An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging

J Labelled Comp Radiopharm. 2016 Apr;59(4):157-63. doi: 10.1002/jlcr.3384. Epub 2016 Mar 9.

Abstract

This study aimed to provide an easy method for synthesis of 1-hydroxy-2-(3-pyridyl) ethylidene bisphosphonic acid monosodium (sod. risedronate) with a high yield of 71%. The synthesized risedronate was labeled with technetium-99 m using two different reducing agents (SnCl2 .2H2 O and NaBH4 ) where NaBH4 gave stable complex and higher radiochemical yield more than SnCl2 .2H2 O. The results showed that, the radiochemical purity of (99m) Tc(NaBH4 )-risedronate was 99.2 ± 0.6% and its stability was up to 6 h. Biodistribution study showed high uptake and long retention of (99m) Tc(NaBH4 )-risedronate in bone starting from 15 min (29 ± 2.5% ID/organ) up to 4 h (35.1 ± 3.2 ID/organ) post injection. This research could introduce an easy and effective method for synthesis and labeling of risedrionate and affording a good tracer for bone imaging.

Keywords: 99mTc; Bisphosphonate; Bone; Imaging; Risedronate; Synthesis.

MeSH terms

  • Animals
  • Bone and Bones / diagnostic imaging*
  • Borohydrides / chemistry
  • Chemistry Techniques, Synthetic
  • Drug Stability
  • Isotope Labeling
  • Kinetics
  • Mice
  • Molecular Imaging / methods*
  • Radiochemistry
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics
  • Reducing Agents / chemistry
  • Risedronic Acid / chemical synthesis*
  • Risedronic Acid / chemistry
  • Risedronic Acid / pharmacokinetics
  • Technetium / chemistry
  • Tin Compounds / chemistry
  • Tissue Distribution

Substances

  • Borohydrides
  • Radiopharmaceuticals
  • Reducing Agents
  • Tin Compounds
  • stannous chloride
  • Technetium
  • sodium borohydride
  • Risedronic Acid