US 2026/0306431 A1 · SULFURIZED IMIDAZOLES IN OPHTHALMIC FORMULATIONS

Abstract

In the embodiments, ophthalmic formulations comprise 0.001-2% (w/v) of L-Ergothioneine or derivatives of L-Ergothioneine, optionally combined with compatible toxicity agents. L-ergothioneine or derivatives of L-Ergothioneine in the ophthalmic formulation is: (1) an active pharmaceutical ingredient (API) for treating oxidative stress-related ocular disorders; and (2) an inactive excipient for use as a stabilizing excipient to enhance bioavailability and prolong shelf-life of co-administered APIs. L-ergothioneine or derivatives of L-ergothioneine in the ophthalmic solution, when applied on an ocular surface, exhibit: improved corneal permeability; reduced degradation of thermolabile components; and synergistic therapeutic effects when used with other neuroprotective agents, as the co-formulated APIs, in the ophthalmic formulations.

Claims20

Dependent claims

An ophthalmic formulation comprising:

a pharmaceutically acceptable aqueous delivery vehicle comprises:
an active ingredient with biological activity or therapeutic effect associated with a labile drug introduced into ocular tissue, wherein the active ingredient is spermine and wherein spermine is present in an amount of 0.01-0.1% (w/v) in the ophthalmic formulation;
L-Ergothioneine (EGT) in a concentration of 0.005% to 0.5% (w/v) of the formulation, wherein the EGT is present in a concentration wherein the EGT behaves as an excipient that:
inhibits degradation of the active ingredient introduced into the ocular tissue, and
inductively expresses OCTN1, thereby increasing bioavailability of the active ingredient.

2 more elements

Dependencies are inferred from the claim text.

Sulfurized imidazoles in ophthalmic formulations

Life of this patent

Sulfurized imidazoles in ophthalmic formulations

Life of this patent

Abstract

Claims20