| 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 : -NHR4, or benzyl or linear or branched 2-30C-acyl (both optionally include heteroatoms consisting of N, O or S); R4 : H, 2-30C-alkyl or branched 3-10C-acyl; 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 mole%, 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 single-dose formulations at a pH of between 7 and 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. MECHANISM OF ACTION : None given. |
