Effects of disodium cantharidinate on the pharmacokinetic behavior of capecitabine in rats
- VernacularTitle:斑蝥酸钠对卡培他滨在大鼠体内药动学行为的影响
- Author:
Kerong HU
1
;
Rui CHEN
2
;
Yujuan BAN
2
;
Jing HUANG
1
Author Information
1. School of Pharmacy，Guizhou Medical University，Guiyang 550004，China
2. Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D，Guiyang 550004，China
- Publication Type:Journal Article
- Keywords:
disodium cantharidinate;
capecitabine;
drug interaction;
UPLC-MS/MS
- From:
China Pharmacy
2023;34(18):2204-2207
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To study the effects of disodium cantharidinate on the pharmacokinetic behavior of capecitabine in rats. METHODS Rats were randomly divided into two control groups and two experimental groups with 6 rats in each group. Two control groups were intraperitoneally injected with normal saline， and two experimental groups were intraperitoneally injected with Disodium cantharidinate injection of 0.5 mL/kg， for 7 consecutive days. Eight days after medication， control group 1 and experimental group 1 were given capecitabine 5 mg/kg intragastrically， while control group 2 and experimental group 2 were given capecitabine 5 mg/kg intravenously. Blood samples were collected at different time points after administration. After extraction with ethyl acetate， the concentration of capecitabine in rat plasma was determined by UPLC-MS/MS method using tolbutamide as the internal standard. The pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS Compared with control group 1， MRT0－∞， cmax， AUC0－30 h， AUC0－∞ and F of experimental group 1 were increased significantly， while CLz/F was decreased significantly （P＜0.01）. Compared with control group 2， t1/2， MRT0－30 h， MRT0-∞， AUC0－30 h and AUC0－∞ of experimental group 2 were increased significantly （P＜0.01）. CONCLUSIONS Disodium cantharidinate can increase the plasma exposure of capecitabine in rats， improve its oral bioavailability， prolong the average residence time， and reduce its clearance rate.
