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The Pharmacokinetics of Technetium-99m-Labeled N,N,N′,N′-Ethylenediaminetetra-Kis-(Methylenephosphonic Acid) in Intact Rats

  • MOLECULAR BIOLOGY PROBLEMS OF DRUG DESIGN AND MECHANISM OF DRUG ACTION
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Pharmaceutical Chemistry Journal Aims and scope

Pharmacokinetic studies of technetium-99m-labeled N,N,N′,N′-ethylenediaminetetra-kis-(methylenephosphonic acid) (99mTc-EDTMP) showed that this radiopharmaceutical (RP) has high in vivo stability. Studies of the biodistribution of 99mTc-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 99mTc-EDTMP content in the skeleton was 4.7 – 24.3 times greater than that of sodium pertechnetate (Na99mTcO4) (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 Na99mTcO4 in in virtually all organs and tissues. These results indicate that 99mTc-EDTMP can be regarded as a potential RP for diagnostic investigations of bone tissues.

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Authors and Affiliations

  1. A. F. Tsyb Medical Radiology Center, P. A. Gertsen Federal Medical Research Center, Ministry of Health of the Russian Federation, Obninsk, Kaluga Region, Russia

    V. M. Petriev, V. K. Tishchenko, K. V. Koptyaeva, O. A. Smoryzanova & V. G. Skvortsov

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  1. V. M. Petriev
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  2. V. K. Tishchenko
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  3. K. V. Koptyaeva
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  4. O. A. Smoryzanova
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  5. V. G. Skvortsov
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 49, No. 5, pp. 3 – 7, May, 2015.

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Petriev, V.M., Tishchenko, V.K., Koptyaeva, K.V. et al. The Pharmacokinetics of Technetium-99m-Labeled N,N,N′,N′-Ethylenediaminetetra-Kis-(Methylenephosphonic Acid) in Intact Rats. Pharm Chem J 49, 287–291 (2015). https://doi.org/10.1007/s11094-015-1271-3

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  • DOI: https://doi.org/10.1007/s11094-015-1271-3

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