Claims for Patent: 12,527,884

Summary for Patent: 12,527,884

Title:	Use of cyclodextrins as a radiostabilizer
Abstract:	The present invention provides a radiopharmaceutical composition comprising the following four components: (i) a radio-labelled compound; (ii) ethanol; (iii) a stabilizer of the radio-labelled compound; and (iv) a cyclodextrin.The present invention also provides a radiopharmaceutical composition comprising: (i) a radio-labelled compound; (ii) a stabilizer of the radio-labelled compound, wherein the stabilizer comprises: ascorbic acid, aspartic acid, cysteine, maleic acid, gentisic acid, glutathione, glutamic acid, mannitol, nicotinamide, calcium chloride, N-t-butyl-alpha-phenylnitrone (PBN), tartaric acid, para-aminobenzoic acid (pABA), chloride ions or salts or combinations thereof; and (iii) a cyclodextrin.
Inventor(s):	Kristine Opsvik WIKENE, IMTIAZ Ahmed KHAN, Graeme McRobbie
Assignee:	GE Healthcare Ltd
Application Number:	US17/770,908
Patent Claims:	1. A radiopharmaceutical composition, comprising: (i) a radio-labelled compound selected from [18F] flurpiridaz, and a pharmaceutically acceptable salt thereof; (ii) ethanol in an amount from about 5 to about 10% (v/v); (iii) ascorbic acid in an amount from about 30 to about 50 mg/mL, wherein the ascorbic acid is a stabilizer of the radio-labelled compound; and (iv) hydroxypropyl-beta-cyclodextrin (HPbCD) in an amount of from about 40 to about 47 mg/mL, wherein HPbCD is a co-stabilizer of the radio-labelled compound. 2. A method of imaging a subject in need thereof, comprising: intravenously administering the radiopharmaceutical composition of claim 1; and acquiring an at least one image from the subject after the administration. 3. A method of positron emission tomography (PET) imaging in a subject in need thereof, comprising intravenously administering the radiopharmaceutical composition of claim 1; and acquiring at least one PET image from the subject after the administration. 4. The radiopharmaceutical composition of claim 1, wherein the ethanol is present in an amount of 7% (v/v). 5. The radiopharmaceutical composition of claim 1, wherein the pH of the composition is 4.5 to 9.5. 6. A stable radiopharmaceutical composition suitable for mammalian administration comprising: [18F] flurpiridaz; about 7% ethanol; about 30 to about 50 mg/mL ascorbic acid; and about 40 to about 47 mg/mL hydroxypropyl-beta-cyclodextrin (HPbCD), wherein the radio chemical purity of the stable radiopharmaceutical composition at 8 hours is 95% or more as measured by HPLC.