Composition of polyethylene glycol maleimide derivative and polymerization inhibitor
AssigneeJenkem Technology Co., Ltd. (Beijing)
InventorsHui ZHU, Meina LIN, Zhen WEI, Xuan ZHAO
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Abstract
The present invention provides a composition of a polyethylene glycol maleimide derivative and a polymerization inhibitor. In particular, the present invention provides a composition of an 8-arm polyethylene glycol maleimide derivative and a phenolic polymerization inhibitor. The ingredient and content of the polymerization inhibitor in the composition are reasonably chosen, thereby significantly increasing stability of the polyethylene glycol maleimide derivative, effectively avoiding the undesirable effect of gel solidifying due to polymerization during storage and transportation, and extending a pot life and shelf life of a product thereof.
Claims18
A composition of a polyethylene glycol maleimide derivative and a polymerization inhibitor, wherein the mass ratio of the polymerization inhibitor to the polyethylene glycol maleimide derivative is ≥0.1 μg:1 g, the polyethylene glycol maleimide derivative contains at least one terminal maleimide group.
A pharmaceutical composition comprising a polymerization inhibitor and a conjugate of a polyethylene glycol maleimide derivative and a drug;
- preferably, the drug is selected from the group consisting of amino acids, polypeptides, proteins, sugars, organic acids, alkaloids, flavonoids, terpenoids, terpenoids, phenylpropanoid phenols, steroids and steroids;
- more preferably the drug is a polypeptide or protein drug;
- further preferably, the polypeptide or protein drug contains free a sulfhydryl group;
- and/or a sulfhydryl group is introduced at a specific site in the polypeptide or protein drug;
- preferably, the polymerization inhibitor is a phenolic polymerization inhibitor, more preferably the polymerization inhibitor is one or more of:
- hydroquinone, p-t-butyl phenol, methyl hydroquinone, p-tert-butyl catechol, 2-tert-butyl hydroquinone, 2, 5-di-tert-butyl hydroquinone, 4-methoxyphenol, 2,6-di-tert-butyl-4-methylphenol, 4,4′-dihydroxybiphenyl, pyrogallol and bisphenol A, most preferably the polymerization inhibitor is hydroquinone and/or p-tert-butyl phenol.
Dependencies are inferred from the claim text.