In Vivo Pharmacokinetics of Puerarin via Different Drug Administration Routes Based on Middle Cerebral Artery Occlusion Model.

BACKGROUND AND OBJECTIVES: Pueraria labata has traditionally been applied in the treatment of stroke in Chinese clinics. Puerarin is the key ingredient in it for brain protection effect. To find a superior administration route for puerarin in the treatment of ischemic cerebrovascular disease, the pharmacokinetics of puerarin based on the middle cerebral artery occlusion (MCAO) rat via different administration routes were studied and compared.

METHODS: Ten rats (MCAO model) divided into two groups were treated with puerarin via intravenous and intranasal routes. Samples of brain and plasma were collected by microdialysis and tested by high-performance liquid chromatography with tandem mass spectrometric detection (HPLC-MS/MS).

RESULTS: In olfactory bulb, the intranasal group got a higher C max , which was eight times higher than that of intravenous group. The AUC of puerarin were 255.96 ± 87.74 and 24.56 ± 15.50 min·μg/ml for intranasal and intravenous group, respectively. The intranasal group also got a longer T 1/2 compared with intravenous group. The drug target index (DTI) of intranasal group was up to 47.98%, which was highly improved, compared with intravenous group.

CONCLUSIONS: The in vivo experiments based on the MCAO model showed that, compared with intravenous route, the bioavailability and brain-targeting of drug were highly improved via intranasal route. In pathological conditions, compared with normal rats, the AUC of puerarin in brain and DTI increased significantly.