title: Practicality of production of ³²P by direct neutron activation for its utilization in bone pain palliation as Na₃[³²P]PO₄.
abstract: Large-scale production of ³²P for its clinical use in palliative care of painful bone metastasis in the form of Na3[³²P]PO₄ (³²P-sodium orthophosphate) has been practiced for six decades. The classical route of production of ³²P by (n,p) reaction on high purity elemental sulfur yields no-carrier-added (NCA) ³²P. Since high specific activity ³²P is not essential for the formulation of Na₃[³²P]PO₄ for bone pain palliation, an alternate route of production of ³²P by direct neutron capture using elemental phosphorus target [(31)P(n,γ)³²P] was envisaged and its suitability for use in bone pain palliation was evaluated. Toward this, irradiation of elemental red phosphorus target was carried out at a neutron flux of 8×10¹³ n/cm².s for 60 days and this yielded ³²P with a specific activity of 230±15 MBq/mg (6.2±0.4 mCi/mg) having >99.9% radionuclidic purity. About 370-555 MBq (10-15 mCi) doses of Na₃[³²P]PO₄ were formulated in sterile saline (pH 7.4) using the ³²P produced. The radiochemical purity of the formulation was found to be ~99% with respect to PO₄³⁻. The formulation exhibited good in vitro stability in saline and in human serum. Biodistribution studies carried out in normal Wistar rats revealed comparable pharmacokinetic properties of the formulation prepared using (n,γ) produced ³²P with that of NCA ³²P produced by (n,p) route. Besides having the advantages of simplicity in radiochemical processing and minimum radioactive waste generation, use of the proposed production route in place of the traditional ³²S(n,p)³²P route would result in better utilization of irradiation volume of research reactors.
authors.affiliation: Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
authors.forename: K V
authors.initials: KV
authors.lastname: Vimalnath
authors.forename: Priyalata
authors.initials: P
authors.lastname: Shetty
authors.forename: Sudipta
authors.initials: S
authors.lastname: Chakraborty
authors.forename: Tapas
authors.initials: T
authors.lastname: Das
authors.forename: Viju
authors.initials: V
authors.lastname: Chirayil
authors.forename: H D
authors.initials: HD
authors.lastname: Sarma
authors.forename: K C
authors.initials: KC
authors.lastname: Jagadeesan
authors.forename: P V
authors.initials: PV
authors.lastname: Joshi
mesh_terms: D000818:Animals; D006801:Humans; D059352:Musculoskeletal Pain / Q000517:prevention & control*; D009502:Neutrons; D063065:Organophosphonates / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010166:Palliative Care; D010710:Phosphates / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011854:Radiochemistry; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: D063065:Organophosphonates; D010710:Phosphates; D019275:Radiopharmaceuticals; C018279:sodium phosphate