Pharmacokinetics of Purine Benzamides PLB-E and PLB-P in Rats
10.13748/j.cnki.issn1007-7693.20224269
- VernacularTitle:嘌呤苯酰胺类化合物PLB-E和PLB-P在大鼠体内的药动学研究
- Author:
Xinru WANG
1
;
Xi MAI
1
;
Zhiwang ZHOU
1
;
Lina HONG
1
;
Lihua FENG
1
Author Information
1. Department of Pharmacy, Nanchang University, Nanchang 330006, China
- Publication Type:Journal Article
- Keywords:
purine benzamides ； PLB-E；PLB-P；HPLC；plasma concentration；pharmacokinetics
- From:
Chinese Journal of Modern Applied Pharmacy
2024;41(12):1615-1620
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE :To establish a method for the determination of the concentrations of anti-tumor lead compounds purine benzamides PLB-E and PLB-P in rat plasma by HPLC and apply to study pharmacokinetics.
METHODS
The established HPLC was used to determine the plasma drug concentrations of rats at different time points after intravenous administration of 5, 10, 20 mg·kg–1 (low, medium, high doses) of PLB-E and PLB-P, and the pharmacokinetic parameters of each compound were calculated using DAS 3.3.0 software.
RESULTS
PLB-E and PLB-P had good linear relationship in the range of 2–120, 3–60 μg·mL–1, respectively(r2>0.999). The RSD of inter-day and intra-day precision were <15%. The extraction recoveries were 87.48%–92.84% and 88.24%–92.60%, respectively. The main pharmacokinetic parameters of PLB-E and PLB-P after a single intravenous injection of 5, 10, 20 mg·kg–1 were as follows, the average Cmax was (20.30±2.39), (40.63±3.40), (63.62±7.55)mg·L–1 and (13.21±1.40), (24.87±1.33), (32.83±0.65)mg·L–1, respectively. AUC(0-∞) were (104.67±48.39), (177.42±84.11), (194.32±91.48)mg·h·L–1 and (106.75±54.21), (179.90±93.59), (253.56±126.17)mg·h·L–1, respectively. Tmax of each dose was 0.08 h.
CONCLUSION
The HPLC method established in this study meets the requirements for the determination of biological samples through methodological verification, which is applicable to the determination of the concentration of PLB-E and PLB-P in rat plasma and the pharmacokinetic study. The pharmacokinetic process of PLB-E and PLB-P in rats conforms to the two-compartment model, and conforms to the nonlinear kinetic elimination.
