[Comparison of the distribution of breviscapine in the brain by different administration routes].
By comparing the drug distribution of breviscapine administered intranasally, orally and intrgvenous injected in rats' brain. After 0.4 mg x kg(-1) breviscapine was given by tail vein, intranasal and gastric perfusion administration to SD rats, cerebrospinal fluid was obtained by erebellomedllery cisternal puncture at different times. 125I labeling was used to determine the drug content of cerebrospinal fluid, cerebrum, cerebellum, medulla oblongata, olfactory region, olfactory bulb and blood in rats. AUCs were calculated by trapezoidal rule. The results showed that AUCs(0-240 min) (microg x min x g(-1)) of brain tissues were 11.686 +/- 1.919, 5.676 +/- 1.025, 7.989 +/- 0.925, 7.956 +/- 1.159, 17.465 +/- 2.136, 24.2 +/- 2.906 and 78.51 +/- 12.05, respectively, in the intranasal administration group; while those in the tail vein administration groups were 6.79 +/- 0.661, 6.251 +/- 0.40, 10.805 +/- 1.161, 9.146 +/- 1.04, 9.892 +/- 1.532, 7.871 +/- 0.842 and 173.91 +/- 10.02; and oral administration group were 0.868 +/- 0.167, 1.708 +/- 0.266, 2.867 +/- 0.725, 2.067 +/- 0.313, 1.361 +/- 0.308, 1.206 +/- 0.255 and 45.2 +/- 7.52, respectively. AUCs(0-240 min) of the brain tissues after oral, tail vein and intranasal administration were 22.29%, 29.18%, 95.49% of that of blood, respectively, it means that the absorption rate and drug distribution in the brain tissues after intranasal administration were higher than those of oral and tail vein administration. It is worth to investigate further the pharmacodynamic relationship.
Shi
Sen-lin
SL
Department of Pharmaceutics, Zhejiang Chinese Medical University, Hangzhou 310053, China. pjstone@163.com
Xu
Lian-ying
LY
Wu
Jin-jin
JJ
Li
Chang-yu
CY
Ge
Wei-hong
WH
Dai
Wen-yun
WY
D000281:Administration, Intranasal; D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D054022:Cerebrum / Q000378:metabolism; D016503:Drug Delivery Systems; D049919:Erigeron / Q000737:chemistry; D005419:Flavonoids / Q000008:administration & dosage / Q000097:blood / Q000134:cerebrospinal fluid / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D008297:Male; D008526:Medulla Oblongata / Q000378:metabolism; D009830:Olfactory Bulb / Q000378:metabolism; D009833:Olfactory Pathways / Q000378:metabolism; D010946:Plants, Medicinal / Q000737:chemistry; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D005419:Flavonoids; C061097:breviscapine