Pharmacokinetic studies of technetium-99m-labeled N,N,N¢,N¢-ethylenediaminetetra-kis-(methylenephosphonic acid) ( 99m Tc-EDTMP) showed that this radiopharmaceutical (RP) has high in vivo stability. Studies of the biodistribution of 99m Tc-EDTMP were performed in healthy rats. Labeled agent was found to accumulate mainly in bone tissue. The greatest activity in the skeleton, (1.93 ± 0.12)%/g, was seen 1 h after i.v. administration. Accumulation of 99m Tc-EDTMP content in the skeleton was 4.7 -24.3 times greater than that of sodium pertechnetate (Na 99m TcO 4 ) (p < 0.001). Numerical values for differential accumulation coefficients (DAC) for activity in bones and internal organs and tissues were found to increase gradually to maximum values 3 h after i.v. administration. RP was eliminated mainly via the urinary tract. Study agent was rapidly cleared from the blood and only minor quantities accumulated in the internal organs. Contents were lower than those of Na 99m TcO 4 in in virtually all organs and tissues. These results indicate that 99m Tc-EDTMP can be regarded as a potential RP for diagnostic investigations of bone tissues.The main method for diagnosis of metastatic lesions in bone tissue is bone scintigraphy using 99m Tc-labeled phosphonic acids. 99m Tc has an optimum decay halflife (6 h) and gamma quantum energy (140 keV). These agents have affinity for hydroxyapatite in the bone matrix and show selective accumulation in zones with increased mineralization requirements, predominantly metastatic and inflammatory-destructive foci [1 -11]. At the same time, the need for osteoscintigraphy with maximal sensitivity and specificity is driving an intense search for new radiopharmaceuticals (RP) based on phosphonic acids.Among the polyaminophosphonic acids, there is great interest in N,N,N¢,N¢-ethylenediaminetetra-kis-(methylenephosphonic acid) (EDTMP). This is used as the basis of the agent 153 Sn-EDTMP (Lexidronam), which has undergone clinical trials and is used in clinical practice.Analysis of published data indicates that 99m Tc-EDTMP has tropism for bony tissue, though systematic studies in this area remain to be performed [12,13].We have therefore conducted detailed studies of the pharmacokinetic properties of 99m Tc-EDTMP in intact laboratory animals.
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