The root of Astragalus membranaceus also known as
Huang Qi in China is a common traditional Chinese herb with extensive pharmacological activities.
Huangqi injection (HI), a common preparation of
Huang Qi, was wildly co-administered with
gliquidone to treat
diabetes mellitus and
diabetic nephropathy in clinic of China. The aim of the study was to investigate the effect of HI on the pharmacokinetics and hepatic uptake of
gliquidone and related mechanism to ensure the safety and efficacy of their usage. Normal rats (n = 5) and
streptozotocin (STZ)-induced diabetic rats (n = 5) were administered orally with 120 mg/kg
gliquidone alone or in combination with 8 ml/kg HI (i.v.), HI was given intravenously 5 min before that of
gliquidone. The plasma concentration of
gliquidone was determined by HPLC-fluorescence. In addition, hepatic uptake of
gliquidone with or without HI was evaluated in fresh primary rat hepatocytes. Co-administration of HI with
gliquidone could significantly increased the bioavailability of
gliquidone in normal and STZ-induced diabetic rats (n = 5); the concentration of
gliquidone in fresh primary rat hepatocytes was greatly decreased by HI. This study suggested that when HI and
gliquidone co-administering to normal and diabetic rats, the pharmacokinetics of
gliquidone was greatly changed, and these changes connect with HI inhibiting hepatic uptake of
gliquidone, and transportation of
gliquidone across liver mucosal membrane inhibited by HI would be the main mechanisms.