Evaluation on Medication Route of Puerarin by Plasma Concentration- Time Cur ve and Histodistribution Characteristics in Mice / 中药新药与临床药理

ABSTRACT

Objective The rational medication route of puerarin was explore d by studying the concentration- time curve and by comparing the histological and organic distribution difference of puerarin administered by intravenous injecti on or gastric gavage in mice, so as to supply a referential data for its rationa l application. Methods The NIH mice were used as experimental subject. The pu erarin concentrations in the plasma, tissue and organs at different time points were determined by HPLC. The PK solutions 2.0 program, a noncompartmental model software, was applied to calculate the pharmacokinetic parameters of puerarin an d to construct its plasma concentration- time curve. Results (1)The pharmacok inetic parameters of puerarin in mice were shown that the T1/2E of puerarin susp ension (0.2 mg? g- 1) by oral administration is 38.061min, CL =991.534 mL? mi n- 1, Cmax =3.6? g? mL- 1, Tmax =30 min, and AUC(0- ∞ ) =201.7? g? min? mL- 1, the bioavailability of puerarin suspension is 3.77 % compared to i.v puerarin injection. (2) Administered by intravenous injection (i.v), the puerari n distributed in the liver, kidney, plasma, spleen, muscle, lung, uterus and tes ticle rapidly, and the concentration of puerarin was the highest in the liver an d kidney and lower in the heart and brain. Distribution of puerarin suspension b y oral administration is similar to puerarin injection by i.v. However, the conc entration of puerarin in the tissues and organs by oral administration was lower than by i.v; the liver/heart, liver/brain, kidney/heart and kidney/brain concen tration ratios of puerarin by gavage administration were lower than those by i.v . Conclusion The bioavailability of puerarin by oral administration was poor, but the histological distribution characteristics of puerarin shows that the tox ic and side effects of puerarin are lesser by oral use than by intravenous injec tion.