Investigation of pharmacokinetic characteristics of the 99mTc- and 188Re-labeled monopotassium salt of 1-hydroxyethylidenediphosphonic acid (KHEDP) in rats showed that the level of accumulated activity at 5 min and 1 and 3 h after i.v. injection of 188Re-KHEDP is higher in most organs and tissues than that after injection of 99mTc-KHEDP. In the subsequent period (6 and 24 h), the specific activities in the majority of soft organs and tissues equalized due to greater elimination of 188Re-KHEDP. The dynamics of labeled drug accumulation in bone tissues is characterized by a gradual increase in the activity concentration followed by its slow decrease. The maximum accumulation of 99mTc-KHEDP in bone was achieved within 3 – 6 h whereas the activity of 188Re-KHEDP was at a maximum 1 h after injection. The activity gradually decreases after reaching the maximum value. The rate of 99mTc-KHEDP elimination from bone is slower than that for 188Re-KHEDP. The ratios of the specific activity in organs and tissues upon i.v. injection of 99mTc-KHEDP and 188Re-KHEDP are illustrated more clearly by the coefficients of differential accumulation (CDA) of activity in bone (bone of femur, rib, skull, and spine) relative to soft organs and tissues. The dynamics of the change in these values is characterized by a gradual increase over 24 h after injection. The growth is more pronounced for 188Re-KHEDP than for 99mTc-KHEDP. These data show that the elimination of activity from bone upon injection of 188Re-KHEDP is faster than that for 99mTc-KHEDP. A comparative analysis of the CDA values allows the dynamics of drug accumulation and elimination rates from soft organs and tissues to be evaluated in comparison to bone. Using the CDA values, it is also possible to determine the optimum conditions for carrying out scintigraphy studies of the skeleton using a gamma camera. The results from the study of the pharmacokinetic characteristics of 99mTc-KHEDP and 188Re-KHEDP in rats showed that these complexes have similar structures and substantially different biological properties, as indicated by the substantial differences in their in vivo behavior upon i.v. injection.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 45, No. 6, pp. 14 – 21, June, 2011.
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Shiryaeva, V.K., Petriev, V.M., Bryukhanova, A.A. et al. Comparative analysis of pharmacokinetic characteristics of radiopharmaceuticals based on the monopotassium salt of 1-hydroxyethylidenediphosphonic acid labeled by 99mT9c and 188Re. Pharm Chem J 45, 333–340 (2011). https://doi.org/10.1007/s11094-011-0628-5
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DOI: https://doi.org/10.1007/s11094-011-0628-5