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Xenobiotica
the fate of foreign compounds in biological systems
Volume 49, 2019 - Issue 10
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Animal Pharmacokinetics and Metabolism

Effects of astragaloside IV on the pharmacokinetics of puerarin in rats

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Pages 1173-1177 | Received 09 Apr 2018, Accepted 22 May 2018, Published online: 14 Jun 2019
 

Abstract

  1. Radix astragali and puerarin are always used together for cardiovascular disease in China clinics.

  2. This study investigates the effects of astragaloside IV (AS-IV, the main components of radix astragali) on the pharmacokinetics of puerarin in rats.

  3. The pharmacokinetics of orally administered puerarin (50 mg/kg) with or without AS-IV pretreatment (100 mg/kg/day for seven days) were investigated. The plasma concentration of puerarin was determined using LC–MS/MS method, and the pharmacokinetics profiles were calculated and compared. Caco-2 cell transwell model was also used to investigate the effects of AS-IV on the transport pf puerarin.

  4. The results showed that when the rats were pretreated with AS-IV, the maximum concentration (Cmax) of puerarin decreased from 760 to 467 ng/mL (p < .05, n = 6, 90% CI, 293 ± 61.28), and the area under the concentration-time curve from zero to infinity (AUC0–inf) also decreased from 4097 to 2330 μg·h/L (p < .05, n = 6). The oral clearance of puerarin increased significantly from 11.9 to 22.4 L/h/kg (p < .05, n = 6). The Caco-2 cell transwell experiments indicated that AS-IV could increase the efflux ratio of puerarin from 1.81 to 2.79 through inducing the activity of P-gp.

  5. In conclusion, these results indicated that AS-IV could affect the pharmacokinetics of puerarin, possibly by decreasing the systemic exposure of puerarin by inducing the activity of P-gp.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was funded by Talent-development Project of Pudong Health and Family Planning Commission of Shanghai (PWRd 2014-16), and Shanghai Municipal Commission of Health and Family Planning [201540126].

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