Ascorbic Acid Stabilization of Re-188- and I-131-Radiolabeled Peptides for Radiotherapy

Guhlke, Stefan; Zamora, Paul O.; Sartor, J.; Knapp, F.F.; Rhodes, Buck A.; Biersack, H.-J.

doi:10.1524/ract.1997.79.2.93

Cited by 4 publications

(2 citation statements)

References 11 publications

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“…Carrier added 188 Re(V)-DMSA was prepared according to the method of Bisundan et al [4] and modified by addition of ascorbic acid for protection against radiolysis [1,17]. Briefly, 1 ml of generator eluate was added to 10 mg DMSA (Aldrich), 0.5 mg (50 µl of a 10 mg/ml solution) ammonium perrhenate (Aldrich) and 5 mg ascorbic acid (Aldrich).…”

Section: Methodsmentioning

confidence: 99%

¹⁸⁸Re(V)-DMSA: in-vitro and in-vivo studies on the individual stereo isomers

Guhlke¹,

Scheithauer²,

Oetjen³

et al. 2004

Radiochimica Acta

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188 Re(V)-DMSA; Re-188 / Stereo isomers / Radio-therapy Summary. The pentavalent rhenium-188 meso-dimercaptosuccinic acid complex 188 Re(V)-DMSA is a beta-emitting analogue of Tc99 m (V)-DMSA, an established tracer that is taken up in a variety of histological different tumors and especially in bone metastases arising from breast and prostate carcinomas. The similar general biodistribution and tumor avidity of 188 Reand 99m Tc(V)-DMSA therefore suggests the use of the rhenium analog as an agent for therapeutic applications. No-carrier-added 188 Re(V)-DMSA is composed of a mixture of three stereoisomers arising from different orientations of the 4 carboxylate groups of the complex. For therapeutic applications it must be known whether there is a difference in the in-vivo biodistribution and kinetics of the individual stereo isomers. The aim of this study was therefore a) to characterize the chemical stability of each of the 3 stereoisomers with respect to time, temperature and pH and b) to evaluate if there are differences in the in-vivo organ distribution of the pure isomers compared to the isomeric mixture.The in-vitro results revealed for all three individual isomers of 188 Re(V)-DMSA a rather slow (with respect to half-life of Re-188) temperature and pH dependent rate of interconversion which would justify the application of pure isomers. The data obtained from urine samples of rats showed a faster interconversion rate and reached a stable isomer distribution after about six to ten hours, depending on which isomer was injected. However there was no evidence for isomer specific excretion rates. The organ biodistribution patterns of all three isomers were very similar at all times studied (10 min up to 24 hours p.i). The tumor uptake in a rat mammary carcinoma model at 1 hour p.i. did also not show any significant differences.In conclusion the preparation and administration of pure stereoisomers of 188 Re-DMSA is possible, however, in-vivo no significant differences in organ distribution and kinetics were observed which would favour the use of purified stereo isomers over the isomeric mixture of 188 Re(V)-DMSA.

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Section: Methodsmentioning

confidence: 99%

¹⁸⁸Re(V)-DMSA: in-vitro and in-vivo studies on the individual stereo isomers

Guhlke¹,

Scheithauer²,

Oetjen³

et al. 2004

Radiochimica Acta

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“…Some investigators have described the use of ascorbic acid, gentisic acid or a-tocopherol. [31][32][33] The most commonly used antioxidant is ascorbic acid. A combination of ascorbic acid and gentisic acid could also be used for example.…”

Section: Additivesmentioning

confidence: 99%

A kit formulation for the labelling of lipiodol with generator‐produced ¹⁸⁸Re

Lepareur

Garin

Noiret

et al. 2004

Labelled Comp Radiopharmac

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SummaryA lyophilised kit formulation for the efficient labelling of lipiodol with generatorproduced Radiochemical purity (RCP) was greater than 90% and the yield of extraction was about 88%. The role of the different kit components has been studied in detail to find the most efficient formulation (amount of reducing agent, antioxidant). The use of 0.8 mg of stannous chloride, with 40 mg of potassium oxalate and 30 mg of ascorbic acid, was found necessary. The stability of the 188 Re-radiolabelled lipiodol has been investigated, in the presence of plasma. The radiolabelled lipiodol ( 188 Re-SSS lipiodol) is stable at least 48 h (RCP=91.0 AE 4.0%).

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