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US 2016/0101196 A1Published application
Contrast medium formulation and related preparation method
AssigneeGuerbet
InventorsChristelle Medina, Monique Sabatou, Anne Petit, Marc Port
Life of this patent
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Abstract
The present invention relates to a liquid pharmaceutical composition including a complex of formula (I), in which M is an ion of a paramagnetic metal and R1 to R3, X1 to X3 and K1 to K12 are such as defined in claim 1, said composition also including a calcium complex of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid. The invention also relates to the preparation method thereof and to an imaging method involving said composition.
Claims16
A liquid pharmaceutical composition comprising a complex of formula (I):
- in which R1, R2 and R3 represent —COOH,
- X1, X2 and X3 represent, independently of one another, L-Y in which L represents a C1-C3 alkylene group, preferably (CH2)n with n=1 to 3, and Y represents —CONH2, —CO—NR7R8 or —NR7—CO—R8, in which R7 represents H or a C1-C6 alkyl group or a C1-C6 hydroxyalkyl group, which is in particular C2-C4, advantageously —CH2—CH2OH, —CHOH—CH2OH, —CH—(CH2OH)2, —(CH2)m—(CHOH)p—CH2OH with m=1 to 3, p=1 to 4 and m+p=2 to 5 or —C—(CH2OH)3 and R8 represents a C1-C6 alkyl or C1-C6 hydroxyalkyl group, which is in particular C2-C4, advantageously —CH2—CH2OH, —CHOH—CH2OH, —CH—(CH2OH)2, —(CH2)m—(CHOH)p—CH2OH with m=1 to 3, p=1 to 4 and m+p=2 to 5 or —C—(CH2OH)3, provided that at least R7 or R8 represents a C1-C6 hydroxyalkyl group;
- D represents CH or N;
- E represents CH or N;
- F1 represents CH or N;
- K1 to K12 each independently represent H, —(CH2)j—CH3 or —(CH2)i—OH in which j=0 to 3 and i=1 to 3, advantageously H, or K3 or K4 with K5 or K6, and/or K7 or K8 with K9 or K10 forming a ring having 3 to 6 carbon atoms;
- and
- M represents an ion of a paramagnetic metal;
- or an enantiomer or a diastereoisomer (preferentially chosen from the RRS, RSR and RSS diastereoisomers) thereof or mixtures thereof,
- said composition also comprising a calcium complex of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, and having a concentration of free paramagnetic metal of less than 1 ppm (m/v), preferentially less than 0.5 ppm (m/v).
7 more elements
Dependencies are inferred from the claim text.