Labeled iodinated tropane formulation
AssigneeAlseres Pharmaceuticals, Inc.
InventorsChris Sterzinger, Cara Ferreira, David Leyh, Richard Thorn
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Abstract
A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl)nortropane.
Claims3
A method of preparing [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane comprising the steps of:
- (a) preparing a precursor solution comprising 2β-Carbomethoxy-3β-(4-fluorophenyl)-N-(3-tributyltin-E-allyl) nortropane, ethanol, hydrogen peroxide, and phosphate buffer;
- (b) preparing a sodium [123I]-iodide solution comprising sodium [123I]-iodide and trifluoroacetic acid having a pH of less than about 2;
- and
- (c) heating a mixture of precursor solution and sodium [123I]-iodide solution at a temperature of about 80° C. for about 15 minutes, wherein the resulting [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane is stable for at least 48 hours.
A method of preparing an aqueous solution of [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane comprising the steps of:
- (a) eluting the [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane through a C18 preparative HPLC column with an eluent, wherein the eluent comprises about 15% (v/v) ethanol;
- and
- (b) collecting the product peak in sodium chloride in an acetic acid buffer, wherein the radioactive concentration of the resulting solution is at least about 23 mCi/mL, and wherein the resulting [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane is stable for at least 48 hours.
A method of preparing an aqueous solution of [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane comprising the steps of:
- (a) eluting a solution of [123I]-2β-carbomethoxy-3γ-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane through a C18 preparative HPLC column with an eluent, wherein the eluent comprises about 80% (v/v) ethanol, and about 20% ascorbic acid (20 g/L) in sterile water for injection;
- and
- (b) collecting the product peak in sodium chloride in an acetic acid buffer, wherein the radioactive concentration of the resulting solution is at least about 20 mCi/mL, and wherein the resulting [123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane is stable for at least 48 hours.
Dependencies are inferred from the claim text.