intranasal (i.n.) and intragastric (i.g.) administration were compared with intravenous (i.v.) administration. The bioavailabilities of paeonol were 52.37% and 15.81% for i.n. and i.g, respectively, while T_max values were 3.05 ± 1.46 min and 6.30 ± 0.70 min. MRT (Mean Residence Time) were 23.19 ± 6.46 min, 41.49 ± 2.96 min and 23.09 ± 5.88 min for i.n., i.g. and i.v. methods, respectively. The results demonstrate that paeonol could be absorbed promptly and thoroughly by i.n. administration in rats.

【 授权许可】

CC BY   
© 2010 by the authors; licensee MDPI, Basel, Switzerland.