Pharmacokinetics of BMEDA after Intravenous Administration in Beagle Dogs

Molecules

Chih-Hsien Chang¹  Si-Yen Liu¹ 

[1] Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan; E-Mails:

关键词: acute toxicity;    radiopharmaceutical;    BMEDA;    ¹⁸⁸Re-BMEDA-liposome;    pharmacokinetics;   

DOI  :  10.3390/molecules19010538

来源: mdpi

【 摘 要 】

The pharmacokinetics of N,N-bis(2-mercapatoethly)-N',N'-diethylenediamine (BMEDA), a molecule that can form a chelate with rhenium-188 (¹⁸⁸Re) to produce the ¹⁸⁸Re-BMEDA-liposomes, was studied. In this work, beagles received a single injection of BMEDA, at doses of 1, 2, or 5 mg/kg; the concentration of BMEDA in the beagles’ plasma was then analyzed and determined by liquid chromatography-mass spectrometry/mass spectrometry. Based on the pharmacokinetic parameters of BMEDA, we found that male and female animals shared similar patterns indicating that the pharmacokinetics of BMEDA is independent of gender differences. In addition, the pharmacokinetics of BMEDA was seen to be non-linear because the increase of mean AUC_0–t and AUC_0–∞ values tend to be greater than dose proportional while the mean Vss and CL values of BMEDA appeared to be dose dependent. The information on the pharmacokinetics of BMEDA generated from this study will serve as a basis to design appropriate pharmacology and toxicology studies for future human use.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.