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PubMed1980

Preparation and biological distribution of technetium diphosphonate radiotracers synthesized without stannous ion.

Two HEDP complexes of technetium (either Tc-99 or a mixture of Tc-99 and Tc-99m) have been prepared without the use of stannous ion. The first, Tc(NaBH4)-HEDP, is synthesized by reduction of TcO4- with NaBH4 in the presence of excess HEDP; this is analogous to the preparation of Tc(Sn)-HEDP in commercial kits wherein SN(II) functions as the reductant. The second, Tc-HEDP, is prepared by substitution of HEDP onto the pre-formed, pre-reduced, technetium center TcBr62-. The HEDP-to-Tc ratio in Tc-HEDP was found to be 1.0 by double-labeling procedures (Tc-99 and [3H]HEDP), implying that in solution this material is polymeric or at least dimeric. Preparations of Tc(NaBH4)-HEDP and Tc-HEDP with Tc-99m are excellent bone-imaging agents in both rats and dogs. Tissue distribution studies in rats show that uptake of Tc(NaBH4)-HEDP and Tc-HEDP by the bone is at least equivalent to that achieved by Tc(Sn)-HEDP prepared in commercial kits with Sn(II) as the reductant. Tin is therefore not necessary for the bone-seeking properties of Tc(Sn)-HEDP, and the in vivo distribution of a given HEDP radiotracer seems to depend primarily on the presence of the HEDP ligand and not on the exact nature of the technetium complex itself. Synthesis of technetium radiotracers by a substitution route, rather than by redox, is practicable; this route has the potential of introducing hitherto unattainable flexibility and subtlety into the preparation of technetium radiotracers.

Etidronic Acid↗
PubMed1982

[Treatment of Paget's disease with 1-ethane-1-hydroxy-1-diphosphonate].

The authors treated 11 patients suffering from severe and/or quickly developing Paget's disease (3 of whom had leontiasis ossea), using etidronate (E.H.D.P.) at doses of 7 to 15 mg.kg/day for a period of 6 months. The patients were followed up for 18 months, on average. The following were the conclusions of the investigation: E.H.D.P. is an effective treatment of Paget's disease: the decrease in hydroxyprolinuria was greater and more durable than that of the alcalin phosphatases; a variation between these two values even seems to appear under treatment. However, although some patients responded very well to the treatment, others were less responsive; at the dosages used, E.H.D.P. reduced the scanning hyperfixation of the active pagetic areas in 6 patients: it likewise more or less markedly reduced hyperosteoclastosis, with no apparent increase in the osteoid volume; two patients suffering from upper maxillary disease regressed clinically (dentures had become too large); headache and hypacusia were not modified; the response to the treatment seems to depend on three factors: the activity of the patient, the dosage used, and an individual factor which may be linked to the severity of the osteoidosis.

Aged↗