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Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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From each fraction, a ~1 g aliquot was taken by weight into 20 mL LSC<br />

vials. Volumes of 1.5 mL deionized water <strong>and</strong> 10 mL of Ultima Gold AB liquid<br />

scintillator were added into each vial. Measurements were carried out using a<br />

Wallac 1411 spectrometer. The spectra of these three fractions are shown in<br />

Fig. 9.1.<br />

Fraction 1 contained the total <strong>90</strong> Sr activity with a few counts of <strong>90</strong> Y owing<br />

to the decay of <strong>90</strong> Sr during collection of the <strong>90</strong> Sr fraction <strong>and</strong> measurement.<br />

Fractions 2 <strong>and</strong> 3 did not contain any activity. The spectra showed only<br />

background counts.<br />

The relationship between the added <strong>and</strong> measured <strong>90</strong> Sr activity is shown<br />

in Fig. 9.2. The intersection point of the straight line with the ordinate axis<br />

determines the <strong>90</strong> Sr activity in <strong>90</strong> Y used <strong>for</strong> validation. The determination limit<br />

of <strong>90</strong> Sr in 230 MBq of <strong>90</strong> Y was equal to 3.5 × 10 –6 % <strong>for</strong> a measurement time of<br />

200 s. This limit can be lowered to 1×10 –6 % <strong>for</strong> a 3600 s measurement time.<br />

9.2. COMPARISON OF METHODS FOR<br />

CHROMATOGRAPHIC SEPARATION OF DMSA COMPLEXES<br />

WITH 99m Tc AND <strong>188</strong> Re IN (III) AND (V) OXIDATION STATES;<br />

IMPLICATIONS OF PRODUCT DEVELOPMENT<br />

(IN COLLABORATION WITH VINČA INSTITUTE OF<br />

NUCLEAR SCIENCES, BELGRADE, SERBIA)<br />

The reliable method <strong>for</strong> determination of RCP is key to the success of<br />

further radiopharmaceutical development. This is especially relevant when more<br />

than one type of radiometal lig<strong>and</strong> complex can be <strong>for</strong>med during labelling. In the<br />

case of DMSA complexes with 99m Tc or <strong>188</strong> Re, depending on the pH, the metal can<br />

occur at +3 or +5 oxidation states [9.6]. Although, the European Pharmacopoeia<br />

monograph [9.7] describes RCP tests <strong>for</strong> 99m Tc(III) DMSA based on ITLC SG<br />

chromatography, this method is not specific <strong>for</strong> distinct <strong>for</strong>ms of complex <strong>and</strong><br />

allows only determination of free 99m Tc pertechnetate. Both 99m Tc(III) DMSA<br />

<strong>and</strong> 99m Tc(V) DMSA are retained at the origin similar to colloidal residues of<br />

99m Tc. The method proposed by Westera et al. [9.8] utilizing SG coated plates<br />

<strong>and</strong> BuOH:H 2 O:acetic acid (3:3:2) allows separation of 99m Tc(III) DMSA from<br />

99m Tc(V) DMSA complexes in a separation process lasting 2 h, but still does not<br />

allow determination of technetium tin colloid (BuOH = butanol).<br />

The goal of this work was to evaluate possibilities <strong>for</strong> optimization<br />

of chromatographic systems leading to a one step analytical method <strong>for</strong><br />

determination of the RCP of DMSA complexes with 99m Tc or <strong>188</strong> Re.<br />

137

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