Pharmacokinetics of fospropofol disodium and its active metabolites in pregnant rats
10.13699/j.cnki.1001-6821.2024.23.015
- VernacularTitle:磷丙泊酚二钠及其活性代谢产物在妊娠大鼠体内的药代动力学研究
- Author:
Meng-yuan WANG
1
;
Wen-hao CHU
1
;
Wen-li LI
1
;
Tian-tian ZHANG
1
;
Wei CHEN
1
;
Ye YUAN
1
;
Zhi-qing ZHANG
1
Author Information
1. 河北医科大学第二医院药学部,河北石家庄 050000
- Publication Type:Journal Article
- Keywords:
fospropofol disodium;
propofol;
liquid chromatography tandem mass spectrometry;
pharmacokinetics;
pregnant rats
- From:
The Chinese Journal of Clinical Pharmacology
2024;40(23):3439-3443
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the pharmacokinetics of fospropofol disodium and its active metabolite propofol in pregnant rats.Methods A liquid chromatography tandem mass spectrometry(LC-MS/MS)method for simultaneous determination of fospropofol disodium and propofol in plasma of SD rats was establish and investigated methodologically.Pregnant SD rats were given 120 mg·kg-1 fospropofol disodium intravenously,and blood was taken from the inner canthus before administration and 3,6,10,15,30,45,60,90,120,150min after administration.Plasma drug concentration was determined by LC-MS/MS method,and pharmacokinetic parameters of fospropofol disodium and propofol were calculated by DAS software.Results The standard curve equations of fospropofol disodium and propofol were y=0.77x+0.08(r=0.997 2)and y=8.90 × 10-3x+4.70 × 10-3(r=0.997 1),and the linear ranges were 0.2-250.0 μg·mL-1 and 1.0-80.0 μg·mL-1.After intravenous administration of fospropofol disodium,the tmax of propofol was(9.50±3.33)min,theCmaxof fospropofol disodium and propofol were(349.50±154.10)and(28.33±15.30)μg·mL-1,t1/2 was(24.35±11.33)and(43.87±4.86)min,and AUC0→t were(79.40±21.53)and(25.13±15.71)μg·mL-1·h.Conclusion The LC-MS/MS method established in this study can simultaneously determine the concentration of fospropofol disodium and propofol in plasma of rats,and fospropofol disodium can also be quickly converted into active metabolite propofol after intravenous administration to pregnant rats.
