Pharmacokinetics of Arctigenin in Fructus Arctii Extract in Piglets

[Objectives]This study was conducted to investigate the pharmacokinetic characteristics of arctigenin from water extract of Fructus Arctii in piglets,understand its absorption,distribution,transformation and excretion in piglets,and provide theoretical reference for the development and clinical use of new veterinary drugs.[Methods]Six healthy piglets,weighing(30.0±5.0)kg,were selected and administered by gavage with a Fructus Arctii water extract at 1.0 g/kg·bw.Blood was collected from the anterior vena cava at different time points.The concentration of arctigenin in pig plasma was determined by HPLC.The main pharmacokinetic parameters were:absorption half-life(t1/2 ka)(0.098±0.006)h,distribution half-life(t1/2α)(0.208±0.009)h,elimination half-life(t1/2β)(23.816±2.151)h,apparent volume of distribution(Vd)(32.212±4.033)L/kg,apparent volume of distribution(Vd)(32.212±4.033)L/kg,clearance(CLb)(2.384±1.589)L/(h·kg),peak time(tmax)(0.251±0.011)h,peak concentration(Cmax)(0.560±0.063)μg/ml,and the area under the curve(AUC)at the time of drug administration(9.620±0.752)μg·h/ml.[Results]After oral administration of the water extract powder of Fructus Arctii,arctigenin showed a two-compartment model with absorption in piglets,with the characteristics of fast absorption,wide distribution and slow elimination.Arctigenin might have a hepatoenteral circulation in piglets,and the drug effect could last for a long time.[Conclusions]This study provides a theoretical basis and reference for the development and clinical use of new veterinary drugs.

Optimization of the processing technology of Fructus Arctii by response surface methodology

The present study was designed to optimize the processing of Fructus Arctii by response surface methodology （RSM）. Based on single factor studies, a three-variable, three-level Box-Behnken design （BBD） was used to monitor the effects of independent variables, including processing temperature and time, on the dependent variables. Response surfaces and contour plots of the contents of total lignans, chlorogenic acid, arctiin, and aretigenin were obtained through ultraviolet and visible （UV-Vis） monitoring and high performance liquid chromatography （HPLC）. Fructus Arctii should be processed under heating in a pot at 311℃, medicine at 119℃ for 123s with flipping frequently. The experimental values under the optimized processing technology were consistent with the predicted values. In conclusion, RSM is an effective method to optimize the processing of traditional Chinese medicine （TCM）.

Determination of Total Lignanoids in Tangjiangshenkang Granules by Two-Wavelength Ultraviolet Spectrophotometry

[Objectives] To establish a determination method for the content of total lignanoids in Tangjiangshenkang granules. [Methods] Two-wavelength ultraviolet spectrophotometry (TWBS) was used to scan arctiin control solution, chlorogenic acid control solution and Tangjiangshenkang granule test solution in the range of 200-400 nm. In the ultraviolet scanning diagram of arctiin reference solution, the maximum absorption wavelength of 280 nm was determined as the determination wavelength λ 1, the detection wavelength in the ultraviolet scanning diagram of chlorogenic acid reference solution ( λ 1=280 nm) was determined, and 350 nm was the reference wavelength λ 2;the content of total lignosides in Tangjiangshenkang granules was determined with arctiin as the reference substance. [Results] The precision, accuracy, and durability of this method were fine. The concentration of arctiin was linearly correlated with the absorbance difference in the range of 0.007 95-0.071 55 mg/mL ( r =0. 999 9). The average recovery of arctiin was 100.8%, and the RSD value was 1.04% ( n =6). Calculated as arctiin, three batches of Tangjiangshenkang granules contain no less than 20% of total lignosides. [Conclusions] The method has the advantages of simple operation, good accuracy, precision and reliable stability. It can be used as the content determination and quality control method of total lignosides in Tangjiangshenkang granules.