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Composition in injectable aqueous solution form with specific pH value, useful to treat diabetes, comprises basal insulin with specific isoelectric point and polyamino acid bearing carboxylate charges and substituted with hydrophobic group
专利权人:
ADOCIA;ADOCIA
发明人:
SOULA OLIVIER,OLIVIER SOULA
申请号:
FR1250224
公开号:
FR2985429A1
申请日:
2012.01.09
申请国别(地区):
FR
年份:
2013
代理人:
摘要:
Composition in the form of an injectable aqueous solution having a pH of 6-8, comprises a basal insulin having an isoelectric point of 5.8-8.5, and a polyamino acid bearing carboxylate charges and substituted with hydrophobic groups. Composition in the form of an injectable aqueous solution having a pH of 6-8, comprises a basal insulin having an isoelectric point of 5.8-8.5, and a polyamino acid bearing carboxylate charges and substituted with hydrophobic groups, of formula (R1-[NH-CH(A-C(=O)-R)-C(=O)] n-[NH-CH(A-C(=O)-R3)-C(=O)] m-R2) (I). A, B1 : -CH 2- (aspartic unit) or -CH 2-CH 2- group (glutamic unit); R1 : H, linear 2-10C-acyl, branched 3-10C-acyl, benzyl, terminal amino acid unit or pyroglutamate unit; R2 : -N(R1a)(R2a); either R1a, R2a : 1-10C-alkyl or benzyl; or NR1aR2a : one or more optionally saturated and/or aromatic rings, which are carbon-based and/or which optionally comprise heteroatoms consisting of O, N or S; R3 : H or a cationic entity comprising metal cations; R : monovalent radical of formula (-NH-CH(B1-C(=O)-O-R11)-C(=O)-O-R11) or (-NH-CH(R5)-C(=O)-O-R11), or R11; R11 : linear or branched 8-30C-radical (optionally saturated and optionally contains heteroatoms) or a radical capable of forming carbonaceous rings, which are optionally saturated and/or aromatic and optionally contain hetero atoms, where the rings are optionally ortho-condensed or peri-condensed; R5 : H, 1-4C-alkyl or a benzyl group; and n/(n+m) : = 1-50 mol.%, where n/(n+m) represents molar degree of grafting with hydrophobic radical of the monomeric units, n+m represents the degree of polymerization of the polyamino acid, i.e. the average number of monomeric units per chain of polyamino acid, and the n+m is 5-1000. Independent claims are included for a single-dose formulation at a pH of 7-7.8, comprising the basal insulin and a prandial insulin, or the basal insulin and a gut hormone, or the basal insulin, the prandial insulin and the gut hormone. ACTIVITY : Antidiabetic. MECHANI
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