Preparation of ~(99)Tc~m-ASON-EGF and its pharmacokinetic features in rabbits
- VernacularTitle:~(99)Tc~m-ASON-EGF的制备及其药代动力学研究
- Author:
Jiajun HUANG
;
Mengjie DONG
;
Juan XIE
;
Shaoli LI
- Publication Type:Journal Article
- Keywords:
pharmacokinetics;
~(99)Tc~m;
epidermal growth factor;
antisense oligonucleotide
- From:Journal of Third Military Medical University
2003;0(23):-
- CountryChina
- Language:Chinese
-
Abstract:
Objective To prepare and explore the pharmacokinetic parameters for ~ 99 Tc~ m -ASON-EGF in healthy rabbits. Methods ~ 99 Tc~ m -ASON-EGF was prepared according to previous methods and its changes of concentration in blood were measured by radioactivity counts per minute. The experimental data were dealt with by 3p97 software and its true compartment model was estimated by AIC value, R~ 2 value, the 1/c and F test. Subsequently, its half-life of distribution (T_ 1/2 ?), half-life of elimination (T_ 1/2 ?), central compartment volume of distribution (Vc), total apparent volume of distribution (Vd) and total rate of clearance (CL) were calculated by the software. Finally, the binding rate of plasma protein was determined by trichloroacetic acid precipitation. Results The best model of ~ 99 Tc~ m -ASON-EGF in vivo was two-compartment model and its T_ 1/2 ?, T_ 1/2 ?, Vc, Vd and CL were 5.28 min, 89.23 min, 67.8 ml, 915.6 ml and 7.1 ml/min respectively. After being incubated with fresh plasma for 1.5 h, its binding rate was 10.69%. Conclusion Its process of transportation in healthy rabbits is fitted to two-compartment model and the pharmacokinetic properties are desirable.
