Claims for Patent: 8,986,653

Summary for Patent: 8,986,653

Title:	Labeled iodinated tropane formulation
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 [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l)nortropane.
Inventor(s):	Sterzinger; Chris (Vancouver, CA), Ferreira; Cara (Vancouver, CA), Leyh; David (Vancouver, CA), Thorn; Richard (Boston, MA)
Assignee:	Alseres Pharmaceuticals, Inc. (Hopkinton, MA)
Application Number:	14/044,267
Patent Claims:	1. A method of preparing [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) nortropane comprising the steps of: (a) preparing a precursor solution comprising 2.beta.-Carbomethoxy-3.beta.-(4-fluorophenyl)-N-(3-tributyltin-E-allyl) nortropane, ethanol, hydrogen peroxide, and phosphate buffer; (b) preparing a sodium [.sup.123I]-iodide solution comprising sodium [.sup.123I]-iodide and trifluoroacetic acid having a pH of less than about 2; and (c) heating a mixture of precursor solution and sodium [.sup.123I]-iodide solution at a temperature of about 80.degree. C. for about 15 minutes, wherein the resulting [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) nortropane is stable for at least 48 hours. 2. A method of preparing an aqueous solution of [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) nortropane comprising the steps of: (a) eluting the [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) 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 [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) nortropane is stable for at least 48 hours. 3. A method of preparing an aqueous solution of [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) nortropane comprising the steps of: (a) eluting a solution of [.sup.123I]-2.beta.-carbomethoxy-3.gamma.-(4-flurophenyl)-N-(3-iodo-E-all- yl) 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 [.sup.123I]-2.beta.-carbomethoxy-3.beta.-(4-flurophenyl)-N-(3-iodo-E-ally- l) nortropane is stable for at least 48 hours.

Details for Patent 8,986,653

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2027-10-31