Pharmacokinetics and Brain-targeting Ability of Gastrodin Nasal in Situ Gel in Rats / 中国药师

ABSTRACT

Objective:To study the pharmacokinetic parameters of gastrodin nasal in situ gel ( ISG) with the base of TMC-P407-P188-carbomer, and evaluate its brain-targeting ability preliminarily. Methods:Rats were used as the model animals. The experiment group was treated with gastrodin nasal in situ gel, and the control group was treated with gastrodin solution with intravenous administra-tion. The plasma sample and brain tissue ( cerebrum and cerebellum) were taken out at the predetermined time points, and the concen-tration of gastrodin in plasma and gastrodigenin in brain tissues were determined by HPLC to draw the curve of concentration vs time. The pharmacokinetic parameters such as MRT and AUC were calculated by 3P97 software. The bioavailability F (%) and the brain-targeting index BTI were compared between the groups. Results:The concentration of gastrodigenin in the brain tissues of grastrodin in situ gel was higher than that of gastrodin solution with intravenous administration (P<0. 05). AUC of cerebrum and cerebellum both increased significantly with BTI of 2. 38 and 1. 93, respectively. MRT increased by nearly two-fold in the gel group when compared with that in the control group, and F(%) increased significantly in cerebrum and cerebellum as well. Conclusion:Gastrodin nasal in situ gel with the base of TMC-P407-P188-carbomer has promising effectiveness. Meanwhile, it can improve the brain-targeting ability of gastrodin with sustained release.